Zobrazeno 1 - 10
of 31
pro vyhledávání: '"Donna D. Wei"'
Autor:
Yanling Huang, Murali Gururajan, Cullen L. Cavallaro, Zhuyin Li, Ashok V. Purandare, Jessica J. Wong, Jenny Xie, Sylwia Stachura, Huadong Sun, Lalgudi S. Harikrishnan, Javed Khan, Brian E. Fink, Carolyn A. Weigelt, Honghe Wan, Peter K. Park, Daniel O'malley, Michele Agler, Cliff Chen, John S. Sack, Donna D. Wei, Zheming Ruan, Melissa Yarde, Heidi L. Perez, Monique Anthony, Virna Borowski, Max Ruzanov
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 35:127778
The discovery of a series of substituted diarylether compounds as retinoic acid related orphan receptor γt (RORγt) agonists is described. Compound 1 was identified from deck mining as a RORγt agonist. Hit-to-lead optimization led to the identifica
Autor:
Gregory D. Vite, Randy Talbott, Joseph G. Naglich, Caroline Fanslau, Jinping Gan, Donna D. Wei, Charu Chaudhry, Joseph Fargnoli, Kyoung S. Kim, Robert M. Borzilleri, Ming Lei, Ragini Vuppugalla, Stuart Emanuel, Sarah C. Traeger, Heidi L. Perez
Publikováno v:
Journal of Medicinal Chemistry. 58:1556-1562
The prominent role of IAPs in controlling cell death and their overexpression in a variety of cancers has prompted the development of IAP antagonists as potential antitumor therapies. We describe the identification of a series of heterodimeric antago
Autor:
Erik M. Stang, Heidi L. Perez, Andrew F. Donnell, Robert M. Borzilleri, Gregory D. Vite, Yong Zhang, Sanjeev Gangwar, Chetana Rao, Donna D. Wei, Andrew J. Tebben, Gretchen M. Schroeder, Chin Pan
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(23)
Macrocyclic pyrrolobenzodiazepine dimers were designed and evaluated for use as antibody-drug conjugate payloads. Initial structure-activity exploration established that macrocyclization could increase the potency of PBD dimers compared with non-macr
Autor:
John E. Leet, Ravindra W. Tejwani, Louis J. Lombardo, Yueping Zhang, Benjamin M. Johnson, Xiaohong Liu, Rajeev S. Bhide, Donna D. Wei, Ligang Qian, Yue-Zhong Shu, Amrita Kamath
Publikováno v:
Drug Metabolism and Disposition. 36:2475-2483
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) is a potent and selective vascular endothelial growth factor receptor-2 antagonist. In this study, liquid chroma
Autor:
Robert J. Schmidt, Benjamin J. Henley, Celia D’Arienzo, Jonathan Lippy, John S. Sack, Yueping Zhang, Yongmi An, John T. Hunt, Amrita Kamath, John S. Tokarski, Barri Wautlet, Veeraswamy Manne, Dianlin Xie, Punit Marathe, Donna D. Wei, Louis J. Lombardo, Kyoung S. Kim, Robert Jeyaseelan, David K. Williams, Joseph Fargnoli, Liping Zhang, Yaquan Zhang, Johnni Gullo-Brown, Zhen-Wei Cai, George L. Trainor, Robert M. Borzilleri
Publikováno v:
Journal of Medicinal Chemistry. 51:5330-5341
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. T
Autor:
Amrita Kamath, Yongmi An, John T. Hunt, Punit Marathe, Veeraswamy Manne, Zhen-Wei Cai, Donna D. Wei, John S. Sack, Robert J. Schmidt, Yueping Zhang, Robert M. Borzilleri, Kyoung S. Kim, Cornelius Lyndon A M, Gretchen M. Schroeder, David K. Williams, Xiao-Tao Chen, Joseph Fargnoli, Louis J. Lombardo, John S. Tokarski
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3224-3229
A series of acylurea analogs derived from pyrrolopyridine and aminopyridine scaffolds were identified as potent inhibitors of Met kinase activity. The SAR at various positions of the two kinase scaffolds was investigated. These studies led to the dis
Autor:
Ligang Qian, Carl Thibeault, Amrita Kamath, Barri Wautlet, Alain Martel, George L. Trainor, Punit Marathe, Celia D’Arienzo, Benjamin J. Henley, Steven Mortillo, Donna D. Wei, Robert Jeyaseelan, Ravindra W. Tejwani, John T. Hunt, Louis J. Lombardo, Rejean Ruel, Yueping Zhang, Zhen-Wei Cai, Joseph Fargnoli, Arvind Mathur, Alexandre L'Heureux, Joel C. Barrish, Rajeev S. Bhide, George M. Derbin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:2985-2989
We report herein a series of substituted N-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amines as inhibitors of vascular endothelial growth factor receptor-2 tyrosine kinase. Through structure–activity relationship studies, biochem
Autor:
Celia D’Arienzo, Daniel W. Kukral, Stephanie Barbosa, Steve Mortillo, John T. Hunt, Lawrence Wu, Punit Marathe, George M. Derbin, Joseph Fargnoli, Yong-Zheng Zhang, Robert M. Borzilleri, Joel C. Barrish, Zhongping Shi, Jeffrey A. Robl, Robert Jeyaseelan, Rajeev S. Bhide, Ligang Qian, Donna D. Wei, Junying Fan, Amrita Kamath, Xiaoping Zheng, Zhen-Wei Cai, Louis J. Lombardo, Barri Wautlet
Publikováno v:
Journal of Medicinal Chemistry. 51:1976-1980
A series of amino acid ester prodrugs of the dual VEGFR-2/FGFR-1 kinase inhibitor 1 (BMS-540215) was prepared in an effort to improve the aqueous solubility and oral bioavailability of the parent compound. These prodrugs were evaluated for their abil
Autor:
Georgia Cornelius, Joseph Fargnoli, Joseph G. Naglich, Yong Zhang, Shana L. Posy, Benjamin A. Seigal, Charu Chaudhry, Ling Li, Yingru Zhang, Ragini Vuppugalla, Robert J. Schmidt, Percy H. Carter, Gregory D. Vite, Ming Lei, Martin Patrick Allen, Donna D. Wei, Chunlei Wang, Michael M. Miller, Randy Talbott, Robert M. Borzilleri, Nicholas K. Terrett
Publikováno v:
ACS medicinal chemistry letters. 6(7)
A series of dimeric macrocyclic compounds were prepared and evaluated as antagonists for inhibitor of apoptosis proteins. The most potent analogue 11, which binds to XIAP and c-IAP proteins with high affinity and induces caspase-3 activation and ulti
Autor:
Johnni Gullo-Brown, Michael A. Poss, Wayne Vaccaro, Tram N. Huynh, Stephanie Barbosa, Carolyn S. Ricca, Mark E. Salvati, Veeraswamy Manne, Zhong Chen, Kenneth J. Leavitt, Soong-Hoon Kim, David R. Tortolani, Donna D. Wei
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:628-632
The synthesis and SAR of a series of pyrrolopyridazine MEK inhibitors are reported. Optimal activity was achieved by incorporation of a 4-phenoxyaniline substituent at C4 and an acylated amine at C6.