Zobrazeno 1 - 7
of 7
pro vyhledávání: '"Chunshan Xie"'
Autor:
Matthew D. Hill, Haiquan Fang, Derek Norris, George V. Delucca, Hong Huang, Mikkel DeBenedetto, Claude Quesnelle, William D. Schmitz, John S. Tokarski, Steven Sheriff, Chunhong Yan, Caroline Fanslau, Zuzana Haarhoff, Christine Huang, Melissa Kramer, Shilpa Madari, Krista Menard, Laura Monereau, John Morrison, Nirmala Raghavan, Eric E. Shields, Jean Simmermacher-Mayer, Michael Sinz, Ching Kim Tye, Richard Westhouse, Chunshan Xie, Haiying Zhang, Lisa Zhang, Tatyana Zvyaga, Francis Lee, Ashvinikumar V. Gavai, Andrew P. Degnan
Publikováno v:
ACS Medicinal Chemistry Letters. 13:1165-1171
We describe the synthesis of triazole-containing carboline derivatives and their utility as bromodomain and extra-terminal (BET) inhibitors. A convergent synthetic route permitted the detailed investigation of deuteration and fluorination strategies
Autor:
Michael A. Schmidt, Chunshan Xie, Naidu S. Chowdari, Ankita G. Niyogi, David R. Langley, Heng Cheng, Gregory D. Vite, Sivakrishna Guturi, Rajappa Vaidyanathan, Sanjeev Gangwar, Ivar M. McDonald, Kishorekumar Kanagavel, Yichen Tan, Prasanna Sivaprakasam, Souvik Rakshit, Chin Pan, Umamaheswararao Kanusu, Martin D. Eastgate, Madhura Deshpande, Somprabha Sidhar, Bin Zheng, Christiana I. Iwuagwu, Michael R. Luzung, Ganapathy Sarma, Kevin M. Peese, Thirumalai Lakshminarasimhan, Patrick G. Holder, Pina M. Cardarelli, Patricia Cho, Srikanth Kotapati, Chetana Rao
Publikováno v:
ACS Med Chem Lett
[Image: see text] A new series with the tetrahydroisoquinoline-fused benzodiazepine (TBD) ring system combined with the surrogates of (1-methyl-1H-pyrrol-3-yl)benzene (“MPB”) payloads were designed and executed for conjugation with a monoclonal a
Autor:
Chunshan Xie, Qian Zhang, Anindya Sarkar, Joseph G. Naglich, Heng Cheng, Prasanna Sivaprakasam, Sanjeev Gangwar, Anushka C. Galasiti Kankanamalage, Dale L. Boger
Publikováno v:
Med Chem Res
A comprehensive SAR study of a putative TLR 3/8/9 agonist was conducted. Despite the excitement surrounding the potential of the first small molecule TLR3 agonist with a compound that additionally displayed agonist activity for TLR8 and TLR9, compoun
Autor:
Andrew P. Degnan, Haiquan Fang, Tatyana Zvyaga, Zuzana Haarhoff, Claude A. Quesnelle, Melissa Kramer, Frank Marsilio, Richard A. Westhouse, John S. Tokarski, Shilpa Madari, Jiuqiao Zhao, Amy Wiebesiek, Chunhong Yan, Francis Y. Lee, Michael Sinz, John Morrison, Jean Simmermacher-Mayer, Carolynn Fanslau, Steven Sheriff, Lisa Huang, Ashvinikumar V. Gavai, Chunshan Xie, Matthew D. Hill, Gerry Everlof
Publikováno v:
Bioorganicmedicinal chemistry letters. 51
We describe our efforts to introduce structural diversity to a previously described triazole-containing N1-carboline series of bromodomain and extra-terminal (BET) inhibitors. N9 carbolines were designed to retain favorable binding interactions that
Autor:
Gary G. Cao, Min Zhou, Ramya Jayaram, Douglas B. Moore, Andres S. Hernandez, Tao Wang, Jean M. Whaley, Yue-Zhong Shu, Carrie Xu, Lori Kunselman, Atsu Apedo, William R. Ewing, Reshma Panemangalore, Qi Gao, Arvind Mathur, Richard Rampulla, Bradley A. Zinker, Lauren Haque, Mary Ellen Cvijic, Marta Dabros, Arun Kumar Gupta, Heng Liu, Jeffrey A. Robl, Bruce A. Ellsworth, Jun Shi, Zhengxiang Gu, Jason J. Wilkes, Akin H. Davulcu, Kristin N. Williams, Elizabeth A. Dierks, John Krupinski, Zhenqiu Hong, Edward J. Brady, Ximao Wu, Qin Sun, Hong Cai, Chunshan Xie, Elizabeth A. Jurica, Kimberly A. Foster
Publikováno v:
Journal of medicinal chemistry. 61(3)
G protein-coupled receptor 40 (GPR40) has become an attractive target for the treatment of diabetes since it was shown clinically to promote glucose-stimulated insulin secretion. Herein, we report our efforts to develop highly selective and potent GP
Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode
Autor:
William R. Ewing, Carrie Xu, Heng Liu, Brian J. Murphy, Neil Flynn, Tao Wang, Douglas B. Moore, Lori Kunselman, Bruce A. Ellsworth, Elizabeth A. Jurica, Kimberly A. Foster, Atsu Apedo, Yuan Tian, Yang Hong, Arvind Mathur, Bradley A. Zinker, Biji Jacob, Kristin N. Williams, Min Zhou, Brad D. Maxwell, Gary Cao, Andres S. Hernandez, Qin Sun, Hong Cai, Jean M. Whaley, Elizabeth A. Dierks, Joel C. Barrish, Dora M. Schnur, Ximao Wu, Doree F. Sitkoff, Mary Ellen Cvijic, Richard Rampulla, Chunshan Xie, David S. Nirschl, Reshma Panemangalore, Michael B. Hicks, Jeffrey A. Robl, Jason J. Wilkes
Publikováno v:
Journal of medicinal chemistry. 60(4)
A novel series of pyrrolidine-containing GPR40 agonists is described as a potential treatment for type 2 diabetes. The initial pyrrolidine hit was modified by moving the position of the carboxylic acid, a key pharmacophore for GPR40. Addition of a 4-
Autor:
Jurica, Elizabeth A., Ximao Wu, Williams, Kristin N., Hernandez, Andres S., Nirschl, David S., Rampulla, Richard A., Mathur, Arvind, Min Zhou, Cao, Gary, Chunshan Xie, Jacob, Biji, Hong Cai, Tao Wang, Murphy, Brian J., Heng Liu, Xu, Carrie, Kunselman, Lori K., Hicks, Michael B., Qin Sun, Schnur, Dora M.
Publikováno v:
Journal of Medicinal Chemistry; 2/23/2017, Vol. 60 Issue 4, p1417-1431, 15p