Novel colchicine derivatives and their anti-cancer activity

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

Research output: Contribution to journalReview article

8 Scopus citations

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 over-expressed in cancer and decreasing it for normal cells thereby widening the therapeutic window.

Original languageEnglish (US)
Pages (from-to)2538-2558
Number of pages21
JournalCurrent Topics in Medicinal Chemistry
Volume17
Issue number22
DOIs
StatePublished - Sep 1 2017

Keywords

  • Animal tests
  • Anti-cancer
  • Colchicine Scaffold
  • Pharmacophore
  • Tubulin β isotypes

ASJC Scopus subject areas

  • Drug Discovery

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  • Cite this

    Johnson, L., Goping, I. S., Rieger, A., Mane, J. Y., Huzil, T., Banerjee, A., Luduena, R., Hassani, B., Winter, P., & Tuszynski, J. A. (2017). Novel colchicine derivatives and their anti-cancer activity. Current Topics in Medicinal Chemistry, 17(22), 2538-2558. https://doi.org/10.2174/1568026617666170104143618