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 language | English (US) |
---|---|
Pages (from-to) | 2538-2558 |
Number of pages | 21 |
Journal | Current topics in medicinal chemistry |
Volume | 17 |
Issue number | 22 |
DOIs | |
State | Published - Sep 1 2017 |
Keywords
- Animal tests
- Anti-cancer
- Colchicine Scaffold
- Pharmacophore
- Tubulin β isotypes
ASJC Scopus subject areas
- Drug Discovery