当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Synthesis and biological evaluation of novel 3,4-diaryl-1,2,5-selenadiazol analogues of combretastatin A-4.

Synthesis and biological evaluation of novel 3,4-diaryl-1,2,5-selenadiazol analogues of combretastatin A-4.

Abstract：

:A set of novel selenium-containing heterocyclic analogues of combretastatin A-4 (CA-4) have been designed and synthesised using a rigid 1,2,5-selenadiazole as a linker to fix the cis-orientation of ring-A and ring-B. All of the target compounds were evaluated for their in vitro anti-proliferative activities. Among these compounds, compounds 3a, 3i, 3n and 3q exhibited superior potency against different tumour cell lines with IC50 values at the nanomolar level. Moreover, compound 3n significantly induced cell cycle arrest in the G2/M phase, inhibited tubulin polymerisation into microtubules and caused microtubule destabilisation. A molecular modelling study of compound 3n was performed to elucidate its binding mode at the colchicine site in the tubulin dimer and to provide a basis for the further structure-guided design of novel CA-4 analogues.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Guan Q,Yang F,Guo D,Xu J,Jiang M,Liu C,Bao K,Wu Y,Zhang W

doi

10.1016/j.ejmech.2014.09.046

subject

Has Abstract

pub_date

2014-11-24 00:00:00

pages

1-9

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(14)00864-2

journal_volume

87

pub_type

杂志文章

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