Rapid synthesis of triazine inhibitors of inosine monophosphate dehydrogenase

William J Pitts; Junqing Guo; T G Murali Dhar; Zhongqi Shen; Henry H Gu; Scott H Watterson; Mark S Bednarz; Bang Chi Chen; Joel C Barrish; Donna Bassolino; Daniel Cheney; Catherine A Fleener; Katherine A Rouleau; Diane L Hollenbaugh; Edwin J Iwanowicz

doi:10.1016/s0960-894x(02)00351-7

Rapid synthesis of triazine inhibitors of inosine monophosphate dehydrogenase

Bioorg Med Chem Lett. 2002 Aug 19;12(16):2137-40. doi: 10.1016/s0960-894x(02)00351-7.

Authors

William J Pitts¹, Junqing Guo, T G Murali Dhar, Zhongqi Shen, Henry H Gu, Scott H Watterson, Mark S Bednarz, Bang Chi Chen, Joel C Barrish, Donna Bassolino, Daniel Cheney, Catherine A Fleener, Katherine A Rouleau, Diane L Hollenbaugh, Edwin J Iwanowicz

Affiliation

¹ Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. [email protected]

PMID: 12127522
DOI: 10.1016/s0960-894x(02)00351-7

Abstract

A series of novel triazine-based small molecule inhibitors (IV) of inosine monophosphate dehydrogenase was prepared. The synthesis and the structure-activity relationships (SAR) derived from in vitro studies are described.

MeSH terms

Animals
Cell Division / drug effects
Cells, Cultured
IMP Dehydrogenase / antagonists & inhibitors*
Inhibitory Concentration 50
Models, Molecular
Molecular Conformation
Molecular Structure
Structure-Activity Relationship
T-Lymphocytes / cytology
T-Lymphocytes / drug effects
Triazines / chemical synthesis*
Triazines / chemistry
Triazines / pharmacology*

Substances

Triazines
IMP Dehydrogenase