Novel Colchicine Derivatives and their Anti-cancer Activity

Title:Novel Colchicine Derivatives and their Anti-cancer Activity

Volume: 17 Issue: 22

Author(s): Lorelei Johnson*, Ing Swie Goping, Aja Rieger, Jonathan Y. Mane, Torin Huzil, Asok Banerjee, Richard Luduena, Bashar Hassani, Philip Winter and Jack A. Tuszynski

Affiliation:

• Department of Oncology, University of Alberta, Edmonton, Alberta,Canada

Keywords: Anti-cancer, Tubulin β isotypes, Colchicine Scaffold, Pharmacophore, Animal tests

Abstract: In this paper we provide an overview of the status of various colchicine derivatives in preclinical development with special focus on their anti-cancer activity. We discuss several groups of compounds that have been designed to differentially bind with specific affinities for tubulin β isotypes, especially in regard to βIII, which is commonly over-expressed in cancer. Computational prediction, protein-based and cell-based assays are summarized as well as some animal tests conducted on these compounds. It is concluded that an untapped potential exists for exploiting the colchicine scaffold as a pharmacophore with the possibility of increasing its affinity for tubulin isotypes overexpressed in cancer and decreasing it for normal cells thereby widening the therapeutic window.

Cite this article as:

Johnson Lorelei*, Goping Swie Ing, Rieger Aja, Mane Y. Jonathan, Huzil Torin, Banerjee Asok, Luduena Richard, Hassani Bashar, Winter Philip and Tuszynski A. Jack, Novel Colchicine Derivatives and their Anti-cancer Activity, Current Topics in Medicinal Chemistry 2017; 17 (22) . https://dx.doi.org/10.2174/1568026617666170104143618