Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Wheeseong Lee"'
Publikováno v:
Trends in Endocrinology & Metabolism. 33:722-735
Metabolites generated from cellular and tissue metabolism have been rediscovered in recent years as signalling molecules. They may act as cofactor of enzymes or be linked to proteins as post-translational modifiers. They also act as ligands for speci
Publikováno v:
Inflammatory Bowel Diseases. 29:S4-S5
Macrophages are the first line of defense against self-stimuli and non-self-pathogens and adopt diverse activation states by reprogramming their cell metabolism and thereby polarizing their phenotypes in order to drive their pro-inflammatory or pro-r
Autor:
Wheeseong Lee, Scott E. Denmark
Publikováno v:
Chemistry - An Asian Journal. 3:327-341
A model compound was de- signed to study the relative orientation of enol silane and carbonyl moieties in the Mukaiyama aldol reaction.The cyclization must proceed with either a synclinal or an antiperiplanar orienta- tion of the aldehyde with respec
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:
Dao Lentz, Marc Whitlow, Kenneth J. Shaw, Karna Lyn Sacchi, Sakata Steven T, Janette Walters, Kathy White, Joseph Post, Bin Ye, Wheeseong Lee, Kochanny Monica, Elena Ho, Amy Liang, Ron Vergona, Janice Ewing, Morrissey Michael M, Karanjawala Rushad E, Gary Phillips, Zuchun Zhao, Brian D. Griedel, Babu Subramanyam, Marc Adler
Publikováno v:
Bioorganic & Medicinal Chemistry. 15:2127-2146
A series of thiophene-containing non-amidine factor Xa inhibitors is described. Simple methyl-substituted thiophene analogs were relatively weak inhibitors. However, introduction of hydrophilic substituents at C-4 or C-5 of the thiophene afforded inh
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:
Kenneth J. Shaw, Bauer Shawn M, Amy Liang, Brad O. Buckman, Wheeseong Lee, Brian D. Griedel, Ghannam Ameen F, Qingyu Wu, Zuchun Zhao, Khim Seock-Kyu, Karna Lyn Sacchi, Bin Ye
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:3361-3365
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. 26
Autor:
Scott E. Denmark, Wheeseong Lee
Publikováno v:
Tetrahedron Letters. 33:7729-7732
In aqueous medium, base-induced aldol condensations of keto aldehyde 1 show high anti-selectivity independent of metal ion and water content of the solvent. The acid-induced aldol condensations affords syn-aldol products in variable selectivity depen
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