Novel Colchicine Derivatives and their Anti-cancer Activity

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

Journal Name: Current Topics in Medicinal Chemistry

Volume 17 , Issue 22 , 2017

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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.

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

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Article Details

VOLUME: 17
ISSUE: 22
Year: 2017
Page: [2538 - 2558]
Pages: 21
DOI: 10.2174/1568026617666170104143618
Price: $58

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