Discovery of potent T-type calcium channel blocker.
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.
Seo
Han Na
HN
Research Institute for Basic Sciences and Department of Chemistry, Kyung Hee University, Seoul 130-701, Republic of Korea.
Choi
Ja Youn
JY
Choe
Yun Jeong
YJ
Kim
Yoonjee
Y
Rhim
Hyewhon
H
Lee
So Ha
SH
Kim
Jungahn
J
Joo
Dong Jun
DJ
Lee
Jae Yeol
JY
D002121:Calcium Channel Blockers / Q000737:chemistry* / Q000494:pharmacology*; D020747:Calcium Channels, T-Type / Q000187:drug effects*; D002460:Cell Line; D006801:Humans; D011799:Quinazolines / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D002121:Calcium Channel Blockers; D020747:Calcium Channels, T-Type; D011799:Quinazolines