2. Academic Validation
  3. 3,4-Dihydroquinazoline derivatives as novel selective T-type Ca2+ channel blockers

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.
Yong Sup Lee 1,  Bum Hoon Lee,  Seong Jun Park,  Soon Bang Kang,  Hyewhon Rhim,  Jin-Yong Park,  Jung-Ha Lee,  Seong-Woo Jeong,  Jae Yeol Lee
Affiliations

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.

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