Discovery of potent T-type calcium channel blocker

  • Bioorg Med Chem Lett. 2007 Nov 1;17(21):5740-3. doi: 10.1016/j.bmcl.2007.08.070.
Han Na Seo  1 ,  Ja Youn Choi ,  Yun Jeong Choe ,  Yoonjee Kim ,  Hyewhon Rhim ,  So Ha Lee ,  Jungahn Kim ,  Dong Jun Joo ,  Jae Yeol Lee
Affiliations
  • 1. Research Institute for Basic Sciences and Department of Chemistry, Kyung Hee University, Seoul 130-701, Republic of Korea.
PMID: 17869104 DOI: 10.1016/j.bmcl.2007.08.070
Abstract

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.