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ID: ALA1140360

Journal: Bioorg Med Chem Lett

Title: Synthesis and biological activity of 3,4-dihydroquinazolines for selective T-type Ca2+ channel blockers.

Authors: Rhim H, Lee YS, Park SJ, Chung BY, Lee JY.

Abstract: We have synthesized 3,4-dihydroquinazoline derivatives for the potent and selective T-type Ca(2+) channel blockers and evaluated for their inhibitory activities against two subtypes T-type Ca(2+) channels and N-type Ca(2+) channels. Among them, 5b (KYS05044, IC(50)=0.56+/-0.10 microM) was identified as potent T-type Ca(2+) channel blocker with in vitro selectivity profile at meaningful level (T/N-type, SI=>100).

CiteXplore: 15603940

DOI: 10.1016/j.bmcl.2004.10.078