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Synthesis and biological evaluation of novel T-type calcium channel blockers.
Choi, Ja Youn; Seo, Han Na; Lee, Min Joo; Park, Seong Jun; Park, Sung Jun; Jeon, Ji Young; Kang, Joo Hi; Pae, Ae Nim; Rhim, Hyewhon; Lee, Jae Yeol.
Bioorg Med Chem Lett ; 17(2): 471-5, 2007 Jan 15.
Article in English | MEDLINE | ID: mdl-17064894

ABSTRACT

3,4-Dihydroquinazoline analogues substituted by N-methyl-N-(5-pyrrolidinopentyl)amine at the 2-position were synthesized and their blocking effects were evaluated for T- and N-type calcium channels. Compound 11b (KYS05080), compared to mibefradil (IC50=1.34+/-0.49 microM), was about 5-fold potent (IC50=0.26+/-0.01 microM) for T-type calcium channel (alpha1G) blocking and its selectivity of T/N-type was also improved (7.5 versus 1.4 of mibefradil).


Subject(s)
Calcium Channel Blockers/chemical synthesis , Calcium Channel Blockers/pharmacology , Calcium Channels, T-Type/drug effects , Pyrrolidines/chemical synthesis , Pyrrolidines/pharmacology , Quinazolines/chemical synthesis , Quinazolines/pharmacology , Animals , Calcium Channels, N-Type/drug effects , Cell Line, Tumor , Crystallography, X-Ray , Indicators and Reagents , Magnetic Resonance Spectroscopy , Mibefradil/pharmacology , Models, Molecular , Oocytes/drug effects , Oocytes/metabolism , Xenopus
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