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Pyrazolone based TGFbetaR1 kinase inhibitors.

Guckian, Kevin; Carter, Mary Beth; Lin, Edward Yin-Shiang; Choi, Michael; Sun, Lihong; Boriack-Sjodin, P Ann; Chuaqui, Claudio; Lane, Benjamin; Cheung, Kam; Ling, Leona; Lee, Wen-Cherng.
Bioorg Med Chem Lett; 20(1): 326-9, 2010 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-19914068
Interruption of TGFbeta signaling through inhibition of the TGFbetaR1 kinase domain may prove to have beneficial effect in both fibrotic and oncological diseases. Herein we describe the SAR of a novel series of TGFbetaR1 kinase inhibitors containing a pyrazolone core. Most TGFbetaR1 kinase inhibitors described to date contain a core five-membered ring bearing N as H-bond acceptor. Described herein is a novel strategy to replace the core structure with pyrazolone ring, in which the carbonyl group is designed as an H-bond acceptor to interact with catalytic Lys 232.
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