PMID

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Article Title

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Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.

Nerviano Medical Sciences

Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).

Exelixis

Design and optimization of selective protein kinase C¿ (PKC¿) inhibitors for the treatment of autoimmune diseases.

Vertex Pharmaceuticals

Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.

Cellzome

Structure-activity relationship and pharmacokinetic studies of sotrastaurin (AEB071), a promising novel medicine for prevention of graft rejection and treatment of psoriasis.

Novartis Institutes For Biomedical Research

2,6-Naphthyridines as potent and selective inhibitors of the novel protein kinase C isozymes.

Novartis Institutes For Biomedical Research

Structure-activity studies on the spiroketal moiety of a simplified analogue of debromoaplysiatoxin with antiproliferative activity.

Kyoto University

Structure-based optimization of aminopyridines as PKC¿ inhibitors.

Vertex Pharmaceuticals

A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity.

Nerviano Medical Sciences Oncology

C-5 substituted heteroaryl-3-pyridinecarbonitriles as PKCtheta inhibitors: part II.

Wyeth Research

Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.

University Of California

Synthesis and PKCtheta inhibitory activity of a series of 4-(indol-5-ylamino)thieno[2,3-b]pyridine-5-carbonitriles.

Wyeth Research

A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.

University Of Oxford

Novel pyrazolo[1,5-a]pyrimidines as c-Src kinase inhibitors that reduce IKr channel blockade.

Kissei Pharmaceutical

Design and physicochemical properties of new fluorescent ligands of protein kinase C isozymes focused on CH/pi interaction.

Kyoto University

Novel bis(indolyl)maleimide pyridinophanes that are potent, selective inhibitors of glycogen synthase kinase-3.

Johnson & Johnson Pharmaceutical Research & Development

Synthesis and c-Src inhibitory activity of imidazo[1,5-a]pyrazine derivatives as an agent for treatment of acute ischemic stroke.

Kissei Pharmaceutical

Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.

Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories

Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3.

Eli Lilly

Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors.

Central Pharmaceutical Research Institute

Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors.

Johnson And Johnson Pharmaceutical Research And Development

Synthesis and PKC isozyme surrogate binding of indothiolactam-V, a new thioamide analogue of tumor promoting indolactam-V.

Kyoto University

Adenosine-5'-carboxylic acid peptidyl derivatives as inhibitors of protein kinases.

Tartu University

 

Synthesis and PKC inhibitory activities of balanol analogs with a cyclopentane substructure

TBA

Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.

Glaxosmithkline

5-(2-amino-pyrimidin-4-yl)-1H-pyrrole and 2-(2-amino-pyrimidin-4-yl)-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one derivatives as new classes of selective and orally available Polo-like kinase 1 inhibitors.

Nerviano Medical Sciences

Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).

Ansaris

9-substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as highly selective and potent anaplastic lymphoma kinase inhibitors.

Chugai Pharmaceutical

Generation of 'Unnatural Natural Product' library and identification of a small molecule inhibitor of XIAP.

Keio University

Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.

Chugai Pharmaceutical

NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.

Nerviano Medical Sciences

Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.

Vertex Pharmaceuticals

5-amino-pyrazoles as potent and selective p38a inhibitors.

Bristol-Myers Squibb Research And Development

Identification of potent ITK inhibitors through focused compound library design including structural information.

Nycomed

Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.

Nerviano Medical Sciences

Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity.

Kyoto University

Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.

Nerviano Medical Sciences Oncology

Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors.

Nerviano Medical Sciences

2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability.

Wyeth Research

Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.

Wyeth Research

Optimization of 5-vinylaryl-3-pyridinecarbonitriles as PKCtheta inhibitors.

Wyeth Research

Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.

Cgi Pharmaceuticals

Discovery of highly potent and selective type I B-Raf kinase inhibitors.

Wyeth Research

Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles.

Wyeth Research

First generation 5-vinyl-3-pyridinecarbonitrile PKCtheta inhibitors.

Wyeth Research

C-5 Substituted heteroaryl 3-pyridinecarbonitriles as PKCtheta inhibitors: Part I.

Wyeth Research

Anti-AIDS Agents, 11. Betulinic Acid and Platanic Acid as Anti-HIV Principles from Syzigium claviflorum, and the Anti-HIV Activity of Structurally Related Triterpenoids

TBA

 

Synthesis and protein kinase C inhibitory activities of indane analogs of balanol

TBA

 

Potent and selective PKC inhibitory 5-membered ring analogs of balanol with replacement of the carboxamide moiety

TBA

 

Heteroatom effect in the PKC inhibitory activities of perhydroazepine analogs of balanol

TBA

 

Synthesis of bisindolylmaleimide macrocycles

TBA

 

Novel PKC inhibitory analogs of balanol with replacement of the ester functionality

TBA

 

Protein kinase C inhibitory activities of balanol analogs bearing carboxylic acid replacements

TBA

 

2-aryl-indolyl maleimides - novel and potent inhibitors of protein kinase C

TBA

Optimization of 5-phenyl-3-pyridinecarbonitriles as PKCtheta inhibitors.

Wyeth Research

Conformationally constrained analogues of diacylglycerol (DAG). 31. Modulation of the biological properties of diacylgycerol lactones (DAG-lactones) containing rigid-rod acyl groups separated from the core lactone by spacer units of different lengths.

National Cancer Institute-Frederick

Second generation 4-(4-methyl-1H-indol-5-ylamino)-2-phenylthieno[2,3-b]pyridine-5-carbonitrile PKCtheta inhibitors.

Wyeth Research

(-)-Cercosporamide derivatives as novel antihyperglycemic agents.

Daiichi Sankyo

Beyond the MEK-pocket: can current MEK kinase inhibitors be utilized to synthesize novel type III NCKIs? Does the MEK-pocket exist in kinases other than MEK?

Pfizer

2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.

Wyeth Research

A novel Syk family kinase inhibitor: design, synthesis, and structure-activity relationship of 1,2,4-triazolo[4,3-c]pyrimidine and 1,2,4-triazolo[1,5-c]pyrimidine derivatives.

Kissei Pharmaceutical

Minocycline down-regulates MHC II expression in microglia and macrophages through inhibition of IRF-1 and protein kinase C (PKC)alpha/betaII.

University Of Wisconsin

Synthesis, conformational analysis, and biological evaluation of 1-hexylindolactam-V10 as a selective activator for novel protein kinase C isozymes.

Kyoto University

Optimization of triarylimidazoles for Tie2: influence of conformation on potency.

Glaxosmithkline

Design and synthesis of 8-octyl-benzolactam-V9, a selective activator for protein kinase C epsilon and eta.

Kyoto University

Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety.

Johnson & Johnson Pharmaceutical Research & Development

Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine.

Michigan State University

3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3.

Johnson & Johnson Pharmaceutical Research & Development

Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.

Eli Lilly

New bivalent PKC ligands linked by a carbon spacer: enhancement in binding affinity.

Georgetown University Medical Center

Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.

Johnson & Johnson Pharmaceutical Research & Development

Synthesis and binding selectivity of 7- and 15-decylbenzolactone-V8 for the C1 domains of protein kinase C isozymes.

Kyoto University

Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta.

Eli Lilly

Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity.

Glaxosmithkline

Rational design, synthesis, and biological evaluation of rigid pyrrolidone analogues as potential inhibitors of prostate cancer cell growth.

Georgetotwn University

The amide hydrogen of (-)-indolactam-V and benzolactam-V8's plays a critical role in protein kinase C binding and tumor-promoting activities.

Kyoto University

The C4 hydroxyl group of phorbol esters is not necessary for protein kinase C binding.

Kyoto University

Selective binding of bryostatin analogues to the cysteine rich domains of protein kinase C isozymes.

Stanford University

Modeling, chemistry, and biology of the benzolactam analogues of indolactam V (ILV). 2. Identification of the binding site of the benzolactams in the CRD2 activator-binding domain of PKCdelta and discovery of an ILV analogue of improved isozyme selectivity.

Georgetown University Medical Center

Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety.

Eli Lilly

(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta.

Eli Lilly

Synthesis and in vitro opioid activity profiles of DALDA analogues.

Clinical Research Institute Of Montreal

Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues.

Emory University

Binding of rasagiline-related inhibitors to human monoamine oxidases: a kinetic and crystallographic analysis.

University Of Pavia

Methyl analogues of the experimental Alzheimer drug phenserine: synthesis and structure/activity relationships for acetyl- and butyrylcholinesterase inhibitory action.

National Institutes Of Health

Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.

National Institutes Of Health

Design, synthesis, and biological evaluation of conformationally restricted rivastigmine analogues.

University Of Bologna

3-(4-[[Benzyl(methyl)amino]methyl]phenyl)-6,7-dimethoxy-2H-2-chromenone (AP2238) inhibits both acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation: a dual function lead for Alzheimer's disease therapy.

University Of Bologna

Bis-huperzine B: highly potent and selective acetylcholinesterase inhibitors.

Shanghai Institute Of Materia Medica

Specificity and affinity of natural product cyclopentapeptide inhibitors against A. fumigatus, human, and bacterial chitinases.

University Of Dundee

Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum.

Cnrs