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Issue 5, 2015
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Synthesis and biological evaluation of 2,3-diarylthiophene analogues of combretastatin A-4

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Abstract

A series of novel 2,3-diarylthiophene analogues of combretastatin A-4 (CA-4) were designed with a rigid thiophene moiety to retain the cis-olefin configuration of CA-4 and were subsequently synthesised. All of the target compounds were evaluated for their in vitro anti-proliferative activities. Among these compounds, 5f and 8d exhibited superior potency against different tumour cell lines with IC50 values at sub-micromolar levels. Moreover, compound 8d significantly inhibited tubulin polymerisation to microtubules and caused microtubule destabilisation. In addition, a molecular modelling study of compound 8d was performed to clarify its binding mode at the colchicine site in the tubulin dimer and to provide a basis for further structure-guided design of novel CA-4 analogues.

Graphical abstract: Synthesis and biological evaluation of 2,3-diarylthiophene analogues of combretastatin A-4

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Article information


Submitted
20 Jan 2015
Accepted
01 Apr 2015
First published
02 Apr 2015

Med. Chem. Commun., 2015,6, 971-976
Article type
Concise Article

Synthesis and biological evaluation of 2,3-diarylthiophene analogues of combretastatin A-4

Z. Wang, Q. Yang, Z. Bai, J. Sun, X. Jiang, H. Song, Y. Wu and W. Zhang, Med. Chem. Commun., 2015, 6, 971
DOI: 10.1039/C5MD00028A

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