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  • Title: Pyrazolone based TGFbetaR1 kinase inhibitors.
    Author: Guckian K, Carter MB, Lin EY, Choi M, Sun L, Boriack-Sjodin PA, Chuaqui C, Lane B, Cheung K, Ling L, Lee WC.
    Journal: Bioorg Med Chem Lett; 2010 Jan 01; 20(1):326-9. PubMed ID: 19914068.
    Abstract:
    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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