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Elaboration of thorough simplified vinca alkaloids as antimitotic agents based on pharmacophore similarity.

Abstract：

:Thorough simplification of vinca alkaloids based on pharmacophore similarity has been conducted. A concise process for the syntheses of target compounds was successfully developed with yields from poor to excellent (19-98%). Cell growth inhibitory activities of these synthesized compounds were evaluated in five cancer cell lines including MCF-7, MDA-MB-231, HepG2, HepG2/ADM and K562. Almost all compounds exhibited moderate antitumor activity with optimal IC50 value of 0.89 ± 0.07 μM in MCF-7 cells. Investigation of structure-activity relationship (SAR) indicates that electron-withdraw substituents on the ring contribute to the enhancement of the antitumor activities. The simplified vinca alkaloids are confirmed as antimitotic agents, which inhibit the polymerization of tubulin just like vinblastine.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Zheng J,Deng L,Chen M,Xiao X,Xiao S,Guo C,Xiao G,Bai L,Ye W,Zhang D,Chen H

doi

10.1016/j.ejmech.2013.04.057

subject

Has Abstract

pub_date

2013-07-01 00:00:00

pages

158-67

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(13)00289-4

journal_volume

65

pub_type

杂志文章

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