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.
