Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Yuo-Ling Chou"'
Autor:
Richard I. Feldman, Gary Phillips, Marc Adler, Daguang Zhu, Elena Ho, Wheeseong Lee, Mark A. Polokoff, Hongyi Yu, Dao Lentz, Marc Whitlow, Arnaiz Damian O, Kochanny Monica, Babu Subramanyam, Imadul Islam, James M. Wu, Judi Bryant, Yuo-Ling Chou
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3814-3818
HTS screening identified 1 with micromolar inhibitory activity against PDK1. Optimization of 1 afforded 4i (BX-517) which has single-digit nanomolar activity against PDK1 and excellent selectivity against PKA.
Autor:
Dave Davey, Arnaiz Damian O, Shou-Fu Lu, Laura Dunning, Yuo-Ling Chou, James Onuffer, Robert G. Wei, Gary Phillips, Wheeseong Lee, Bin Ye
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:231-234
High throughput screening (HTS) led to the identification of the guanylhydrazone of 2-(4-chlorobenzyloxy)-5-bromobenzaldehyde as a CCR5 receptor antagonist. Initial modifications of the guanylhydrazone series indicated that substitution of the benzyl
Autor:
Chad A. Van Huis, Jeremy J. Edmunds, Kenneth J. Shaw, Marc Whitlow, Arnaiz Damian O, Marc Adler, Cuiman Cai, David R. Light, Kamlai Saiya-Cork, J. Adam Willardsen, Lakshmi Narasimhan, Erli Zhang, Stephen T. Rapundalo, Kevin J. Filipski, Wayne L. Cody, Kirk Mclean, Danette Dudley, Jeffrey T. Kohrt, Cecile McKnight, Robert J. Leadley, Yuo-Ling Chou
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:4752-4756
The activated Factor VII/tissue factor complex (FVIIa/TF) plays a key role in the formation of blood clots. Inhibition of this complex may lead to new antithrombotic drugs. An X-ray crystal structure of a fluoropyridine-based FVIIa/TF inhibitor bound
Publikováno v:
Tetrahedron Letters. 39:757-760
A novel serine-derived linker has been developed that allows phenolic templates to be cleaved from the resin with fluoride ion. The linker is stable to acids such as TFA and bases such as pyrrolidine. The linker should provide utility in multi-step s
Publikováno v:
Tetrahedron Letters. 37:3963-3966
The Pictet-Spengler cyclization utilizing tryptophan linked to the Kaiser oxime resin and aldehydes affords the 1,2,3,4-tetrahydro-β-carboline derivatives 6 which can be further functionalized by reaction with acylating reagents. Nucleophilic cleava
Autor:
Yuo-Ling Chou, John Morser, Marc Adler, Wheeseong Lee, Joseph Post, David R. Light, Kochanny Monica, Karna Lyn Sacchi, Dao Lentz, Arnaiz Damian O, Marc Whitlow, Bin Ye, Amy Liang, Ron Vergona, Richard W. Fitch, Mark E. Sullivan, Sarah Cheeseman, Janice Ewing, Zuchun Zhao, Babu Subramanyam, Kathy White, Kenneth J. Shaw, Karanjawala Rushad E, Janette Walters, Brian D. Griedel, Yi-Xin Wang, William P. Dole, Michael M. Morrissey, Steven T. Sakata, Galina Rumennik, Shung C. Wu
Publikováno v:
Journal of medicinal chemistry. 50(13)
There remains a high unmet medical need for a safe oral therapy for thrombotic disorders. The serine protease factor Xa (fXa), with its central role in the coagulation cascade, is among the more promising targets for anticoagulant therapy and has bee
Autor:
Amy Liang, Dao Lentz, Lan Trinh, Yuo-Ling Chou, Brad O. Buckman, David R. Light, Raju Mohan, Kenneth J. Shaw, Morrissey Michael M, Meg Mccarrick
Publikováno v:
Bioorganicmedicinal chemistry letters. 15(9)
Reductive amination followed by acylation of polymer-linked formyl aryl amidines generate combinatorial libraries of aryl amidines 8-13. Potent small molecule naphthylamidine inhibitors 12 (Ki
Autor:
Bin Ye, Yuo-Ling Chou, Rushad Karanjawala, Wheeseong Lee, Shou-Fu Lu, Kenneth J. Shaw, Steven Jones, Dao Lentz, Amy Liang, Jih-Lie Tseng, Qingyu Wu, Zuchun Zhao
Publikováno v:
Bioorganicmedicinal chemistry letters. 14(3)
Compound 2 was identified by high throughput screening as a novel PAI-1 inhibitor. Systematic optimization of the A, B, and C segments of 2 resulted in the identification of a more potent compound 39 with good oral bioavailability. The synthesis and
Publikováno v:
ChemInform. 34
Autor:
Brian D. Griedel, Keith Eagen, Shung C. Wu, Morrissey Michael M, Yuo-Ling Chou, Karna Lyn Sacchi, Lan Trinh, David D. Davey, Kenneth J. Shaw, Karanjawala Rushad E, Dao Lentz, Kochanny Monica, Amy Liang, Gary Phillips
Publikováno v:
Bioorganicmedicinal chemistry letters. 13(3)
Compound 1 was identified by high throughput screening as a novel, potent, non-amidine factor Xa inhibitor with good selectivity against thrombin and trypsin. A series of modifications of the three aromatic groups of 1 was investigated. Substitution