Discovery of potent T-type calcium channel blocker.

Bioorg Med Chem Lett

Research Institute for Basic Sciences and Department of Chemistry, Kyung Hee University, Seoul 130-701, Republic of Korea.

Published: November 2007

The intensive SAR study of 3,4-dihydroquinazoline series led to the most potent compound 10 (KYS05090: IC(50)=41+/-1 nM) against T-type calcium channel and its potency is nearly comparable to that of Kurtoxin. As a small organic molecule, this compound showed the highest blocking activity reported to date.

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http://dx.doi.org/10.1016/j.bmcl.2007.08.070DOI Listing

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