Novel cyanocombretastatins as potent tubulin polymerisation inhibitors
Novel cyanocombretastatins as potent tubulin polymerisation inhibitors
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DOI：
10.1016/j.bmcl.2012.08.089
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发表时间：
2012-11-01
影响因子：
2.7
通讯作者：
Rossington, Steven B.
中科院分区：
文献类型：
--
作者：
Jalily, Pouria H.;Hadfield, John A.;Rossington, Steven B.
A series of novel cyanocombretastatins bearing a 3,4,5-trimethoxyphenyl moiety combined with a variety of substituted phenyl rings, were synthesised and their antitumour activity was evaluated. The Z-cyanocombretastatins were synthesised in a one-step protocol in high purity and yield. Fluoro, bromo, iodo, and derivatives with boronic acid and an ethyne function at meta position of the B ring were synthesised. In vitro MTT bioassays against human chronic myelogenous leukaemia (K562) and transfected breast adenocarcinoma (MDA NQO1) cell lines, revealed promising IC50 inhibitory values in nanomolar range (
