The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28613895 |
66 |
A Highly Selective Hydantoin Inhibitor of Aggrecanase-1 and Aggrecanase-2 with a Low Projected Human Dose. |
Eli Lilly |
27966948 |
86 |
Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach. |
Pharmaceutical |
27914947 |
11 |
Synthesis and binding monitoring of a new nanomolar PAMAM-based matrix metalloproteinases inhibitor (MMPIs). |
University of Florence |
27825552 |
152 |
Design, synthesis, and biological activity of novel, potent, and highly selective fused pyrimidine-2-carboxamide-4-one-based matrix metalloproteinase (MMP)-13 zinc-binding inhibitors. |
Takeda Pharmaceutical |
27739691 |
7 |
Fragment-to-Lead Medicinal Chemistry Publications in 2015. |
Astex Pharmaceuticals |
26881908 |
13 |
De Novo Design at the Edge of Chaos. |
Swiss Federal Institute of Technology (Eth) |
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 |
26288689 |
37 |
Discovery of Potent and Selective Inhibitors for ADAMTS-4 through DNA-Encoded Library Technology (ELT). |
Glaxosmithkline |
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 |
25725607 |
15 |
2-Benzisothiazolylimino-5-benzylidene-4-thiazolidinones as protective agents against cartilage destruction. |
University of Catania |
25415648 |
63 |
Identification of potent and selective hydantoin inhibitors of aggrecanase-1 and aggrecanase-2 that are efficacious in both chemical and surgical models of osteoarthritis. |
Eli Lilly |
25330343 |
49 |
Characterization of selective exosite-binding inhibitors of matrix metalloproteinase 13 that prevent articular cartilage degradation in vitro. |
Translational Research Institute |
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£ |
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£ |
23246356 |
52 |
MMP inhibition by barbiturate homodimers. |
Trinity College |
17275314 |
701 |
Matrix metalloproteinases (MMPs): chemical-biological functions and (Q)SARs. |
Pomona College |
21669521 |
44 |
Selective non zinc binding inhibitors of MMP13. |
Astrazeneca |
12217355 |
39 |
Analogue based design of MMP-13 (Collagenase-3) inhibitors. |
Gvk Biosciences |
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 |
22540974 |
67 |
A new class of highly potent matrix metalloproteinase inhibitors based on triazole-substituted hydroxamates: (radio)synthesis and in vitro and first in vivo evaluation. |
University Hospital M£Nster |
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 |
19715320 |
87 |
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. |
University of Florida |
18358729 |
31 |
High throughput screening of potentially selective MMP-13 exosite inhibitors utilizing a triple-helical FRET substrate. |
Florida Atlantic University |
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 |
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 |
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 |
17956082 |
86 |
Novel fluorinated derivatives of the broad-spectrum MMP inhibitors N-hydroxy-2(R)-[[(4-methoxyphenyl)sulfonyl](benzyl)- and (3-picolyl)-amino]-3-methyl-butanamide as potential tools for the molecular imaging of activated MMPs with PET. |
University Hospital of The Westf£Lische Wilhelms-Universit£T M£Nster |
15214773 |
76 |
Fragment-based drug discovery. |
Sunesis Pharmaceuticals |
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 |
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 |
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 |
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 |
11133099 |
43 |
Synthesis and activity of selective MMP inhibitors with an aryl backbone. |
Pharmacia |
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 |
22175825 |
19 |
Potent inhibitors of LpxC for the treatment of Gram-negative infections. |
Pfizer |
22118188 |
50 |
A new generation of radiofluorinated pyrimidine-2,4,6-triones as MMP-targeted radiotracers for positron emission tomography. |
University Hospital M£Nster |
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 |
22153340 |
37 |
Discovery of potent and selective matrix metalloprotease 12 inhibitors for the potential treatment of chronic obstructive pulmonary disease (COPD). |
Pfizer |
22088955 |
33 |
Identification of novel molecular scaffolds for the design of MMP-13 inhibitors: a first round of lead optimization. |
Universit£ |
21937229 |
82 |
Potent and selective 2-naphthylsulfonamide substituted hydroxamic acid inhibitors of matrix metalloproteinase-13. |
Novartis Institutes For Biomedical Research |
21925881 |
60 |
Discovery of novel Cobactin-T based matrix metalloproteinase inhibitors via a ring closing metathesis strategy. |
Johnson & Johnson Pharmaceutical Research & Development |
21982494 |
75 |
Continued exploration of biphenylsulfonamide scaffold as a platform for aggrecanase-1 inhibition. |
Pfizer |
20726512 |
282 |
Orally active MMP-1 sparinga-tetrahydropyranyl anda-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease. |
Pfizer |
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 |
20965620 |
50 |
Structure-based approach to nanomolar, water soluble matrix metalloproteinases inhibitors (MMPIs). |
Protera |
21106451 |
39 |
Novel TNF-a converting enzyme (TACE) inhibitors as potential treatment for inflammatory diseases. |
Merck Research Laboratories |
20675133 |
32 |
SAR studies of non-zinc-chelating MMP-13 inhibitors: improving selectivity and metabolic stability. |
Boehringer Ingelheim Pharmaceuticals |
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 |
20172725 |
49 |
Discovery and SAR of hydantoin TACE inhibitors. |
Merck Research Laboratories |
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 |
19899765 |
69 |
Phosphinic tripeptides as dual angiotensin-converting enzyme C-domain and endothelin-converting enzyme-1 inhibitors. |
Cea |
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£ |
19625186 |
59 |
3,4-Disubstituted benzofuran P1' MMP-13 inhibitors: optimization of selectivity and reduction of protein binding. |
Wyeth Research |
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£ |
| 17 |
Design and synthesis of the cartilage protective agent (CPA, Ro32-3555) |
TBA |
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 |
19053764 |
101 |
Dual inhibitors of matrix metalloproteinases and carbonic anhydrases: iminodiacetyl-based hydroxamate-benzenesulfonamide conjugates. |
Instituto Superior TéCnico |
19042129 |
4 |
Calculation of binding free energies for non-zinc chelating pyrimidine dicarboxamide inhibitors with MMP-13. |
Stony Brook University |
18974001 |
72 |
N-((8-hydroxy-5-substituted-quinolin-7-yl)(phenyl)methyl)-2-phenyloxy/amino-acetamide inhibitors of ADAMTS-5 (Aggrecanase-2). |
Wyeth Research |
18790648 |
317 |
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge. |
University of Athens |
18364257 |
16 |
Ranking the selectivity of PubChem screening hits by activity-based protein profiling: MMP13 as a case study. |
The Scripps Research Institute |
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 |
18029177 |
57 |
A novel series of highly selective inhibitors of MMP-3. |
Pfizer |
17935984 |
29 |
Potent, selective spiropyrrolidine pyrimidinetrione inhibitors of MMP-13. |
Pfizer |
17591762 |
102 |
Potent and selective nonpeptidic inhibitors of procollagen C-proteinase. |
Pfizer |
17576061 |
132 |
Synthesis and structure-activity relationship of a novel, non-hydroxamate series of TNF-alpha converting enzyme inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
17531482 |
67 |
Design and synthesis of 3,3-piperidine hydroxamate analogs as selective TACE inhibitors. |
Wyeth Research |
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 |
17267227 |
12 |
Synthesis and in vitro evaluation of targeted tetracycline derivatives: effects on inhibition of matrix metalloproteinases. |
Clermont Auvergne University |
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 |
16942871 |
38 |
Potent, selective pyrimidinetrione-based inhibitors of MMP-13. |
Pfizer |
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 |
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 |
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 |
16002291 |
24 |
Structure-based design and synthesis of novel non-zinc chelating MMP-12 inhibitors. |
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 |
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 |
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 |
15125955 |
84 |
Reverse hydroxamate-based selective TACE inhibitors. |
Kaken Pharmaceutical |
14711305 |
26 |
Evaluation of P1'-diversified phosphinic peptides leads to the development of highly selective inhibitors of MMP-11. |
University of Athens |
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 |
12798337 |
6 |
Synthesis of radiolabeled biphenylsulfonamide matrix metalloproteinase inhibitors as new potential PET cancer imaging agents. |
Indiana University School of Medicine |
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 |
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 |
11754593 |
148 |
Phenoxyphenyl sulfone N-formylhydroxylamines (retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors. |
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 |
11563922 |
147 |
Structure-based design and synthesis of potent matrix metalloproteinase inhibitors derived from a 6H-1,3,4-thiadiazine scaffold. |
UniversitäT Bielefeld |
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 |
11454461 |
111 |
The development of new carboxylic acid-based MMP inhibitors derived from a cyclohexylglycine scaffold. |
Procter and Gamble Pharmaceuticals |
11384231 |
26 |
2-(2-Oxo-1,4-dihydro-2H-quinazolin-3-yl)- and 2-(2,2-dioxo-1,4-dihydro-2H-2lambda6-benzo[1,2,6]thiadiazin-3-yl)-N-hydroxy-acetamides as potent and selective peptide deformylase inhibitors. |
F. Hoffmann-La Roche |
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 |
11266157 |
12 |
Chemoenzymatic synthesis of functionalized cyclohexylglycines and alpha-methylcyclohexylglycines via Kazmaier-Claisen rearrangement. |
University of Florida |
31874775 |
176 |
Virtual screening identification and chemical optimization of substituted 2-arylbenzimidazoles as new non-zinc-binding MMP-2 inhibitors. |
"A. Moro" University of Bari |
11229774 |
40 |
Discovery of potent and selective succinyl hydroxamate inhibitors of matrix metalloprotease-3 (stromelysin-1). |
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 |
32379447 |
44 |
Validating the 1,2-Difluoro Motif As a Hybrid Bioisostere of CF |
Westf£Lische Wilhelms-Universit£T M£Nster |
10915056 |
8 |
Difluoroketones as inhibitors of matrix metalloprotease-13. |
Pfizer |
10882354 |
19 |
Structure-based design and synthesis of a potent matrix metalloproteinase-13 inhibitor based on a pyrrolidinone scaffold. |
Pfizer |
27194201 |
164 |
Use of Osmotic Pumps to Establish the Pharmacokinetic-Pharmacodynamic Relationship and Define Desirable Human Performance Characteristics for Aggrecanase Inhibitors. |
Eli Lilly |
10794702 |
340 |
Protease inhibitors: synthesis of potent bacterial collagenase and matrix metalloproteinase inhibitors incorporating N-4-nitrobenzylsulfonylglycine hydroxamate moieties. |
Università |
30688452 |
94 |
Synthesis and Structural/Functional Characterization of Selective M14 Metallocarboxypeptidase Inhibitors Based on Phosphinic Pseudopeptide Scaffold: Implications on the Design of Specific Optical Probes. |
Universitat Aut£Noma De Barcelona |
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 |
10522712 |
109 |
The synthesis and biological evaluation of non-peptidic matrix metalloproteinase inhibitors. |
British Biotech Pharmaceuticals |
30954331 |
54 |
Proline-based hydroxamates targeting the zinc-dependent deacetylase LpxC: Synthesis, antibacterial properties, and docking studies. |
University of Hamburg |
10406637 |
20 |
Synthesis and identification of conformationally constrained selective MMP inhibitors. |
Searle Discovery Research |
10230616 |
30 |
Discovery of a novel series of selective MMP inhibitors: identification of the gamma-sulfone-thiols. |
Searle Discovery Research |
10021913 |
42 |
Inhibition of MMP-1 and MMP-13 with phosphinic acids that exploit binding in the S2 pocket. |
Pfizer |
30846252 |
23 |
Recent developments in the synthesis and applications of phosphinic peptide analogs. |
Wroclaw University of Technology |
26810711 |
30 |
Fluorinated matrix metalloproteinases inhibitors--Phosphonate based potential probes for positron emission tomography. |
Westf£Lische Wilhelms-Universit£T |
24355348 |
1 |
4-Thiazolidinones: the advances continue?. |
Institute of Technology |
23899323 |
87 |
Inverse 1,2,3-triazole-1-yl-ethyl substituted hydroxamates as highly potent matrix metalloproteinase inhibitors: (radio)synthesis, in vitro and first in vivo evaluation. |
University Hospital M£Nster |
28818461 |
67 |
Discovery and process development of a novel TACE inhibitor for the topical treatment of psoriasis. |
Nestl� |
29191557 |
10 |
Synthesis of radioiodinated probes targeted toward matrix metalloproteinase-12. |
Kobe Pharmaceutical University |
30249495 |
241 |
Development of matrix metalloproteinase-13 inhibitors - A structure-activity/structure-property relationship study. |
Graz University of Technology |
28626528 |
10 |
Exploitation of Conformational Dynamics in Imparting Selective Inhibition for Related Matrix Metalloproteinases. |
University of Notre Dame |
27996256 |
4 |
Zinc-Metalloproteinase Inhibitors: Evaluation of the Complex Role Played by the Zinc-Binding Group on Potency and Selectivity. |
Universit£ |
28850227 |
85 |
Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry. |
St. John'S University |
28953404 |
70 |
Targeted Polypharmacology: Discovery of a Highly Potent Non-Hydroxamate Dual Matrix Metalloproteinase (MMP)-10/-13 Inhibitor. |
Zhaw Zurich University of Applied Sciences |
28558971 |
38 |
Fused bi-heteroaryl substituted hydantoin compounds as TACE inhibitors. |
Merck |
28408220 |
55 |
First insight into structure-activity relationships of selective meprin? inhibitors. |
Fraunhofer Institute For Cell Therapy and Immunology Izi |
28653849 |
67 |
Structure-Based Design and Synthesis of Potent and Selective Matrix Metalloproteinase 13 Inhibitors. |
Scripps Florida |
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 |
16206837 |
9 |
Tyrosinase inhibition: conformational analysis based studies on molecular dynamics calculations of bipiperidine based inhibitors. |
University of Karachi |
11916140 |
21 |
Carbonic anhydrase activity modulators: synthesis of inhibitors and activators incorporating 2-substituted-thiazol-4-yl-methyl scaffolds. |
UniversitÀ |
9463476 |
21 |
DL-threo-beta-benzyloxyaspartate, a potent blocker of excitatory amino acid transporters. |
Suntory Institute For Bioorganic Research |
9353361 |
3 |
[3H]RY 80: A high-affinity, selective ligand for gamma-aminobutyric acidA receptors containing alpha-5 subunits. |
National Institute of Diabetes and Digestive and Kidney Diseases |
8632342 |
110 |
Pharmacologic characterization of the human 5-hydroxytryptamine2B receptor: evidence for species differences. |
Eli Lilly |
8358562 |
29 |
Development of a radioligand binding assay for 5-HT4 receptors in guinea-pig and rat brain. |
Glaxo Group Research |
7651361 |
32 |
Characterization of (+/-)(-)[3H]epibatidine binding to nicotinic cholinergic receptors in rat and human brain. |
Georgetown University |
7515823 |
54 |
Actions of phenylglycine analogs at subtypes of the metabotropic glutamate receptor family. |
Novo Nordisk |
7509389 |
8 |
Pharmacological profile of FK480, a novel cholecystokinin type-A receptor antagonist: comparison to loxiglumide. |
Fujisawa Pharmaceutical |
18355729 |
12 |
Structure-based dissection of the natural product cyclopentapeptide chitinase inhibitor argifin. |
University of Dundee |
19345579 |
14 |
Synthesis and PKCtheta inhibitory activity of a series of 4-indolylamino-5-phenyl-3-pyridinecarbonitriles. |
Wyeth Research |