The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27452283 |
241 |
Robust design of some selective matrix metalloproteinase-2 inhibitors over matrix metalloproteinase-9 through in silico/fragment-based lead identification and de novo lead modification: Syntheses and biological assays. |
Jadavpur University |
26871660 |
68 |
Discovery of a new selective inhibitor of A Disintegrin And Metalloprotease 10 (ADAM-10) able to reduce the shedding of NKG2D ligands in Hodgkin's lymphoma cell models. |
San Raffaele Scientific Institute |
26653735 |
81 |
Discovery of N-(4-Fluoro-3-methoxybenzyl)-6-(2-(((2S,5R)-5-(hydroxymethyl)-1,4-dioxan-2-yl)methyl)-2H-tetrazol-5-yl)-2-methylpyrimidine-4-carboxamide. A Highly Selective and Orally Bioavailable Matrix Metalloproteinase-13 Inhibitor for the Potential Treatment of Osteoarthritis. |
Pfizer |
26753813 |
22 |
Design and synthesis of an activity-based protein profiling probe derived from cinnamic hydroxamic acid. |
University of Minnesota |
26263024 |
47 |
N-O-Isopropyl Sulfonamido-Based Hydroxamates as Matrix Metalloproteinase Inhibitors: Hit Selection and in Vivo Antiangiogenic Activity. |
Universit£ |
25264600 |
64 |
Discovery of novel, highly potent, and selective quinazoline-2-carboxamide-based matrix metalloproteinase (MMP)-13 inhibitors without a zinc binding group using a structure-based design approach. |
Takeda Pharmaceutical |
25265401 |
38 |
Targeting matrix metalloproteinases: exploring the dynamics of the s1' pocket in the design of selective, small molecule inhibitors. |
Universidad Ceu San Pablo |
25192810 |
66 |
Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1¿ binding site. |
Takeda Pharmaceutical |
24735644 |
19 |
Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, substrate-dependent modulators of insulin-degrading enzyme in amyloid-ß hydrolysis. |
University of Lille |
23376997 |
53 |
Arylsulfonamide inhibitors of aggrecanases as potential therapeutic agents for osteoarthritis: synthesis and biological evaluation. |
Universit£ |
23375794 |
220 |
Synthesis and structure-activity relationship analysis of caffeic acid amides as selective matrix metalloproteinase inhibitors. |
Nanjing University of Chinese Medicine |
23353736 |
41 |
Synthesis of derivatives of methyl rosmarinate and their inhibitory activities against matrix metalloproteinase-1 (MMP-1). |
Second Military Medical University |
23287054 |
46 |
Sulphonamides: Deserving class as MMP inhibitors? |
Indian Institute of Technology (Bhu) |
23458498 |
24 |
Synthesis and preliminary evaluation in tumor bearing mice of new (18)F-labeled arylsulfone matrix metalloproteinase inhibitors as tracers for positron emission tomography. |
Universit£ |
17275314 |
701 |
Matrix metalloproteinases (MMPs): chemical-biological functions and (Q)SARs. |
Pomona College |
23134659 |
74 |
Design and synthesis of procollagen C-proteinase inhibitors. |
Fibrogen |
22891645 |
83 |
Discovery of highly potent and selective small molecule ADAMTS-5 inhibitors that inhibit human cartilage degradation via encoded library technology (ELT). |
Glaxosmithkline |
21780776 |
40 |
Remarkable potential of thea-aminophosphonate/phosphinate structural motif in medicinal chemistry. |
Wroclaw University of Technology |
21413800 |
56 |
A one-pot synthesis and biological activity of ageladine A and analogues. |
Macquarie University |
22737278 |
44 |
Structure-Activity Relationship for Thiirane-Based Gelatinase Inhibitors. |
TBA |
22658537 |
76 |
Natural products as a gold mine for selective matrix metalloproteinases inhibitors. |
East China University of Science and Technology |
22175799 |
22 |
Discovery and evaluation of a non-Zn chelating, selective matrix metalloproteinase 13 (MMP-13) inhibitor for potential intra-articular treatment of osteoarthritis. |
Alantos Pharmaceuticals |
22342144 |
72 |
Antidotes to anthrax lethal factor intoxication. Part 3: Evaluation of core structures and further modifications to the C2-side chain. |
Panthera Biopharma |
19715320 |
87 |
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. |
University of Florida |
19635666 |
119 |
Discovery of novel selective HER-2 sheddase inhibitors through optimization of P1 moiety. |
Incyte |
19095454 |
63 |
Current perspective of TACE inhibitors: a review. |
The M. S. University of Baroda |
17981034 |
51 |
1-Hydroxy-2-pyridinone-based MMP inhibitors: synthesis and biological evaluation for the treatment of ischemic stroke. |
Johnson & Johnson Pharmaceutical Research and Development |
18053726 |
364 |
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality. |
Johnson & Johnson Pharmaceutical Research & Development |
17980583 |
46 |
Syntheses and in vitro evaluation of arylsulfone-based MMP inhibitors with heterocycle-derived zinc-binding groups (ZBGs). |
Johnson & Johnson Pharmaceutical Research and Development |
18086526 |
85 |
beta-N-Biaryl ether sulfonamide hydroxamates as potent gelatinase inhibitors: part 1. Design, synthesis, and lead identification. |
Johnson & Johnson Pharmaceutical Research and Development |
18257543 |
16 |
Carbamoylphosphonate matrix metalloproteinase inhibitors 6: cis-2-aminocyclohexylcarbamoylphosphonic acid, a novel orally active antimetastatic matrix metalloproteinase-2 selective inhibitor--synthesis and pharmacodynamic and pharmacokinetic analysis. |
The Hebrew University of Jerusalem |
18251495 |
69 |
Quinazolinones and pyrido[3,4-d]pyrimidin-4-ones as orally active and specific matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis. |
Pfizer |
18061445 |
103 |
Alpha,beta-cyclic-beta-benzamido hydroxamic acids: novel templates for the design, synthesis, and evaluation of selective inhibitors of TNF-alpha converting enzyme (TACE). |
Bristol-Myers Squibb Research and Development |
18029173 |
316 |
Synthesis and evaluation of novel heterocyclic MMP inhibitors. |
North Dakota State University |
16220969 |
219 |
Designed multiple ligands. An emerging drug discovery paradigm. |
Organon Laboratories |
15713379 |
40 |
N-i-Propoxy-N-biphenylsulfonylaminobutylhydroxamic acids as potent and selective inhibitors of MMP-2 and MT1-MMP. |
Universit£ |
15139754 |
17 |
Receptor flexibility in the in silico screening of reagents in the S1' pocket of human collagenase. |
De Novo Pharmaceuticals |
15214773 |
76 |
Fragment-based drug discovery. |
Sunesis Pharmaceuticals |
15139760 |
110 |
Carbamoylphosphonates, a new class of in vivo active matrix metalloproteinase inhibitors. 1. Alkyl- and cycloalkylcarbamoylphosphonic acids. |
The Hebrew University of Jerusalem |
12930146 |
170 |
Stereospecific synthesis of 5-substituted 2-bisarylthiocyclopentane carboxylic acids as specific matrix metalloproteinase inhibitors. |
Institut De Recherches Servier |
12773042 |
195 |
Synthesis and structure-activity relationship of N-substituted 4-arylsulfonylpiperidine-4-hydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis. |
Wyeth Research |
12773041 |
119 |
Synthesis and structure-activity relationship of alpha-sulfonylhydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis. |
Wyeth Research |
11831904 |
172 |
New type of metalloproteinase inhibitor: design and synthesis of new phosphonamide-based hydroxamic acids. |
Nippon Organon K.K. |
11472217 |
157 |
Design, synthesis, and structure-activity relationships of macrocyclic hydroxamic acids that inhibit tumor necrosis factor alpha release in vitro and in vivo. |
Dupont Pharmaceuticals |
11472202 |
143 |
Potent and selective carboxylic acid-based inhibitors of matrix metalloproteinases. |
TBA |
10669559 |
180 |
Protease inhibitors: current status and future prospects. |
University of Queensland |
10649971 |
180 |
Structure-activity relationships and pharmacokinetic analysis for a series of potent, systemically available biphenylsulfonamide matrix metalloproteinase inhibitors. |
Parke-Davis Pharmaceutical Research |
10882358 |
62 |
Hydroxamic acid derivatives as potent peptide deformylase inhibitors and antibacterial agents. |
F. Hoffmann-La Roche |
10579818 |
162 |
Design, synthesis, and biological evaluation of potent thiazine- and thiazepine-based matrix metalloproteinase inhibitors. |
Procter and Gamble Pharmaceuticals |
9888835 |
42 |
Design and synthesis of phosphinamide-based hydroxamic acids as inhibitors of matrix metalloproteinases. |
Procter and Gamble Pharmaceuticals |
9733482 |
31 |
Discovery of potent, achiral matrix metalloproteinase inhibitors. |
Procter and Gamble Pharmaceuticals |
2153207 |
31 |
Phosphoramidate peptide inhibitors of human skin fibroblast collagenase. |
University of Kentucky |
15177439 |
96 |
Pyran-containing sulfonamide hydroxamic acids: potent MMP inhibitors that spare MMP-1. |
Pfizer |
12824028 |
75 |
Phosphinic acid-based MMP-13 inhibitors that spare MMP-1 and MMP-3. |
Pfizer |
11327577 |
86 |
Heterocycle-based MMP inhibitors with P2' substituents. |
Procter and Gamble Pharmaceuticals |
11677139 |
92 |
The discovery of anthranilic acid-based MMP inhibitors. Part 3: incorporation of basic amines. |
Wyeth-Ayerst Research |
11591510 |
57 |
alpha-Alkyl-alpha-amino-beta-sulphone hydroxamates as potent MMP inhibitors that spare MMP-1. |
Pfizer |
11206468 |
24 |
Heteroaryl and cycloalkyl sulfonamide hydroxamic acid inhibitors of matrix metalloproteinases. |
Wyeth-Ayerst Research |
11206467 |
44 |
The discovery of anthranilic acid-based MMP inhibitors. Part 1: SAR of the 3-position. |
Wyeth-Ayerst Research |
11514167 |
88 |
The discovery of anthranilic acid-based MMP inhibitors. Part 2: SAR of the 5-position and P1(1) groups. |
Wyeth-Ayerst Research |
11378378 |
34 |
Arylsulphonyl hydroxamic acids: potent and selective matrix metalloproteinase inhibitors. |
Celltech-Chiroscience |
11133099 |
43 |
Synthesis and activity of selective MMP inhibitors with an aryl backbone. |
Pharmacia |
10340614 |
20 |
Macrocyclic hydroxamate inhibitors of matrix metalloproteinases and TNF-alpha production. |
Dupont Pharmaceuticals |
10450979 |
4 |
Synthesis of an array of potential matrix metalloproteinase inhibitors using a sequence of polymer-supported reagents. |
University of Cambridge |
10397503 |
40 |
Picking the S1, S1' and S2' pockets of matrix metalloproteinases. A niche for potent acyclic sulfonamide inhibitors. |
Universit£ |
9873598 |
39 |
The synthesis and biological activity of a novel series of diazepine MMP inhibitors. |
Wyeth-Ayerst Research |
22386984 |
67 |
In silico scaffold evaluation and solid phase approach to identify new gelatinase inhibitors. |
Colosseum Combinatorial Chemistry Centre For Technology (C4T Scarl) |
22175825 |
19 |
Potent inhibitors of LpxC for the treatment of Gram-negative infections. |
Pfizer |
22153941 |
140 |
Lead optimisation of selective non-zinc binding inhibitors of MMP13. Part 2. |
Astrazeneca |
22018790 |
9 |
Identification of novel, exosite-binding matrix metalloproteinase-13 inhibitor scaffolds. |
Scripps Florida |
22017539 |
75 |
Fragment-based discovery of indole inhibitors of matrix metalloproteinase-13. |
Boehringer Ingelheim Pharmaceuticals |
22017477 |
35 |
Novel 1-hydroxypiperazine-2,6-diones as new leads in the inhibition of metalloproteinases. |
Instituto Superior T£Cnico |
22082667 |
67 |
Time-dependent botulinum neurotoxin serotype A metalloprotease inhibitors. |
Microbiotix |
22088955 |
33 |
Identification of novel molecular scaffolds for the design of MMP-13 inhibitors: a first round of lead optimization. |
Universit£ |
21925881 |
60 |
Discovery of novel Cobactin-T based matrix metalloproteinase inhibitors via a ring closing metathesis strategy. |
Johnson & Johnson Pharmaceutical Research & Development |
21548582 |
57 |
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes. |
University of Illinois At Chicago |
21866961 |
28 |
Selective water-soluble gelatinase inhibitor prodrugs. |
University of Notre Dame |
20726512 |
282 |
Orally active MMP-1 sparinga-tetrahydropyranyl anda-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
Pfizer |
21514700 |
56 |
Synthesis and biological evaluation in U87MG glioma cells of (ethynylthiophene)sulfonamido-based hydroxamates as matrix metalloproteinase inhibitors. |
Universit£ |
21536437 |
219 |
Orally active achiral N-hydroxyformamide inhibitors of ADAM-TS4 (aggrecanase-1) and ADAM-TS5 (aggrecanase-2) for the treatment of osteoarthritis. |
Astrazeneca |
20638281 |
56 |
Structure and activity relationships of tartrate-based TACE inhibitors. |
Merck Research Laboratories |
21507637 |
102 |
MMP-13 selectivea-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres. |
Pfizer |
21493063 |
67 |
MMP-13 selective alpha-sulfone hydroxamates: identification of selective P1' amides. |
Pfizer |
21458257 |
87 |
2-(2-Aminothiazol-4-yl)pyrrolidine-based tartrate diamides as potent, selective and orally bioavailable TACE inhibitors. |
Merck Research Laboratories |
21417219 |
179 |
Discovery of (1S,2R,3R)-2,3-dimethyl-2-phenyl-1-sulfamidocyclopropanecarboxylates: novel and highly selective aggrecanase inhibitors. |
Central Pharmaceutical Research Institute |
21300546 |
129 |
The design and synthesis of novel N-hydroxyformamide inhibitors of ADAM-TS4 for the treatment of osteoarthritis. |
Astrazeneca |
24900296 |
38 |
Sulfonate-Containing Thiiranes as Selective Gelatinase Inhibitors |
TBA |
20965620 |
50 |
Structure-based approach to nanomolar, water soluble matrix metalloproteinases inhibitors (MMPIs). |
Protera |
21078557 |
34 |
Structure based optimization of chromen-based TNF-a converting enzyme (TACE) inhibitors on S1' pocket and their quantitative structure-activity relationship (QSAR) study. |
Yonsei University |
21106451 |
39 |
Novel TNF-a converting enzyme (TACE) inhibitors as potential treatment for inflammatory diseases. |
Merck Research Laboratories |
20529685 |
70 |
MMP-13 selective isonipecotamide alpha-sulfone hydroxamates. |
Pfizer |
20529684 |
112 |
Orally bioavailable dual MMP-1/MMP-14 sparing, MMP-13 selective alpha-sulfone hydroxamates. |
Pfizer |
20180536 |
128 |
Potent arylsulfonamide inhibitors of tumor necrosis factor-alpha converting enzyme able to reduce activated leukocyte cell adhesion molecule shedding in cancer cell models. |
Universit£ |
20172725 |
49 |
Discovery and SAR of hydantoin TACE inhibitors. |
Merck Research Laboratories |
19767207 |
17 |
Synthesis and SAR of 2-phenyl-1-sulfonylaminocyclopropane carboxylates as ADAMTS-5 (Aggrecanase-2) inhibitors. |
Central Pharmaceutical Research Institute |
20022498 |
71 |
The discovery of novel tartrate-based TNF-alpha converting enzyme (TACE) inhibitors. |
Schering-Plough Research Institute |
20005097 |
58 |
Discovery of (pyridin-4-yl)-2H-tetrazole as a novel scaffold to identify highly selective matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis. |
Pfizer |
19703773 |
63 |
The identification of beta-hydroxy carboxylic acids as selective MMP-12 inhibitors. |
Gsk Medicines Research Centre |
19775099 |
184 |
Design, synthesis, biological evaluation, and NMR studies of a new series of arylsulfones as selective and potent matrix metalloproteinase-12 inhibitors. |
Universit£ |
19725580 |
93 |
Identification of an orally efficacious matrix metalloprotease 12 inhibitor for potential treatment of asthma. |
Wyeth Research |
19606871 |
124 |
N-O-isopropyl sulfonamido-based hydroxamates: design, synthesis and biological evaluation of selective matrix metalloproteinase-13 inhibitors as potential therapeutic agents for osteoarthritis. |
Universit£ |
18835710 |
69 |
Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors. Part II: optimization of the S3' pocket. |
Schering-Plough Research Institute |
| 97 |
Inhibition of Matrix Metalloproteinases: An examination of the S1′ pocket |
TBA |
| 1 |
Asymmetric synthesis of a conformationally constrained N-phosphonoalkyl dipeptide |
TBA |
| 30 |
Amide surrogates of matrix metalloproteinase inhibitors: Urea and sulfonamide mimics |
TBA |
| 30 |
Orally active inhibitors of stromelysin-1 (MMP-3) |
TBA |
| 60 |
Inhibition of matrix metalloproteinases by P1 substituted N-carboxyalkyl dipeptides |
TBA |
| 49 |
Phosphinic acid inhibitors of matrix metalloproteinases |
TBA |
| 44 |
Rapid synthesis of novel dipeptide inhibitors of human collagenase and gelatinase using solid phase chemistry |
TBA |
| 15 |
Inhibitors of MMP-1: an examination of P1′ Cα gem-disubstitution in the N-carboxyalkylamine and glutaramide carboxylate series |
TBA |
| 12 |
Inhibitors of MMP-1: an examination of P1′ Cα gem-disubstitution in the succinamide hydroxamate series |
TBA |
| 36 |
Design, synthesis, activity, and structure of a novel class of matrix metalloproteinase inhibitors containing a heterocyclic P2′-P3′ amide bond isostere |
TBA |
| 18 |
Inhibition of matrix metalloproteinases by N-carboxyalkyl peptides containing extended alkyl residues At P1' |
TBA |
| 47 |
Hydroxamate inhibitors of human gelatinase B (92 kDa) |
TBA |
| 39 |
Hydroxamate inhibitors of the matrix metallo-proteinases (MMPs) containing novel P1′ heteroatom based modifications |
TBA |
| 19 |
Relationship between structure and bioavailability in a series of hydroxamate based metalloprotease inhibitors |
TBA |
| 15 |
Synthesis of thiophenol derivatives as inhibitors of human collagenase |
TBA |
| 11 |
Inhibitors of human collagenase: dipeptide mimetics with lactam and azalactam moieties at the P2′/P3′ position |
TBA |
| 66 |
Inhibition of matrix metalloproteinases by N-carboxyalkyl dipeptides: Enhanced potency and selectivity with substituted P1′ homophenylalanines |
TBA |
| 5 |
Inhibition of metalloproteinase by futoenone derivatives |
TBA |
| 40 |
Novel indolactam-based inhibitors of matrix metalloproteinases |
TBA |
| 14 |
Aminophosphonic acid containing inhibitors of human collagenase: modification of the P1 residue |
TBA |
| 2 |
Synthesis and biological evaluation of a library containing potentially 1600 amides / esters. A strategy for rapid compound generation and screening. |
TBA |
| 60 |
Potent and selective inhibitors of gelatinase-A 2. carboxylic and phosphonic acid derivatives |
TBA |
| 76 |
Potent and selective inhibitors of gelatinase-a 1. hydroxamic acid derivatives |
TBA |
| 26 |
Inhibition of stromelysin-1 (MMP-3) by peptidyl phosphinic acids |
TBA |
19457660 |
90 |
Compelling P1 substituent affect on metalloprotease binding profile enables the design of a novel cyclohexyl core scaffold with excellent MMP selectivity and HER-2 sheddase inhibition. |
Incyte |
19410464 |
71 |
Synthesis and activity of tryptophan sulfonamide derivatives as novel non-hydroxamate TNF-alpha converting enzyme (TACE) inhibitors. |
Wyeth Research |
19329309 |
49 |
Synthesis and biological evaluation of ((4-keto)-phenoxy)methyl biphenyl-4-sulfonamides: a class of potent aggrecanase-1 inhibitors. |
Wyeth Research |
19261472 |
16 |
Synthesis of hydroxypyrone- and hydroxythiopyrone-based matrix metalloproteinase inhibitors: developing a structure-activity relationship. |
University of California |
19053764 |
101 |
Dual inhibitors of matrix metalloproteinases and carbonic anhydrases: iminodiacetyl-based hydroxamate-benzenesulfonamide conjugates. |
Instituto Superior TéCnico |
18945617 |
50 |
Succinyl hydroxamates as potent and selective non-peptidic inhibitors of procollagen C-proteinase: design, synthesis, and evaluation as topically applied, dermal anti-scarring agents. |
Pfizer |
18790648 |
317 |
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge. |
University of Athens |
18782669 |
90 |
Introduction of the 4-(4-bromophenyl)benzenesulfonyl group to hydrazide analogs of Ilomastat leads to potent gelatinase B (MMP-9) inhibitors with improved selectivity. |
Université |
18691892 |
52 |
Discovery of betamethasone 17alpha-carbamates as dissociated glucocorticoid receptor modulators in the rat. |
Merck Research Laboratories |
17719700 |
39 |
Peptidyl 3-substituted 1-hydroxyureas as isosteric analogues of succinylhydroxamate MMP inhibitors. |
Università |
17623656 |
34 |
Discovery and characterization of a novel inhibitor of matrix metalloprotease-13 that reduces cartilage damage in vivo without joint fibroplasia side effects. |
Pfizer |
18083558 |
112 |
beta-N-Biaryl ether sulfonamide hydroxamates as potent gelatinase inhibitors: part 2. Optimization of alpha-amino substituents. |
Johnson & Johnson Pharmaceutical Research and Development |
18068976 |
132 |
Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P1' permutations. |
Incyte |
18036818 |
157 |
Design and identification of selective HER-2 sheddase inhibitors via P1' manipulation and unconventional P2' perturbations to induce a molecular metamorphosis. |
Incyte |
18029177 |
57 |
A novel series of highly selective inhibitors of MMP-3. |
Pfizer |
17591762 |
102 |
Potent and selective nonpeptidic inhibitors of procollagen C-proteinase. |
Pfizer |
17512742 |
32 |
Simultaneous presence of unsaturation and long alkyl chain at P'1 of Ilomastat confers selectivity for gelatinase A (MMP-2) over gelatinase B (MMP-9) inhibition as shown by molecular modelling studies. |
Université |
17368021 |
55 |
Hydantoins, triazolones, and imidazolones as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE). |
Bristol-Myers Squibb Pharmaceutical Research Institute |
17276676 |
112 |
A new 4-(2-methylquinolin-4-ylmethyl)phenyl P1' group for the beta-amino hydroxamic acid derived TACE inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
17256836 |
84 |
Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer. |
Incyte |
17188863 |
107 |
Discovery of novel hydantoins as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE). |
Bristol-Myers Squibb Pharmaceutical Research Institute |
17088065 |
106 |
alpha-Biphenylsulfonylamino 2-methylpropyl phosphonates: enantioselective synthesis and selective inhibition of MMPs. |
Università |
17064892 |
123 |
Identification of potent and selective TACE inhibitors via the S1 pocket. |
Wyeth Research |
17027261 |
153 |
Discovery of low nanomolar non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE). |
Bristol-Myers Squibb Pharmaceutical Research Institute |
16723229 |
108 |
Design and synthesis of butynyloxyphenyl beta-sulfone piperidine hydroxamates as TACE inhibitors. |
Wyeth Research |
16632358 |
68 |
Synthesis and SAR of alpha-sulfonylcarboxylic acids as potent matrix metalloproteinase inhibitors. |
Johnson & Johnson Pharmaceutical Research and Development |
16516469 |
39 |
A cassette-dosing approach for improvement of oral bioavailability of dual TACE/MMP inhibitors. |
Novartis Institutes For Biomedical Research |
16516466 |
175 |
Synthesis and structure-activity relationship of a novel, achiral series of TNF-alpha converting enzyme inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
16473009 |
23 |
Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
16426848 |
80 |
Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates. |
Wyeth Research |
16420030 |
38 |
Selective inhibition of matrix metalloproteinase isozymes and in vivo protection against emphysema by substituted gamma-keto carboxylic acids. |
Chinese Academy of Sciences |
16392792 |
29 |
Matrix metalloproteinase target family landscape: a chemometrical approach to ligand selectivity based on protein binding site analysis. |
Aventis Pharma Deutschland |
16289878 |
35 |
Conversion of potent MMP inhibitors into selective TACE inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
16220975 |
40 |
Receptor flexibility in de novo ligand design and docking. |
De Novo Pharmaceuticals |
16153831 |
87 |
Synthesis and SAR of highly selective MMP-13 inhibitors. |
Wyeth Research |
16084720 |
83 |
Acetylenic TACE inhibitors. Part 2: SAR of six-membered cyclic sulfonamide hydroxamates. |
Wyeth Research |
16005220 |
52 |
Identification of potent and selective MMP-13 inhibitors. |
Wyeth Research |
16002291 |
24 |
Structure-based design and synthesis of novel non-zinc chelating MMP-12 inhibitors. |
Pfizer |
15953722 |
56 |
Discovery of 3-OH-3-methylpipecolic hydroxamates: potent orally active inhibitors of aggrecanase and MMP-13. |
Pfizer |
15911259 |
49 |
Discovery of 3,3-dimethyl-5-hydroxypipecolic hydroxamate-based inhibitors of aggrecanase and MMP-13. |
Pfizer |
15908214 |
95 |
Non-hydroxamate 5-phenylpyrimidine-2,4,6-trione derivatives as selective inhibitors of tumor necrosis factor-alpha converting enzyme. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
15837315 |
13 |
A new development of matrix metalloproteinase inhibitors: twin hydroxamic acids as potent inhibitors of MMPs. |
Università |
15780611 |
74 |
Potent pyrimidinetrione-based inhibitors of MMP-13 with enhanced selectivity over MMP-14. |
Pfizer |
15745814 |
75 |
Synthesis and SAR of diazepine and thiazepine TACE and MMP inhibitors. |
Wyeth Research |
15686921 |
55 |
Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13). |
Pharmaceutical Research Institute |
15566296 |
142 |
Synthesis and structure-activity relationships of 4-alkynyloxy phenyl sulfanyl, sulfinyl, and sulfonyl alkyl hydroxamates as tumor necrosis factor-alpha converting enzyme and matrix metalloproteinase inhibitors. |
Wyeth Research |
15357971 |
228 |
Synthesis and structure-activity relationship of a novel sulfone series of TNF-alpha converting enzyme inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
15341955 |
52 |
Synthesis and evaluation of novel oxazoline MMP inhibitors. |
North Dakota State University |
15324896 |
71 |
3-Hydroxy-4-arylsulfonyltetrahydropyranyl-3-hydroxamic acids are novel inhibitors of MMP-13 and aggrecanase. |
Pfizer |
15261259 |
48 |
Benzodiazepine inhibitors of the MMPs and TACE. Part 2. |
Wyeth Research |
15055993 |
30 |
Azasugar-based MMP/ADAM inhibitors as antipsoriatic agents. |
Hokkaido Collaboration Center N-21 |
15006405 |
20 |
Synthesis and biological activity of selective azasugar-based TACE inhibitors. |
Organon K.K. |
14711305 |
26 |
Evaluation of P1'-diversified phosphinic peptides leads to the development of highly selective inhibitors of MMP-11. |
University of Athens |
14684295 |
109 |
Tetrahydroisoquinoline based sulfonamide hydroxamates as potent matrix metalloproteinase inhibitors. |
Chinese Academy of Sciences |
14643313 |
132 |
Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 2: lead optimization. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
14643312 |
39 |
Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 1: lead identification. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
12951101 |
79 |
Synthesis and biological activity of piperazine-based dual MMP-13 and TNF-alpha converting enzyme inhibitors. |
Pfizer |
12877590 |
28 |
A potent, selective inhibitor of matrix metalloproteinase-3 for the topical treatment of chronic dermal ulcers. |
Pfizer |
12873518 |
81 |
Acetylenic TACE inhibitors. Part 1. SAR of the acyclic sulfonamide hydroxamates. |
Wyeth Research |
12873505 |
20 |
Design, synthesis and evaluation of novel azasugar-based MMP/ADAM inhibitors. |
Hokkaido Collaboration Center |
12873504 |
36 |
Structure--activity relationships of azasugar-based MMP/ADAM inhibitors. |
Hokkaido Collaboration Center |
12824039 |
56 |
Novel inhibitors of procollagen C-proteinase. Part 2: glutamic acid hydroxamates. |
Combichem |
12798337 |
6 |
Synthesis of radiolabeled biphenylsulfonamide matrix metalloproteinase inhibitors as new potential PET cancer imaging agents. |
Indiana University School of Medicine |
12781190 |
113 |
Discovery of N-hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamides as potent and selective inhibitors of tumor necrosis factor-alpha converting enzyme (TACE). |
Bristol-Myers Squibb Pharmaceutical Research Institute |
12781187 |
15 |
Discovery of selective phosphonamide-based inhibitors of tumor necrosis factor-alpha converting enzyme (TACE). |
Organon K.K. |
12729664 |
14 |
Improved gelatinase a selectivity by novel zinc binding groups containing galardin derivatives. |
Université |
12723945 |
167 |
Design, synthesis, and evaluation of benzothiadiazepine hydroxamates as selective tumor necrosis factor-alpha converting enzyme inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
12668018 |
138 |
Synthesis and SAR of bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors. |
Wyeth-Ayerst Research |
12408705 |
73 |
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships. |
Bristol-Myers Squibb |
12270165 |
80 |
Benzodiazepine inhibitors of the MMPs and TACE. |
Wyeth Research |
11992783 |
78 |
Synthesis and biological activity of selective pipecolic acid-based TNF-alpha converting enzyme (TACE) inhibitors. |
Pfizer |
11934588 |
69 |
Anthranilate sulfonamide hydroxamate TACE inhibitors. Part 2: SAR of the acetylenic P1' group. |
Wyeth-Ayerst Research |
11934587 |
19 |
Anthranilate sulfonamide hydroxamate TACE inhibitors. Part 1: Structure-based design of novel acetylenic P1' groups. |
Wyeth-Ayerst Research |
11844676 |
48 |
Encounter with unexpected collagenase-1 selective inhibitor: switchover of inhibitor binding pocket induced by fluorine atom. |
Organon K.K. |
11831905 |
33 |
New strategy for antedrug application: development of metalloproteinase inhibitors as antipsoriatic drugs. |
Organon K.K. |
11814800 |
14 |
Design and synthesis of dual inhibitors for matrix metalloproteinase and cathepsin. |
Organon K.K. |
11754593 |
148 |
Phenoxyphenyl sulfone N-formylhydroxylamines (retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors. |
Abbott Laboratories |
11738583 |
45 |
Potent P1' biphenylmethyl substituted aggrecanase inhibitors. |
Bristol-Myers Squibb Pharma |
11708926 |
84 |
Design of selective and soluble inhibitors of tumor necrosis factor-alpha converting enzyme (TACE). |
Glaxosmithkline |
11677124 |
67 |
Discovery of selective hydroxamic acid inhibitors of tumor necrosis factor-alpha converting enzyme. |
Abbott Laboratories |
11591509 |
46 |
alpha-Amino-beta-sulphone hydroxamates as potent MMP-13 inhibitors that spare MMP-1. |
Pfizer |
11585440 |
76 |
Discovery of macrocyclic hydroxamic acids containing biphenylmethyl derivatives at P1', a series of selective TNF-alpha converting enzyme inhibitors with potent cellular activity in the inhibition of TNF-alpha release. |
Dupont Pharmaceuticals |
11585439 |
44 |
Design and synthesis of a series of (2R)-N(4)-hydroxy-2-(3-hydroxybenzyl)-N(1)- [(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide derivatives as potent, selective, and orally bioavailable aggrecanase inhibitors. |
Dupont Pharmaceuticals |
11563922 |
147 |
Structure-based design and synthesis of potent matrix metalloproteinase inhibitors derived from a 6H-1,3,4-thiadiazine scaffold. |
UniversitäT Bielefeld |
11551755 |
18 |
Asymmetric synthesis of BB-3497--a potent peptide deformylase inhibitor. |
British Biotech Pharmaceuticals |
11543676 |
45 |
Design and synthesis of matrix metalloproteinase inhibitors guided by molecular modeling. Picking the S(1) pocket using conformationally constrained inhibitors. |
Université |
11543675 |
104 |
N-Aryl sulfonyl homocysteine hydroxamate inhibitors of matrix metalloproteinases: further probing of the S(1), S(1)', and S(2)' pockets. |
Université |
11514157 |
48 |
N-hydroxyformamide peptidomimetics as TACE/matrix metalloprotease inhibitors: oral activity via P1' isobutyl substitution. |
Glaxosmithkline |
11454461 |
111 |
The development of new carboxylic acid-based MMP inhibitors derived from a cyclohexylglycine scaffold. |
Procter and Gamble Pharmaceuticals |
11428927 |
117 |
A new concept for multidimensional selection of ligand conformations (MultiSelect) and multidimensional scoring (MultiScore) of protein-ligand binding affinities. |
The Royal Danish School of Pharmacy |
11412980 |
48 |
Discovery and characterization of the potent, selective and orally bioavailable MMP inhibitor ABT-770. |
Abbott Laboratories |
11412979 |
67 |
Biaryl ether retrohydroxamates as potent, long-lived, orally bioavailable MMP inhibitors. |
Abbott Laboratories |
11354379 |
37 |
Design and synthesis of 2-oxo-imidazolidine-4-carboxylic acid hydroxyamides as potent matrix metalloproteinase-13 inhibitors. |
Pfizer |
11327602 |
58 |
Novel 5,5-disubstitutedpyrimidine-2,4,6-triones as selective MMP inhibitors. |
Roche Research Center |
11297453 |
173 |
Development of new carboxylic acid-based MMP inhibitors derived from functionalized propargylglycines. |
Procter and Gamble Pharmaceuticals |
11229774 |
40 |
Discovery of potent and selective succinyl hydroxamate inhibitors of matrix metalloprotease-3 (stromelysin-1). |
Pfizer |
11229773 |
73 |
Selectivity of inhibition of matrix metalloproteases MMP-3 and MMP-2 by succinyl hydroxamates and their carboxylic acid analogues is dependent on P3' group chirality. |
Pfizer |
11212095 |
65 |
General synthesis of alpha-substituted 3-bisaryloxy propionic acid derivatives as specific MMP inhibitors. |
Institut De Recherches Servier |
11150165 |
228 |
Development of new hydroxamate matrix metalloproteinase inhibitors derived from functionalized 4-aminoprolines. |
Procter and Gamble Pharmaceuticals |
10937713 |
186 |
Solid-phase synthesis of an arylsulfone hydroxamate library. |
Rhone-Poulenc Rorer |
10882354 |
19 |
Structure-based design and synthesis of a potent matrix metalloproteinase-13 inhibitor based on a pyrrolidinone scaffold. |
Pfizer |
10794702 |
340 |
Protease inhibitors: synthesis of potent bacterial collagenase and matrix metalloproteinase inhibitors incorporating N-4-nitrobenzylsulfonylglycine hydroxamate moieties. |
Università |
10669564 |
189 |
Design and synthesis of piperazine-based matrix metalloproteinase inhibitors. |
Procter and Gamble Pharmaceuticals |
10639284 |
119 |
Design, synthesis, and biological evaluation of matrix metalloproteinase inhibitors derived from a modified proline scaffold. |
University of Florida |
10579851 |
151 |
New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors. |
Astrazeneca |
10560745 |
46 |
Selective inhibition of low affinity IgE receptor (CD23) processing: P1' bicyclomethyl substituents. |
Smithkline Beecham Pharmaceuticals |
10522712 |
109 |
The synthesis and biological evaluation of non-peptidic matrix metalloproteinase inhibitors. |
British Biotech Pharmaceuticals |
10411481 |
144 |
Phosphinic pseudo-tripeptides as potent inhibitors of matrix metalloproteinases: a structure-activity study. |
Cea |
10406637 |
20 |
Synthesis and identification of conformationally constrained selective MMP inhibitors. |
Searle Discovery Research |
10360755 |
17 |
P1, P2'-linked macrocyclic amine derivatives as matrix metalloproteinase inhibitors. |
Dupont Pharmaceuticals |
10230616 |
30 |
Discovery of a novel series of selective MMP inhibitors: identification of the gamma-sulfone-thiols. |
Searle Discovery Research |
10229623 |
82 |
Synthesis of a series of stromelysin-selective thiadiazole urea matrix metalloproteinase inhibitors. |
Pharmacia and Upjohn |
10212120 |
34 |
Identification of highly selective inhibitors of collagenase-1 from combinatorial libraries of diketopiperazines. |
Affymax Research Institute |
10052961 |
24 |
Dual inhibition of phosphodiesterase 4 and matrix metalloproteinases by an (arylsulfonyl)hydroxamic acid template. |
RhôNe-Poulenc Rorer |
10021927 |
80 |
Design and synthesis of thiol containing inhibitors of matrix metalloproteinases. |
Novartis Biomedical Research Institute |
10021913 |
42 |
Inhibition of MMP-1 and MMP-13 with phosphinic acids that exploit binding in the S2 pocket. |
Pfizer |
9873712 |
109 |
Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors. |
Abbott Laboratories |
9873491 |
56 |
The design, synthesis, and structure-activity relationships of a series of macrocyclic MMP inhibitors. |
Abbott Laboratories |
9873489 |
28 |
Design and synthesis of conformationally-constrained MMP inhibitors. |
Procter and Gamble Pharmaceuticals |
9873367 |
39 |
Broad spectrum matrix metalloproteinase inhibitors: an examination of succinamide hydroxamate inhibitors with P1 C alpha gem-disubstitution. |
Abbott Laboratories |
9871728 |
27 |
The asymmetric synthesis and in vitro characterization of succinyl mercaptoalcohol and mercaptoketone inhibitors of matrix metalloproteinases. |
Wyeth-Ayerst Research |
9871727 |
58 |
Malonyl alpha-mercaptoketones and alpha-mercaptoalcohols, a new class of matrix metalloproteinase inhibitors. |
Affymax Research Institute |
9871623 |
48 |
Selective inhibition of low affinity IgE receptor (CD23) processing. |
Smithkline Beecham Pharmaceuticals |
9871622 |
36 |
Hydroxamate-based inhibitors of low affinity IgE receptor (CD23) processing. |
Smithkline Beecham Pharmaceuticals |
9871551 |
48 |
Structure-based design and synthesis of a series of hydroxamic acids with a quaternary-hydroxy group in P1 as inhibitors of matrix metalloproteinases. |
Dupont Pharmaceuticals |
9632351 |
36 |
Rational design and combinatorial evaluation of enzyme inhibitor scaffolds: identification of novel inhibitors of matrix metalloproteinases. |
Affymax Research Institute |
9599226 |
25 |
Macrocyclic amino carboxylates as selective MMP-8 inhibitors. |
Dupont Pharmaceuticals |
9599225 |
9 |
Design and synthesis of cyclic inhibitors of matrix metalloproteinases and TNF-alpha production. |
Dupont Pharmaceuticals |
9548812 |
67 |
Inhibition of membrane-type 1 matrix metalloproteinase by hydroxamate inhibitors: an examination of the subsite pocket. |
Kanebo |
9484512 |
130 |
Highly selective and orally active inhibitors of type IV collagenase (MMP-9 and MMP-2): N-sulfonylamino acid derivatives. |
Shionogi |
9191969 |
31 |
Dual inhibition of human leukocyte elastase and lipid peroxidation: in vitro and in vivo activities of azabicyclo[2.2.2]octane and perhydroindole derivatives. |
Institut De Recherche Servier |
8289190 |
31 |
Synthesis of novel N-phosphonoalkyl dipeptide inhibitors of human collagenase. |
Smithkline Beecham Pharmaceuticals |
8277511 |
57 |
Inhibition of matrix metalloproteinases by N-carboxyalkyl peptides. |
Merck Research Laboratories |
8258825 |
31 |
Synthesis of novel modified dipeptide inhibitors of human collagenase: beta-mercapto carboxylic acid derivatives. |
Smithkline Beecham Pharmaceuticals |
8126708 |
113 |
Matrix metalloproteinase inhibitors containing a (carboxyalkyl)amino zinc ligand: modification of the P1 and P2' residues. |
Glaxo Inc. Research Institute |
7629797 |
73 |
Inhibition of matrix metalloproteinases by hydroxamates containing heteroatom-based modifications of the P1' group. |
Sterling Winthrop Pharmaceuticals Research Division |
22299577 |
12 |
Three new aromatic sulfonamide inhibitors of carbonic anhydrases I, II, IV and XII. |
Universit?? Di Firenze |
21524149 |
13 |
Design, synthesis and pharmacological evaluation of conformationally restricted N-arylsulfonyl-3-aminoalkoxy indoles as a potential 5-HT6 receptor ligands. |
Suven Life Sciences |
9463476 |
21 |
DL-threo-beta-benzyloxyaspartate, a potent blocker of excitatory amino acid transporters. |
Suntory Institute For Bioorganic Research |
8632342 |
110 |
Pharmacologic characterization of the human 5-hydroxytryptamine2B receptor: evidence for species differences. |
Eli Lilly |
7680751 |
48 |
Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs. |
National Institute of Neurological Disorders and Stroke |
19695884 |
156 |
Antagonists of the human A(2A) receptor. Part 6: Further optimization of pyrimidine-4-carboxamides. |
Vernalis (R&D) |
17034127 |
45 |
Small-molecule inhibitors of the MDM2-p53 protein-protein interaction based on an isoindolinone scaffold. |
University of Newcastle Upon Tyne |
19345579 |
14 |
Synthesis and PKCtheta inhibitory activity of a series of 4-indolylamino-5-phenyl-3-pyridinecarbonitriles. |
Wyeth Research |
19267461 |
53 |
Novel tricyclic inhibitors of IkappaB kinase. |
Bristol-Myers Squibb |