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Article Title

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Indolyl-naphthyl-maleimides as potent and selective inhibitors of protein kinase C-a/ß.

Novartis Institutes For Biomedical Research

A nonpromoting phorbol from the samoan medicinal plant Homalanthus nutans inhibits cell killing by HIV-1.

National Cancer Institute-Frederick

Design of potent protein kinase inhibitors using the bisubstrate approach.

Ura Cnrs 1309

Synthesis of quaternary amine ether lipids and evaluation of neoplastic cell growth inhibitory properties.

University Of North Carolina

Synthesis of N-alkyl substituted indolocarbazoles as potent inhibitors of human cytomegalovirus replication.

Glaxosmithkline

Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC¿ inhibitors.

Takeda Pharmaceutical

Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2).

Icahn School Of Medicine At Mount Sinai

Discovery of selective and orally bioavailable protein kinase C¿ (PKC¿) inhibitors from a fragment hit.

Abbvie Bioresearch Center

Diacylglycerol lactones targeting the structural features that distinguish the atypical C1 domains of protein kinase C¿ and¿ from typical C1 domains.

National Cancer Institute-Bethesda

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

Optimisation of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors.

Msd

Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.

Abbott Laboratories

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

Hit to lead account of the discovery of bisbenzamide and related ureidobenzamide inhibitors of Rho kinase.

Boehringer Ingelheim Pharmaceuticals

Binding of curcumin and its long chain derivatives to the activator binding domain of novel protein kinase C.

University Of Houston

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

Wyeth Research

A quantitative analysis of kinase inhibitor selectivity.

Ambit Biosciences

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

Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.

Bristol-Myers Squibb Research And Development

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

University Of Oxford

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

Kyoto University

Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.

Abbott Laboratories

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

Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis.

Hoffmann-La Roche

Conformationally constrained analogues of diacylglycerol (DAG). 23. Hydrophobic ligand-protein interactions versus ligand-lipid interactions of DAG-lactones with protein kinase C (PK-C).

National Cancer Institute-Frederick

Kinase inhibitors: not just for kinases anymore.

Northwestern University

Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.

Millennium Pharmaceuticals

New hexahydroxybiphenyl derivatives as inhibitors of protein kinase C.

University Of North Carolina

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

Kyoto University

Structure-activity relationship studies of flavopiridol analogues.

Mitotix

 

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

TBA

RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: synthesis and biological evaluation.

Hoffmann-La Roche

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

Ansaris

Binding of isoxazole and pyrazole derivatives of curcumin with the activator binding domain of novel protein kinase C.

University Of Houston

Comprehensive analysis of kinase inhibitor selectivity.

Ambit Biosciences

Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.

Bristol-Myers Squibb

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

Keio University

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

Bristol-Myers Squibb Research And Development

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

Kyoto University

AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).

Ambit Biosciences

Actin is the primary cellular receptor of bistramide A.

University Of Chicago

Identification of orally available naphthyridine protein kinase D inhibitors.

Novartis Institutes For Biomedical Research

Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.

Abbott Laboratories

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

Wyeth Research

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

Wyeth Research

2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.

Abbott Laboratories

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

 

Benzo[c]quinoliziniums: A new family of inhibitors for protein kinase CK II

TBA

 

Novel conformationally constrained analogues of diacylglycerol. Protein kinase C binding affinity of simplified compounds based on a 6-membered lactam moiety

TBA

 

A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylation

TBA

 

Potent and selective inhibitors of the Abl-kinase: phenylamino-pyrimidine (PAP) derivatives

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

 

Phenylamino-pyrimidine (PAP) — derivatives: a new class of potent and highly selective PDGF-receptor autophosphorylation inhibitors

TBA

 

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

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

 

Conformationally constrained analogues of diacylglycerol (DAG). 4. Interaction of α-alkylidene-γ-lactones with protein kinase C (PK-C)

TBA

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

Wyeth Research

Design, synthesis, and biological activity of isophthalic acid derivatives targeted to the C1 domain of protein kinase C.

University Of Helsinki

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

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

Wyeth Research

Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2 subunits.

University Of California San Francisco

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

Kyoto University

Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.

Abbott Laboratories

Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors.

Roche Research Center

Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors.

Abbott Laboratories

Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.

Bristol-Myers Squibb Pharmaceutical Research Institute

Conformationally constrained analogues of diacylglycerol. 26. Exploring the chemical space surrounding the C1 domain of protein kinase C with DAG-lactones containing aryl groups at the sn-1 and sn-2 positions.

National Cancer Institute-Frederick

Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

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

Kyoto University

Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.

Abbott Bioresearch Center

Conformationally constrained analogues of diacylglycerol (DAG). 25. Exploration of the sn-1 and sn-2 carbonyl functionality reveals the essential role of the sn-1 carbonyl at the lipid interface in the binding of DAG-lactones to protein kinase C.

National Cancer Institute-Frederick

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

Johnson & Johnson Pharmaceutical Research & Development

Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.

Bristol-Myers Squibb Pharmaceutical Research Institute

The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.

Bristol-Myers Squibb

Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.

Bristol-Myers Squibb Pharmaceutical Research Institute

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

Novel IKK inhibitors: beta-carbolines.

Millennium Pharmaceuticals

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

Eli Lilly

Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.

Boehringer Ingelheim Pharmaceuticals

Synthesis and kinase inhibitory activity of 3'-(S)-epi-K-252a.

Cephalon

Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.

Abbott Bioresearch Center

Beta-carbolines as specific inhibitors of cyclin-dependent kinases.

Institute Of Molecular And Cell Biology

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

Georgetotwn University

Molecular models of N-benzyladriamycin-14-valerate (AD 198) in complex with the phorbol ester-binding C1b domain of protein kinase C-delta.

University Of Tennessee College Of Medicine

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

Synthesis of 7,8-disubstituted benzolactam-V8 and its binding to protein kinase C.

Institute Of Organic Chemistry

Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.

Merck

Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I.

Basf Bioresearch

Inhibition of Chikungunya Virus-Induced Cell Death by Salicylate-Derived Bryostatin Analogues Provides Additional Evidence for a PKC-Independent Pathway.

Stanford University

Synthesis and biological activities of NB-506 analogues modified at the glucose group.

Banyu Tsukuba Research Institute

Role of the hydrophobic moiety of tumor promoters. Synthesis and activity of 2-alkylated benzolactams.

University Of Tokyo

4-Pyridin-5-yl-2-(3,4,5-trimethoxyphenylamino)pyrimidines: potent and selective inhibitors of ZAP 70.

Celltech Therapeutics

Synthesis and biological activities of NB-506 analogues: Effects of the positions of two hydroxyl groups at the indole rings.

Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories

Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design.

Chinese Academy Of Sciences

Protein kinase C modulators bearing dicarba-CLOSO-dodecaborane as a hydrophobic pharmacophore.

University Of Tokyo

Discovery of Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase C? (PKC?) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis.

Vertex Pharmaceuticals

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

Stanford University

Discovery of 4

TBA

Synthesis and Structure-Activity Relationship Correlations of Gnidimacrin Derivatives as Potent HIV-1 Inhibitors and HIV Latency Reversing Agents.

Toho University

A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.

China Pharmaceutical University

Clarification of the binding mode of teleocidin and benzolactams to the Cys2 domain of protein kinase Cdelta by synthesis of hydrophobically modified, teleocidin-mimicking benzolactams and computational docking simulation.

University Of Tokyo

ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.

University Of Florida

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

Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.

Takeda Pharmaceutical

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

Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.

Abbvie Bioresearch Center

Synthesis, biological evaluation and SAR of 3-benzoates of ingenol for treatment of actinic keratosis and non-melanoma skin cancer.

Leo Pharma

Syntheses, biological evaluation and SAR of ingenol mebutate analogues for treatment of actinic keratosis and non-melanoma skin cancer.

Leo Pharma

Effects of the methoxy group in the side chain of debromoaplysiatoxin on its tumor-promoting and anti-proliferative activities.

Kyoto University

Structure-activity studies on the side chain of a simplified analog of aplysiatoxin (aplog-1) with anti-proliferative activity.

Kyoto University

Glycoglycerolipid analogues inhibit PKC translocation to the plasma membrane and downstream signaling pathways in PMA-treated fibroblasts and human glioblastoma cells, U87MG.

University Of Milan

New cytotoxic peroxylactones from the marine sponge, Plakinastrella onkodes.

Harbor Branch Oceanographic Institution

Bioactive peroxides as potential therapeutic agents.

The Hebrew University Of Jerusalem

Syntheses and biological activities of rebeccamycin analogues. Introduction of a halogenoacetyl substituent.

Universit£

Syntheses and biological evaluation of indolocarbazoles, analogues of rebeccamycin, modified at the imide heterocycle.

Universit£

An aminopyridazine-based inhibitor of a pro-apoptotic protein kinase attenuates hypoxia-ischemia induced acute brain injury.

Northwestern University

Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.

Kaohsiung Medical University

A novel 2,4-diaminopyrimidine derivative as selective inhibitor of protein kinase C theta prevents allograft rejection in a rat heart transplant model.

Astellas Pharma

Natural Products with Heteroatom-Rich Ring Systems.

University Of Auckland

Isolation, Characterization, and Structure-Activity Relationship Analysis of Abietane Diterpenoids from Callicarpa bodinieri as Spleen Tyrosine Kinase Inhibitors.

Yunnan University

Discovery of Novel Small-Molecule Inhibitors of NF-?B Signaling with Antiinflammatory and Anticancer Properties.

University Of Colorado

?-Arylidene Diacylglycerol-Lactones (DAG-Lactones) as Selective Ras Guanine-Releasing Protein 3 (RasGRP3) Ligands.

Seoul National University

Methyl 3-(3-(4-(2,4,4-Trimethylpentan-2-yl)phenoxy)-propanamido)benzoate as a Novel and Dual Malate Dehydrogenase (MDH) 1/2 Inhibitor Targeting Cancer Metabolism.

Dongguk University

Reverse Biosynthesis: Generating Combinatorial Pools of Drug Leads from Enzyme-Mediated Fragmentation of Natural Products.

The University Of Sydney

Inhibitors of Glycogen Synthase Kinase 3 with Exquisite Kinome-Wide Selectivity and Their Functional Effects.

Harvard Medical School

Thiazolidine-diones. Biochemical and biological activity of a novel class of tyrosine protein kinase inhibitors.

Ciba-Geigy

[3H]LY341495 binding to group II metabotropic glutamate receptors in rat brain.

Eli Lilly

Synthesis and in vitro opioid activity profiles of DALDA analogues.

Clinical Research Institute Of Montreal

Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors.

Johnson & Johnson Pharmaceutical

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

 

DISCOVERY AND STRUCTURE-ACTIVITY STUDIES OF A NOVEL SERIES OF PYRIDO[2,3-d]PYRIMIDINE TYROSINE KINASE INHIBITORS

Parke-Davis Pharmaceutical Research