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Xiaoping Zheng
Researcher at Bristol-Myers Squibb
Publications - 8
Citations - 687
Xiaoping Zheng is an academic researcher from Bristol-Myers Squibb. The author has contributed to research in topics: Growth factor receptor & Moiety. The author has an hindex of 8, co-authored 8 publications receiving 651 citations.
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Journal ArticleDOI
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.
Rajeev S. Bhide,Zhen-Wei Cai,Yong-Zheng Zhang,Ligang Qian,Donna D. Wei,Stephanie Barbosa,Louis J. Lombardo,Robert M. Borzilleri,Xiaoping Zheng,Laurence I. Wu,Joel C. Barrish,Soong-Hoon Kim,Kenneth J. Leavitt,Arvind Mathur,Leslie Leith,Sam T. Chao,Barri Wautlet,Steven Mortillo,Robert Jeyaseelan,Daniel W. Kukral,John T. Hunt,Amrita Kamath,Aberra Fura,Viral Vyas,Punit Marathe,Celia D’Arienzo,George M. Derbin,Joseph Fargnoli +27 more
TL;DR: 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.
Journal ArticleDOI
Discovery of brivanib alaninate ((S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), a novel prodrug of dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinase inhibitor (BMS-540215).
Zhen-Wei Cai,Yong-Zheng Zhang,Robert M. Borzilleri,Ligang Qian,Stephanie Barbosa,Donna D. Wei,Xiaoping Zheng,Lawrence Wu,Junying Fan,Zhongping Shi,Barri Wautlet,Steve Mortillo,Robert Jeyaseelan,Daniel W. Kukral,Amrita Kamath,Punit Marathe,Celia D’Arienzo,George M. Derbin,Joel C. Barrish,Jeffrey A. Robl,John T. Hunt,Louis J. Lombardo,Joseph Fargnoli,Rajeev S. Bhide +23 more
TL;DR: A series of amino acid ester prodrugs of the dual VEGFR-2/FGFR-1 kinase inhibitor 1 was prepared in an effort to improve the aqueous solubility and oral bioavailability of the parent compound.
Journal ArticleDOI
A Novel Application of a Pd(0)-Catalyzed Nucleophilic Substitution Reaction to the Regio- and Stereoselective Synthesis of Lactam Analogues of the Epothilone Natural Products
Robert M. Borzilleri,Xiaoping Zheng,Robert J. Schmidt,James A. Johnson,Soong-Hoon Kim,John D. Dimarco,Craig R. Fairchild,Jack Z. Gougoutas,Francis Y. Lee,and Byron H. Long,Gregory D. Vite +10 more
TL;DR: Several lactam analogues of the epothilones were prepared using a concise semisynthetic approach starting with the unprotected natural products and a novel regio- and stereoselective Pd(0)-catalyzed azidation reaction of a macrocyclic lactone resulted in satisfactory overall yields.
Journal ArticleDOI
Discovery of the Pyrrolo[2,1-f][1,2,4]triazine Nucleus as a New Kinase Inhibitor Template
John T. Hunt,Toomas Mitt,Robert M. Borzilleri,Johnni Gullo-Brown,Joseph Fargnoli,Brian E. Fink,Wen-Ching Han,Steven Mortillo,Gregory D. Vite,Barri Wautlet,Tai Wong,Chiang Yu,Xiaoping Zheng,Rajeev S. Bhide +13 more
TL;DR: Preliminary inhibition studies with varying ATP concentrations suggest that, like the quinazoline-based kinase inhibitors, the pyrrolotriazine-based inhibitors bind in the ATP pocket.
Journal ArticleDOI
Synthesis and Biological Activity of Novel Epothilone Aziridines
Alicia Regueiro-Ren,Robert M. Borzilleri,Xiaoping Zheng,Soong-Hoon Kim,James A. Johnson,Craig R. Fairchild,Francis Y. Lee,Byron H. Long,Gregory D. Vite +8 more
TL;DR: The results indicate that the aziridine moiety is a viable isosteric replacement for the epoxide in the case of epothilones.