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Bioorg Med Chem Lett ; 17(21): 5740-3, 2007 Nov 01.
Article in English | MEDLINE | ID: mdl-17869104

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.


Subject(s)
Calcium Channel Blockers/chemistry , Calcium Channel Blockers/pharmacology , Calcium Channels, T-Type/drug effects , Quinazolines/chemistry , Quinazolines/pharmacology , Cell Line , Humans , Structure-Activity Relationship
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