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Novel Colchicine Derivatives and their Anti-cancer Activity

[ Vol. 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   Pages 2538 - 2558 ( 21 )

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

Affiliation:

Department of Oncology, University of Alberta, Edmonton, Alberta, Department of Biochemistry, University of Alberta, Edmonton, Alberta, Department of Biochemistry, University of Alberta, Edmonton, Alberta, Department of Oncology, University of Alberta, Edmonton, Alberta, Department of Oncology, University of Alberta, Edmonton, Alberta, Department of Biochemistry, University of Texas Health Science Center at San Antonio, San Antonio, TX 78240, Department of Biochemistry, University of Texas Health Science Center at San Antonio, San Antonio, TX 78240, Department of Oncology, University of Alberta, Edmonton, Alberta, Department of Oncology, University of Alberta, Edmonton, Alberta, Department of Oncology, University of Alberta, Edmonton, Alberta

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