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Discovery of potent T-type calcium channel blocker

Authors
Seo, Han Na; Choi, Ja Youn; Choe, Yun Jeong; Kim, Yoonjee; Rhim, Hyewhon; Lee, So Ha; Kim, Jungahn; Joo, Dong Jun; Lee, Jae Yeol
Issue Date
2007-11-01
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Citation
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.17, no.21, pp.5740 - 5743
Abstract
The intensive SAR study of 3,.4-dihydroquinazoline series led to the most potent compound 10 (KYS05090: IC50 = 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. (c) 2007 Elsevier Ltd. All rights reserved.
Keywords
BIOLOGICAL EVALUATION; STABLE ANGINA; DERIVATIVES; ANTAGONISTS; RELEASE; DESIGN; MUSCLE; PAIN; BIOLOGICAL EVALUATION; STABLE ANGINA; DERIVATIVES; ANTAGONISTS; RELEASE; DESIGN; MUSCLE; PAIN; T-type calcium channel; 3,4-dihydroquinazoline; kurtoxin; blocker
ISSN
0960-894X
URI
https://pubs.kist.re.kr/handle/201004/133990
DOI
10.1016/j.bmcl.2007.08.070
Appears in Collections:
KIST Article > 2007
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