T-type Ca2+ channel blockers suppress the growth of human cancer cells

Bioorg Med Chem Lett. 2008 Jul 15;18(14):3899-901. doi: 10.1016/j.bmcl.2008.06.034. Epub 2008 Jun 14.

Abstract

In order to further clarify the role of T-type Ca(2+) channels in cell proliferation, we have measured the growth inhibition of human cancer cells by using our potent T-type Ca(2+) channel blockers. As a result, KYS05090, a most potent T-type Ca(2+) channel blocker, was found to be as potent as doxorubicin against some human cancer cells without acute toxicity. Therefore, this letter provides the biological results that T-type calcium channel is important in regulating the important cellular phenotype transition leading to cell proliferation, and thus novel T-type Ca(2+) channel blocker presents new prospects for cancer treatment.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Calcium Channel Blockers / chemical synthesis*
  • Calcium Channel Blockers / pharmacology*
  • Calcium Channels, T-Type / chemistry*
  • Calcium Channels, T-Type / metabolism
  • Cell Line, Tumor
  • Cell Proliferation
  • Chemistry, Pharmaceutical / methods
  • Doxorubicin / pharmacology
  • Drug Design
  • Drug Screening Assays, Antitumor*
  • Humans
  • Inhibitory Concentration 50
  • Mice
  • Models, Chemical
  • Quinazolines / chemical synthesis
  • Quinazolines / pharmacology*

Substances

  • Antineoplastic Agents
  • Calcium Channel Blockers
  • Calcium Channels, T-Type
  • KYS05080
  • Quinazolines
  • Doxorubicin