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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

New Anti-Mitotic Drugs with Distinct Anti-Calmodulin Activity

Author(s): F. Orosz, I. Horvath and J. Ovadi

Volume 6, Issue 10, 2006

Page: [1145 - 1157] Pages: 13

DOI: 10.2174/138955706778560094

Price: $65


Bisindole Vinca alkaloids target microtubule system causing anti-mitotic activity. The problem of their clinical application is the lack of selectivity resulting in toxic side effects. In this paper we review the late history of new bisindole derivatives focusing on KARs recognized as potent anti-cancer drugs with low side effect. KARs, just as other bisindoles, impede microtubule assembly of mitotic spindle, however, they display no anti-calmodulin activity. This new drug family appears to be less potent than vinblastine in vitro systems, but it shows high antitumor efficacy with considerably higher doses being well tolerated in the animal tumor models. 3D data of calmodulin complexed with KAR-2 explain the specificity and unique pharmacology of KAR derivatives.

Keywords: Tubulin/microtubule, vinca alkaloid, anticancer agent, calmodulin, bisindoles

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