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Bioorg Med Chem Lett ; 18(14): 3899-901, 2008 Jul 15.
Article in English | MEDLINE | ID: mdl-18585035

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.


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