PMID

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Article Title

Organization

Discovery of triazole aminopyrazines as a highly potent and selective series of PI3Kd inhibitors.

Astrazeneca

Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety.

Xi'An Jiaotong University

Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kd inhibitors.

Bristol-Myers Squibb

Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors.

Hangzhou Xixi Hospital

Non-kinase targets of protein kinase inhibitors.

The University Of Sydney

Novel pyrazolo[1,5-a]pyridines with improved aqueous solubility as p110a-selective PI3 kinase inhibitors.

University Of Auckland

Discovery of a Potent, Selective, and Orally Available PI3Kd Inhibitor for the Treatment of Inflammatory Diseases.

RhôNe-Poulenc Rorer

6-Aryl substituted 4-(4-cyanomethyl) phenylamino quinazolines as a new class of isoform-selective PI3K-alpha inhibitors.

Csir-Indian Institute Of Integrative Medicine

Discovery of novel pyrrolidineoxy-substituted heteroaromatics as potent and selective PI3K delta inhibitors with improved physicochemical properties.

Novartis Institutes For Biomedical Research

Structure-based optimization leads to the discovery of NSC765844, a highly potent, less toxic and orally efficacious dual PI3K/mTOR inhibitor.

Second Military Medical University

Discovery and antiplatelet activity of a selective PI3Kß inhibitor (MIPS-9922).

Monash University

Imidazopyridazine Inhibitors of PI3Kß.

Dart Neuroscience

Synthesis of linear and angular aryl-morpholino-naphth-oxazines, their DNA-PK, PI3K, PDE3A and antiplatelet activity.

La Trobe University

Rational Design of Novel Highly Potent and Selective Phosphatidylinositol 4-Kinase IIIß (PI4KB) Inhibitors as Broad-Spectrum Antiviral Agents and Tools for Chemical Biology.

Academy Of Sciences Of The Czech Republic

Class II Phosphoinositide 3-Kinases as Novel Drug Targets.

Curtin University

Increasing metabolic stability via the deuterium kinetic isotope effect: An example from a proline-amide-urea aminothiazole series of phosphatidylinositol-3 kinase alpha inhibitors.

Novartis Institutes For Biomedical Research

Concise SAR Exploration Based on the"Head-to-Tail" Approach: Discovery of PI4KIIIa Inhibitors Bearing Diverse Scaffolds.

Japan Tobacco

Discovery of a Series of 5,11-Dihydro-6

Dana-Farber Cancer Institute

Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-¿ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate.

Infinity Pharmaceuticals

Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities.

West China Hospital Of Sichuan University

Discovery of novel 7-azaindoles as PDK1 inhibitors.

Merck

Optimization of the phenylurea moiety in a phosphoinositide 3-kinase (PI3K) inhibitor to improve water solubility and the PK profile by introducing a solubilizing group and ortho substituents.

Chugai Pharmaceutical

Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors.

Novartis Institutes For Biomedical Research

Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.

Novartis Institutes For Biomedical Research

Potent, Selective, and Orally Bioavailable Inhibitors of VPS34 Provide Chemical Tools to Modulate Autophagy in Vivo.

Novartis Institutes For Biomedical Research

Discovery of 2-(2-aminopyrimidin-5-yl)-4-morpholino-N-(pyridin-3-yl)quinazolin-7-amines as novel PI3K/mTOR inhibitors and anticancer agents.

Sun Yat-Sen University

Synthesis, structure elucidation, DNA-PK and PI3K and anti-cancer activity of 8- and 6-aryl-substituted-1-3-benzoxazines.

La Trobe University

Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma.

Second Military Medical University

Discovery of imidazo[1,2-a]-pyridine inhibitors of pan-PI3 kinases that are efficacious in a mouse xenograft model.

Novartis Institutes For Biomedical Research

Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators.

Shandong University

The imidazo[1,2-a]pyridine ring system as a scaffold for potent dual phosphoinositide-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitors.

Amgen

Synthesis and anticancer effects evaluation of 1-alkyl-3-(6-(2-methoxy-3-sulfonylaminopyridin-5-yl)benzo[d]thiazol-2-yl)urea as anticancer agents with low toxicity.

Xi'An Jiaotong University

Discovery of a novel tricyclic 4H-thiazolo[5',4':4,5]pyrano[2,3-c]pyridine-2-amino scaffold and its application in a PI3Ka inhibitor with high PI3K isoform selectivity and potent cellular activity.

Novartis Institutes For Biomedical Research

Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors.

Novartis Institutes For Biomedical Research

Modification of N-(6-(2-methoxy-3-(4-fluorophenylsulfonamido)pyridin-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)acetamide as PI3Ks inhibitor by replacement of the acetamide group with alkylurea.

Xi'An Jiaotong University

Discovery of potent, selective small molecule inhibitors ofa-subtype of type III phosphatidylinositol-4-kinase (PI4KIIIa).

Astrazeneca

Design, synthesis and biological evaluation of novel condensed pyrrolo[1,2-c]pyrimidines featuring morpholine moiety as PI3Ka inhibitors.

Cairo University

Design of selective PI3Ka inhibitors starting from a promiscuous pan kinase scaffold.

Astrazeneca

Exploring the isoform selectivity of TGX-221 related pyrido[1,2-a]pyrimidinone-based Class IA PI 3-kinase inhibitors: synthesis, biological evaluation and molecular modelling.

University Of Auckland

Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase¿.

Vertex Pharmaceuticals

Discovery of a Potent Class of PI3Ka Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT).

Glaxosmithkline

Discovery of a Novel Series of Thienopyrimidine as Highly Potent and Selective PI3K Inhibitors.

Pkucare Pharmaceutical R & D Center

Discovery of AZD3147: a potent, selective dual inhibitor of mTORC1 and mTORC2.

Astrazeneca

Discovery of (R)-8-(1-(3,5-difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide (AZD8186): a potent and selective inhibitor of PI3Kß and PI3Kd for the treatment of PTEN-deficient cancers.

Astrazeneca

Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors.

Vertex Pharmaceuticals

6,7-Dihydrobenzo[f]benzo[4,5]imidazo[1,2-d][1,4]oxazepine derivatives as selective inhibitors of PI3Ka.

Nanjing University

Synthesis and SAR study of potent and selective PI3Kd inhibitors.

Amgen

Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring.

University Hospital Hradec Kralove

Discovery of 9-(1-phenoxyethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as oral PI3Kß inhibitors, useful as antiplatelet agents.

Astrazeneca

Discovery of 9-(1-anilinoethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as PI3Kß/d inhibitors for the treatment of PTEN-deficient tumours.

Astrazeneca

Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness.

Northeastern University

Discovery of 4-aryl-N-arylcarbonyl-2-aminothiazoles as Hec1/Nek2 inhibitors. Part I: optimization of in vitro potencies and pharmacokinetic properties.

Development Center For Biotechnology

Preparation and optimization of new 4-(2-(indolin-1-yl)-2-oxoethyl)-2-morpholinothiazole-5-carboxylic acid and amide derivatives as potent and selective PI3Kß inhibitors.

Sanofi

Discovery and optimization of pyrimidone indoline amide PI3Kß inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.

Sanofi

Inhibitors of PI3K? as Potential Treatment for Cancer.

Therachem Research Medilab (India)

1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity.

Newcastle University

Structure guided optimization of a fragment hit to imidazopyridine inhibitors of PI3K.

Novartis Institutes For Biomedical Research

Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.

Novartis Institutes For Biomedical Research

Synthesis and biological evaluation of novel phosphatidylinositol 3-kinase inhibitors: Solubilized 4-substituted benzimidazole analogs of 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474).

University Of Auckland

Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): aß-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity.

Genentech

Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinaseß isoform.

Genentech

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

Exelixis

Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014.

Astrazeneca

Synthesis and cancer stem cell-based activity of substituted 5-morpholino-7H-thieno[3,2-b]pyran-7-ones designed as next generation PI3K inhibitors.

The University Of Arizona

Regioselective synthesis of 5- and 6-methoxybenzimidazole-1,3,5-triazines as inhibitors of phosphoinositide 3-kinase.

Monash Institute Of Pharmaceutical Sciences

L-Aminoacyl-triazine derivatives are isoform-selective PI3K? inhibitors that target non-conserved Asp862 of PI3K?

Monash University (Parkville Campus)

Discovery of a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Ka.

Celgene Avilomics Research

Rational Design, Synthesis, and SAR of a Novel Thiazolopyrimidinone Series of Selective PI3K-beta Inhibitors.

TBA

PI3Kd and PI3K¿ as targets for autoimmune and inflammatory diseases.

Amgen

Synthesis, DNA-PK inhibition, anti-platelet activity studies of 2-(N-substituted-3-aminopyridine)-substituted-1,3-benzoxazines and DNA-PK and PI3K inhibition, homology modelling studies of 2-morpholino-(7,8-di and 8-substituted)-1,3-benzoxazines.

La Trobe University

Synthesis and structure-activity relationships of dual PI3K/mTOR inhibitors based on a 4-amino-6-methyl-1,3,5-triazine sulfonamide scaffold.

Amgen

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

Recent results in protein kinase inhibition for tropical diseases.

Montclair State University

Potent and highly selective benzimidazole inhibitors of PI3-kinase delta.

Genentech

Discovery and in vivo evaluation of dual PI3Kß/d inhibitors.

Amgen

Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors.

Amgen

Discovery of phosphoinositide 3-kinases (PI3K) p110ß isoform inhibitor 4-[2-hydroxyethyl(1-naphthylmethyl)amino]-6-[(2S)-2-methylmorpholin-4-yl]-1H-pyrimidin-2-one, an effective antithrombotic agent without associated bleeding and insulin resistance.

Astrazeneca

Structure-based design of a novel series of potent, selective inhibitors of the class I phosphatidylinositol 3-kinases.

Amgen

Discovery of 4-morpholino-pyrimidin-6-one and 4-morpholino-pyrimidin-2-one-containing Phosphoinositide 3-kinase (PI3K) p110ß isoform inhibitors through structure-based fragment optimisation.

Astrazeneca

Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.

Exelixis

Preparation and optimization of new 4-(morpholin-4-yl)-(6-oxo-1,6-dihydropyrimidin-2-yl)amide derivatives as PI3Kß inhibitors.

Sanofi

Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway.

Novartis Institutes For Biomedical Research

SAR studies around a series of triazolopyridines as potent and selective PI3K¿ inhibitors.

Cellzome

Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kß inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.

Sanofi Research & Development

Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR.

Spanish National Cancer Research Centre (Cnio)

Discovery of novel PI3K¿/d inhibitors as potential agents for inflammation.

Cellzome

Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.

Ambit Biosciences

Synthesis, biological evaluation and molecular docking studies of 1,3,4-oxadiazole derivatives as potential immunosuppressive agents.

Nanjing University

Synthesis and structure-activity relationships of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones as novel series of potentß isoform selective phosphatidylinositol 3-kinase inhibitors.

Glaxosmithkline

Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer.

TBA

Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor.

Wyeth Research

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

University Of Oxford

Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway.

Novartis Institute For Biomedical Research

Synthesis and biological evaluation of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors.

Astellas Pharma

Synthesis and structure-activity relationships of imidazo[1,2-a]pyrimidin-5(1H)-ones as a novel series of beta isoform selective phosphatidylinositol 3-kinase inhibitors.

Glaxosmithkline

JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs.

Tianjin Key Laboratory On Technologies Enabling Development Of Clinical Therapeutics And Diagnostics

Rational design of phosphoinositide 3-kinasea inhibitors that exhibit selectivity over the phosphoinositide 3-kinaseß isoform.

Genentech

7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.

Ludwig-Maximilians University Of Munich

Novel pyrazolo[1,5-a]pyridines as p110a-selective PI3 kinase inhibitors: Exploring the benzenesulfonohydrazide SAR.

University Of Auckland

Discovery of pyrazolo[1,5-a]pyridines as p110a-selective PI3 kinase inhibitors.

University Of Auckland

Discovery of new aminopyrimidine-based phosphoinositide 3-kinase beta (PI3Kß) inhibitors with selectivity over PI3Ka.

Institute Of Science And Technology (Kaist)

Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer.

Genentech

Phospshoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: discovery and structure-activity relationships of a series of quinoline and quinoxaline derivatives.

Amgen

Synthesis and biological evaluation of novel analogues of the pan class I phosphatidylinositol 3-kinase (PI3K) inhibitor 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474).

University Of Auckland

Comprehensive analysis of kinase inhibitor selectivity.

Ambit Biosciences

Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.

Novartis Institute For Biomedical Research

Structure-activity relationships of phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: investigations of various 6,5-heterocycles to improve metabolic stability.

Amgen

Structure-based design of thienobenzoxepin inhibitors of PI3-kinase.

Genentech

Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.

Amgen

Design and synthesis of imidazopyridine analogues as inhibitors of phosphoinositide 3-kinase signaling and angiogenesis.

Korea Advanced Institute Of Science And Technology

Discovery of triazine-benzimidazoles as selective inhibitors of mTOR.

Amgen

Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799.

Chugai Pharmaceutical

Synthesis and in Vitro and in Vivo Evaluation of Phosphoinositide-3-kinase Inhibitors

TBA

Preparation and evaluation of trisubstituted pyrimidines as phosphatidylinositol 3-kinase inhibitors. 3-Hydroxyphenol analogues and bioisosteric replacements.

The Institute Of Cancer Research

Discovery of novel class 1 phosphatidylinositide 3-kinases (PI3K) fragment inhibitors through structure-based virtual screening.

Astrazeneca R & D M£Lndal

Identification and structure-activity relationship of 2-morpholino 6-(3-hydroxyphenyl) pyrimidines, a class of potent and selective PI3 kinase inhibitors.

Novartis Institutes For Biomedical Research

Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase.

Genentech

PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor.

Pfizer

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

Ambit Biosciences

The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors.

Medical Research Council-Laboratory Of Molecular Biology

5-ureidobenzofuranone indoles as potent and efficacious inhibitors of PI3 kinase-alpha and mTOR for the treatment of breast cancer.

Wyeth Research

Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent.

Wyeth Research

Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.

Genentech

Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer.

Genentech

The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase.

Kudos Pharmaceuticals

Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402.

Wyeth Research

Incorporation of water-solubilizing groups in pyrazolopyrimidine mTOR inhibitors: discovery of highly potent and selective analogs with improved human microsomal stability.

Wyeth Research

Phosphoinositide-3-kinase (PI3K) inhibitors: identification of new scaffolds using virtual screening.

University Of Auckland

Morpholine derivatives greatly enhance the selectivity of mammalian target of rapamycin (mTOR) inhibitors.

Wyeth Research

Optimization of a series of multi-isoform PI3 kinase inhibitors.

Ucb Pharma

Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines.

Ucb Pharma

4-(1,3-Thiazol-2-yl)morpholine derivatives as inhibitors of phosphoinositide 3-kinase.

Ucb Pharma

Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110alpha inhibitors.

University Of Auckland

Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma.

Serono Pharmaceutical Research Institute

Design, synthesis and biological evaluation of novel inosine 5'-monophosphate dehydrogenase (IMPDH) inhibitors.

Nycomed

Semisynthesis of alpha-methyl-gamma-lactones and in vitro evaluation of their activity on protein farnesyltransferase.

Ufr Des Sciences Pharmaceutiques Et Ingenierie De La Sante

Receptor occupancy and adenylate cyclase activation in AR 4-2J rat pancreatic acinar cell membranes by analogs of pituitary adenylate cyclase-activating peptides amino-terminally shortened or modified at position 1, 2, 3, 20, or 21.

Universit&Acute

Inhibitors of tubulin assembly identified through screening a compound library.

The Ohio State University

Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.

University Of California San Francisco

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

Phosphoinositide 3-kinase gamma/delta inhibition limits infarct size after myocardial ischemia/reperfusion injury.

Targegen

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

A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties.

Johnson & Johnson Pharmaceutical

Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy.

Wyeth Research

Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors.

Pfizer

Structural basis for the highly selective inhibition of MMP-13.

Aventis Pharma Deutschland

Homodimeric tacrine congeners as acetylcholinesterase inhibitors.

National Defense Medical Center