2. Academic Validation
  3. Synthesis and biological evaluation of colchicine B-ring analogues tethered with halogenated benzyl moieties

Synthesis and biological evaluation of colchicine B-ring analogues tethered with halogenated benzyl moieties

  • J Med Chem. 2012 Dec 27;55(24):11062-6. doi: 10.1021/jm301151t.
Laura Cosentino 1,  Mariano Redondo-Horcajo,  Ying Zhao,  Ana Rita Santos,  Kaniz F Chowdury,  Victoria Vinader,  Qasem M A Abdallah,  Hamdy Abdel-Rahman,  Jérémie Fournier-Dit-Chabert,  Steven D Shnyder,  Paul M Loadman,  Wei-shuo Fang,  José Fernando Díaz,  Isabel Barasoain,  Philip A Burns,  Klaus Pors
Affiliations

Affiliation

  • 1 Institute of Cancer Therapeutics, University of Bradford, Bradford, West Yorkshire, BD7 1DP, UK.
PMID: 23176628 DOI: 10.1021/jm301151t
Abstract

Deacetylcolchicine was reacted with substituted benzyl halides to provide a library of compounds for biological analysis. Compound 7 (3,4-difluorobenzyl-N-aminocolchicine) was shown to possess cytotoxicity in Cancer cell lines in the low nanomolar range. Significantly, it showed no loss of activity in the resistant A2780AD ovarian carcinoma cell line known to overexpress the ABCB1 drug transporter and was also unaffected by overexpression of class III β-tubulin in HeLa transfected cells.

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