Zhen‐Wei Cai

Bristol-Myers Squibb (Germany)

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Louis J. Lombardo

Bristol-Myers Squibb (United States)

Joseph Fargnoli

Bristol-Myers Squibb (United States)

John T. Hunt

Lawrence Livermore National Laboratory

Barri Wautlet

Bristol-Myers Squibb (United States)

R. M. Borzilleri

Bristol-Myers Squibb (United States)

Robert Jeyaseelan

Bristol-Myers Squibb (Germany)

Donna Wei

Bristol-Myers Squibb (United States)

John S. Tokarski

Bristol-Myers Squibb (United States)

Rajeev S. Bhide

Bristol-Myers Squibb (United States)

Amrita V. Kamath

Institute for Clinical Pharmacodynamics (United States)

Cooperative Institutions

Bristol-Myers Squibb (United States)

Bristol-Myers Squibb (Germany)

Agios Pharmaceuticals (United States)

Princeton University

Rutgers, The State University of New Jersey

Harvard University

Ribon Therapeutics (United States)

Acorda Therapeutics (United States)

Cornell University

Albany Molecular Research (United States)

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Some Observations on the Palladium-Catalyzed Triflate-Arene Cyclization of Electron-Rich Biaryl Substrates

The Journal of Organic Chemistry (1995)

Joseph E. Rice Zhen‐Wei Cai He Zhenmin Edmond J. LaVoie

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSome Observations on the Palladium-Catalyzed Triflate-Arene Cyclization of Electron-Rich Biaryl SubstratesJoseph E. Rice, Zhen-Wei Cai, Zhen-Min He, and Edmond J. LaVoieCite this: J. Org. Chem. 1995, 60, 24, 8101–8104Publication Date (Print):December 1, 1995Publication History Published online1 May 2002Published inissue 1 December 1995https://pubs.acs.org/doi/10.1021/jo00129a064https://doi.org/10.1021/jo00129a064research-articleACS PublicationsRequest reuse permissionsArticle Views393Altmetric-Citations33LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-AlertscloseSupporting Info (2)»Supporting Information Supporting Information Get e-Alerts

Trifluoromethanesulfonate

10.1021/jo00129a064

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Citations (37)

Discovery and Preclinical Studies of (R)-1-(4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an In Vivo Active Potent VEGFR-2 Inhibitor

Journal of Medicinal Chemistry (2006)

Rajeev S. Bhide Zhen‐Wei Cai Yong‐Zheng Zhang Ligang Qian Donna Wei

A series of substituted 4-(4-fluoro-1H-indol-5-yloxy)pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of vascular endothelial growth factor receptor-2 kinase is reported. Structure−activity relationship studies revealed that a methyl group at the 5-position and a substituted alkoxy group at the 6-position of the pyrrolo[2,1-f][1,2,4]triazine core gave potent compounds. Biochemical potency, kinase selectivity, and pharmacokinetics of the series were optimized and in vitro safety liabilities were minimized to afford BMS-540215 (12), which demonstrated robust preclinical in vivo activity in human tumor xenograft models. The l-alanine prodrug of 12, BMS-582664 (21), is currently under evaluation in clinical trials for the treatment of solid tumors.

Triazine

Structure–activity relationship

Molecular model

10.1021/jm051106d

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Citations (129)

Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors

Bioorganic & Medicinal Chemistry Letters (2008)

Zhen‐Wei Cai Donna Wei Gretchen M. Schroeder Lyndon A. M. Cornelius Kyoung Kim

Orally active

2-Aminopyridine

10.1016/j.bmcl.2008.04.047

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Citations (62)

Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors

Bioorganic & Medicinal Chemistry Letters (2005)

R. M. Borzilleri Zhen‐Wei Cai Christopher D. Ellis Joseph Fargnoli Aberra Fura

Triazine

Side chain

10.1016/j.bmcl.2004.12.079

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Citations (39)

Discovery of Pyrrolopyridine−Pyridone Based Inhibitors of Met Kinase: Synthesis, X-ray Crystallographic Analysis, and Biological Activities

Journal of Medicinal Chemistry (2008)

Kyoung Soon Kim Liping Zhang Robert J. Schmidt Zhen‐Wei Cai Donna Wei

Conformationally constrained 2-pyridone analogue 2 is a potent Met kinase inhibitor with an IC50 value of 1.8 nM. Further SAR of the 2-pyridone based inhibitors of Met kinase led to potent 4-pyridone and pyridine N-oxide inhibitors such as 3 and 4. The X-ray crystallographic data of the inhibitor 2 bound to the ATP binding site of Met kinase protein provided insight into the binding modes of these inhibitors, and the SAR of this series of analogues was rationalized. Many of these analogues showed potent antiproliferative activities against the Met dependent GTL-16 gastric carcinoma cell line. Compound 2 also inhibited Flt-3 and VEGFR-2 kinases with IC50 values of 4 and 27 nM, respectively. It possesses a favorable pharmacokinetic profile in mice and demonstrates significant in vivo antitumor activity in the GTL-16 human gastric carcinoma xenograft model.

IC50

Structure–activity relationship

10.1021/jm800476q

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Citations (117)

A palladium-catalyzed intramolecular arene-triflate coupling for the synthesis of fluoranthenes and benzofluoranthenes

Tetrahedron Letters (1992)

Joseph E. Rice Zhen‐Wei Cai

Fluoranthene

Trifluoromethanesulfonate

10.1016/s0040-4039(00)91703-9

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Citations (36)

Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor

Bioorganic & Medicinal Chemistry Letters (2008)

Réjean Ruel Carl Thibeault Alexandre L’Heureux Alain Martel Zhen‐Wei Cai

Isopropyl

Structure–activity relationship

10.1016/j.bmcl.2008.03.057

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Citations (17)

Addition of Benzylic and Allylic Organozinc and Grignard Reagents to Resin-Bound Imines To Provide α-Branched Secondary Amines Bearing a Wide Variety of Functional Groups. Utility in the Synthesis of β-3 Adrenergic Receptor Agonists

Journal of Combinatorial Chemistry (2004)

Gang Wu Zhen‐Wei Cai Mark S. Bednarz Octavian Kocy Ashvinikumar V. Gavai

Benzylic and allylic organozinc and Grignard reagents have been added to resin-bound imines to provide α-branched secondary amines. Many functional groups, including electrophilic groups, were compatible with this methodology. Three modulesa resin-bound primary amine, an aromatic aldehyde, and the organometallicwere independently varied to produce a combinatorial library of α-branched secondary amines designed as β-3 adrenergic receptor agonists.

Functional group

Primary (astronomy)

10.1021/cc0498682

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Citations (7)

Vorasidenib (AG-881): A First-in-Class, Brain-Penetrant Dual Inhibitor of Mutant IDH1 and 2 for Treatment of Glioma

ACS Medicinal Chemistry Letters (2020)

Zenon Konteatis Erin Artin Brandon Nicolay Kimberly Straley Anil K. Padyana

Inhibitors of mutant isocitrate dehydrogenase (mIDH) 1 and 2 cancer-associated enzymes prevent the accumulation of the oncometabolite d-2-hydroxyglutarate (2-HG) and are under clinical investigation for the treatment of several cancers harboring an IDH mutation. Herein, we describe the discovery of vorasidenib (AG-881), a potent, oral, brain-penetrant dual inhibitor of both mIDH1 and mIDH2. X-ray cocrystal structures allowed us to characterize the compound binding site, leading to an understanding of the dual mutant inhibition. Furthermore, vorasidenib penetrates the brain of several preclinical species and inhibits 2-HG production in glioma tissue by >97% in an orthotopic glioma mouse model. Vorasidenib represents a novel dual mIDH1/2 inhibitor and is currently in clinical development for the treatment of low-grade mIDH glioma.

Isocitrate dehydrogenase

Penetrant (biochemical)

10.1021/acsmedchemlett.9b00509

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Citations (138)

A Study of the Favorskii Rearrangement with 3-Bromo-4-oxo-2,2,6,6-tetramethylpiperidine-1-oxyl

The Journal of Organic Chemistry (1995)

George Sosnovsky Zhen‐Wei Cai

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTA Study of the Favorskii Rearrangement with 3-Bromo-4-oxo-2,2,6,6-tetramethylpiperidine-1-oxylGeorge Sosnovsky and Zhen-wei CaiCite this: J. Org. Chem. 1995, 60, 11, 3414–3418Publication Date (Print):June 1, 1995Publication History Published online1 May 2002Published inissue 1 June 1995https://pubs.acs.org/doi/10.1021/jo00116a029https://doi.org/10.1021/jo00116a029research-articleACS PublicationsRequest reuse permissionsArticle Views776Altmetric-Citations45LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InRedditEmail Other access optionsGet e-Alertsclose Get e-Alerts

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10.1021/jo00116a029

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Citations (49)