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
Current Topics in Medicinal Chemistry
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.
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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
DOI https://dx.doi.org/10.2174/1568026617666170104143618 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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