3,4-Dihydroquinazoline derivatives as novel selective T-type Ca2+ channel blockers

Yong Sup Lee; Bum Hoon Lee; Seong Jun Park; Soon Bang Kang; Hyewhon Rhim; Jin-Yong Park; Jung-Ha Lee; Seong-Woo Jeong; Jae Yeol Lee

doi:10.1016/j.bmcl.2004.04.090

3,4-Dihydroquinazoline derivatives as novel selective T-type Ca2+ channel blockers

Bioorg Med Chem Lett. 2004 Jul 5;14(13):3379-84. doi: 10.1016/j.bmcl.2004.04.090.

Authors

Yong Sup Lee¹, Bum Hoon Lee, Seong Jun Park, Soon Bang Kang, Hyewhon Rhim, Jin-Yong Park, Jung-Ha Lee, Seong-Woo Jeong, Jae Yeol Lee

Affiliation

¹ Life Sciences Division, Korea Institute of Science & Technology, PO Box 131, Cheongryang, Seoul 130-650, South Korea.

PMID: 15177437
DOI: 10.1016/j.bmcl.2004.04.090

Abstract

For LVA T-type Ca2+ channel blockers, 3,4-dihydroquinazoline derivatives as new scaffolds were prepared and evaluated for the inhibitory activity against two members of the recombinant T-type Ca2+ channel family. Among them, 8a (KYS05001, IC50=0.9 microM) was nearly equipotent with mibefradil (IC50=0.84 microM) and inhibited LVA T-type Ca2+ channel with greater efficacy than HVA Ca2+ channel.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Calcium Channel Blockers / chemical synthesis*
Calcium Channel Blockers / pharmacology
Calcium Channels, T-Type / drug effects
Calcium Channels, T-Type / metabolism*
Cell Line
Inhibitory Concentration 50
Mibefradil
Molecular Structure
Oocytes / drug effects
Patch-Clamp Techniques
Quinazolines / chemical synthesis*
Quinazolines / pharmacology

Substances

Calcium Channel Blockers
Calcium Channels, T-Type
Quinazolines
Mibefradil