The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27216999 |
30 |
Protective effect of novel substituted nicotine hydrazide analogues against hypoxic brain injury in neonatal rats via inhibition of caspase. |
The Fifth Affiliated Hospital of Guangzhou Medical University |
25171780 |
7 |
Design, synthesis, and structure-activity relationships of novel benzothiazole derivatives bearing the ortho-hydroxy N-carbamoylhydrazone moiety as potent antitumor agents. |
Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University) Ministry of Education |
25011914 |
2 |
In vitro induction of apoptosis by isosclerone from marine-derived fungus Aspergillus fumigatus. |
Pukyong National University |
25468037 |
76 |
Synthesis and evaluation of N-acyl-substituted 1,2-benzisothiazol-3-one derivatives as caspase-3 inhibitors. |
TBA |
25358116 |
84 |
Synthesis of 7-halogenated isatin sulfonamides: nonradioactive counterparts of caspase-3/-7 inhibitor-based potential radiopharmaceuticals for molecular imaging of apoptosis. |
Westf£Lische Wilhelms-Universit£T M£Nster |
24656804 |
44 |
1,2-benzisothiazol-3-one derivatives as a novel class of small-molecule caspase-3 inhibitors. |
Tianjin University of Science and Technology |
23685941 |
53 |
Influence of 4- or 5-substituents on the pyrrolidine ring of 5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin derivatives on their inhibitory activities towards caspases-3 and -7. |
Westf£Lische Wilhelms-Universit£T M£Nster |
23632366 |
33 |
Design, synthesis and evaluation of 1,2-benzisothiazol-3-one derivatives as potent caspase-3 inhibitors. |
Nankai University |
23656488 |
18 |
Synthesis, 18F-radiolabeling, and in vivo biodistribution studies of N-fluorohydroxybutyl isatin sulfonamides using positron emission tomography. |
Westf£Lische Wilhelms-Universit£T M£Nster |
23411396 |
60 |
Synthesis of new fluorinated, 2-substituted 5-pyrrolidinylsulfonyl isatin derivatives as caspase-3 and caspase-7 inhibitors: nonradioactive counterparts of putative PET-compatible apoptosis imaging agents. |
Westf£Lische Wilhelms-Universit£T M£Nster |
24900651 |
50 |
Irreversible inhibitors of cysteine proteases. |
Dart Neuroscience |
22503362 |
35 |
New description of protein-ligand interactions using a spherical self-organizing map. |
Chugai Pharmaceutical |
22224594 |
346 |
Discovery and structure-activity relationship of potent and selective covalent inhibitors of transglutaminase 2 for Huntington's disease. |
Evotec (Uk) |
22652225 |
27 |
A novel class of small-molecule caspase-3 inhibitors prepared by multicomponent reactions. |
Southern Medical University |
22276851 |
4 |
Caspase-1 and -3 inhibiting drimane sesquiterpenoids from the extremophilic fungus Penicillium solitum. |
University of Montana |
21324681 |
23 |
Isatin 1,2,3-triazoles as potent inhibitors against caspase-3. |
University of Oslo |
19715320 |
87 |
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. |
University of Florida |
16870441 |
30 |
Synthesis and evaluation of thiazepines as interleukin-1beta converting enzyme (ICE) inhibitors. |
Procter and Gamble Pharmaceuticals |
16046125 |
18 |
Discovery of novel conformationally restricted diazocan peptidomimetics as inhibitors of interleukin-1beta synthesis. |
Procter & Gamble Pharmaceuticals |
15214773 |
76 |
Fragment-based drug discovery. |
Sunesis Pharmaceuticals |
10669559 |
180 |
Protease inhibitors: current status and future prospects. |
University of Queensland |
14980679 |
30 |
Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid. |
Maxim Pharmaceuticals |
9873373 |
20 |
Peptidyl beta-homo-aspartals: specific inhibitors of interleukin-1 beta converting enzyme and its homologues (caspases). |
Institute For Drug Research |
21903398 |
88 |
Exploiting differences in caspase-2 and -3 S2 subsites for selectivity: structure-based design, solid-phase synthesis and in vitro activity of novel substrate-based caspase-2 inhibitors. |
Chdi Management |
21439692 |
8 |
Aspartic vinyl sulfones: inhibitors of a caspase-3-dependent pathway. |
University of Lisbon |
21441025 |
147 |
Synthesis and evaluation of isatin analogs as caspase-3 inhibitors: introduction of a hydrophilic group increases potency in a whole cell assay. |
Washington University |
20541849 |
21 |
Synthesis and evaluation of vinyl sulfones as caspase-3 inhibitors. A structure-activity study. |
University of Lisbon |
20154666 |
1 |
Turning enzymes ON with small molecules. |
University of California |
17948018 |
17 |
Mechanisms, biology and inhibitors of deubiquitinating enzymes. |
Institute For Bio-Medical Research |
19631549 |
18 |
Design, synthesis, and discovery of novel non-peptide inhibitor of Caspase-3 using ligand based and structure based virtual screening approach. |
Osmania University College For Women |
19445513 |
82 |
Fluorinated isatin derivatives. Part 2. New N-substituted 5-pyrrolidinylsulfonyl isatins as potential tools for molecular imaging of caspases in apoptosis. |
Westfalische Wilhelms-Universitat |
19299147 |
60 |
Fluorinated isatin derivatives. Part 1: synthesis of new N-substituted (S)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatins as potent caspase-3 and -7 inhibitors. |
WestfäLische Wilhelms-UniversitäT |
19049429 |
70 |
Design, synthesis, and biological characterization of a caspase 3/7 selective isatin labeled with 2-[18F]fluoroethylazide. |
Imperial College |
18387304 |
4 |
Structure-based discovery of a novel non-peptidic small molecular inhibitor of caspase-3. |
Tokyo University of Science |
17889532 |
23 |
Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: peptidomimetic replacement of the P(2) amino acid by 2-aminoaryl acids and other non-natural amino acids. |
Epicept |
17585855 |
65 |
Isatin sulfonamide analogs containing a Michael addition acceptor: a new class of caspase 3/7 inhibitors. |
Washington University |
17251019 |
30 |
Solid-phase analogue synthesis of caspase-3 inhibitors via palladium-catalyzed amination of 3-bromopyrazinones. |
Merck Frosst Centre For Therapeutic Research |
17181147 |
10 |
Synthesis of novel caspase inhibitors for characterization of the active caspase proteome in vitro and in vivo. |
University of Edinburgh |
17154501 |
121 |
5-pyrrolidinylsulfonyl isatins as a potential tool for the molecular imaging of caspases in apoptosis. |
University Hospital of The WestfäLische Wilhelms-UniversitäT |
17127070 |
61 |
Synthesis and evaluation of unsaturated caprolactams as interleukin-1beta converting enzyme (ICE) inhibitors. |
Procter & Gamble Pharmaceuticals |
16891117 |
5 |
Synthesis, radiolabeling, and in vivo evaluation of an 18F-labeled isatin analog for imaging caspase-3 activation in apoptosis. |
Washington University |
16782334 |
61 |
Synthesis and evaluation of novel 1-(2-acylhydrazinocarbonyl)-cycloalkyl carboxamides as interleukin-1beta converting enzyme (ICE) inhibitors. |
Procter & Gamble Pharmaceuticals |
16216507 |
87 |
Synthesis and evaluation of novel 8,6-fused bicyclic peptidomimetic compounds as interleukin-1beta converting enzyme inhibitors. |
Procter & Gamble Pharmaceuticals |
16078840 |
94 |
Discovery and structure-activity relationship of 3-aryl-5-aryl-1,2,4-oxadiazoles as a new series of apoptosis inducers and potential anticancer agents. |
Maxim Pharmaceuticals |
16046129 |
18 |
Synthesis and evaluation of tricyclic pyrrolopyrimidinones as dipeptide mimetics: inhibition of interleukin-1beta-converting enzyme. |
Procter & Gamble Pharmaceuticals |
15808464 |
32 |
Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP. |
Merck Research Laboratories |
15713391 |
19 |
Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: peptidomimetic replacement of the P2 alpha-amino acid by a alpha-hydroxy acid. |
Maxim Pharmaceuticals |
15686936 |
210 |
Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors. |
Merck Frosst Centre For Therapeutic Research |
15588079 |
1 |
Design and synthesis of a potent and selective peptidomimetic inhibitor of caspase-3. |
University of Illinois At Chicago |
15454214 |
26 |
Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: SAR of the N-protecting group. |
Maxim Pharmaceuticals |
15109679 |
15 |
Oxamyl dipeptide caspase inhibitors developed for the treatment of stroke. |
Idun Pharmaceuticals |
14505683 |
6 |
Structure-activity relationships within a series of caspase inhibitors: effect of leaving group modifications. |
Idun Pharmaceuticals |
12270186 |
99 |
Acyl dipeptides as reversible caspase inhibitors. Part 2: further optimization. |
Idun Pharmaceuticals |
12270185 |
257 |
Acyl dipeptides as reversible caspase inhibitors. Part 1: initial lead optimization. |
Idun Pharmaceuticals |
12127536 |
22 |
Discovery of potent, selective human granzyme B inhibitors that inhibit CTL mediated apoptosis. |
Merck Research Laboratories |
30660827 |
70 |
Quinolone hybrids and their anti-cancer activities: An overview. |
Qilu University of Technology (Shandong Academy of Sciences) |
27563406 |
128 |
Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors. |
Roche Pharma Research and Early Development |
10978183 |
40 |
Caspases as targets for anti-inflammatory and anti-apoptotic drug discovery. |
Basf Bioresearch |
27594550 |
1 |
Synthesis and activity evaluation of the cyclic dipeptides arylidene N-alkoxydiketopiperazines. |
Hebei University of Science & Technology |
9873617 |
30 |
Conformationally constrained inhibitors of caspase-1 (interleukin-1 beta converting enzyme) and of the human CED-3 homologue caspase-3 (CPP32, apopain). |
Idun Pharmaceuticals |
26522952 |
44 |
Development of a potent and selective cell penetrant Legumain inhibitor. |
Queen'S University Belfast |
10479344 |
3 |
Secobatzellines A and B, two new enzyme inhibitors from a deep-water Caribbean sponge of the genus Batzella. |
Harbor Branch Oceanographic Institution |
9917313 |
1 |
Discorhabdin P, a new enzyme inhibitor from a deep-water Caribbean sponge of the genus Batzella. |
Harbor Branch Oceanographic Institution |
28615111 |
24 |
Synthesis and antitumor activities of 1,2,3-triazines and their benzo- and heterofused derivatives. |
Universit£ |
29650287 |
46 |
Structure-activity relationship study of a series of caspase inhibitors containing ?-amino acid moiety for treatment of cholestatic liver disease. |
Wuxi Apptec (Shanghai) |
29648825 |
47 |
Rational Drug Design of Topically Administered Caspase 1 Inhibitors for the Treatment of Inflammatory Acne. |
Nestl� |
28768102 |
37 |
Chemical Approaches to Intervening in Ubiquitin Specific Protease 7 (USP7) Function for Oncology and Immune Oncology Therapies. |
Progenra |
28820254 |
17 |
Blockade of Asparagine Endopeptidase Inhibits Cancer Metastasis. |
Emory Chemical Biology Discovery Center Emory University School of Medicine Atlanta |
12757844 |
9 |
In vitro characterization of [3H]MethoxyPyEP, an mGluR5 selective radioligand. |
Merck Research Laboratories |
11512051 |
80 |
The in vitro pharmacology of the beta-adrenergic receptor pet ligand (s)-fluorocarazolol reveals high affinity for cloned beta-adrenergic receptors and moderate affinity for the human 5-HT1A receptor. |
Case Western Reserve University |
9108306 |
17 |
Molecular cloning and characterization of a new receptor for galanin. |
Merck Research Laboratories |
18844338 |
4 |
Virtual screening to successfully identify novel janus kinase 3 inhibitors: a sequential focused screening approach. |
Johnson & Johnson Pharmaceutical |
18006306 |
12 |
Biphenyl amide p38 kinase inhibitors 1: Discovery and binding mode. |
Gsk |
18812261 |
8 |
The molecular interactions of buspirone analogues with the serotonin transporter. |
National Medicines Institute |
18307303 |
75 |
Discovery of selective aminothiazole aurora kinase inhibitors. |
Novartis |
18834107 |
22 |
Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. |
The Scripps Research Institute |
18855373 |
10 |
Structure-based virtual screening and biological evaluation of Mycobacterium tuberculosis adenosine 5'-phosphosulfate reductase inhibitors. |
The Scripps Research Institute |
18800762 |
61 |
Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates: a crystallographic and computational investigation. |
National Taiwan University |
18308563 |
39 |
Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases. |
Irbm/Merck Research Laboratories |
17685602 |
33 |
Discovery of 3,3'-(2,4-diaminopteridine-6,7-diyl)diphenol as an isozyme-selective inhibitor of PI3K for the treatment of ischemia reperfusion injury associated with myocardial infarction. |
Targegen |
18754654 |
19 |
The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . |
Piramed Pharma |
18800763 |
93 |
Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase. |
Glaxosmithkline |
17766111 |
17 |
Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP. |
Merck Research Laboratories |
32272481 |
9 |
Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors |
Shanghaitech University |
14698155 |
68 |
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. Part 4: Heterocycles at C3. |
Bristol-Myers Squibb |