Synthesis of terphenyl benzimidazoles as tubulin polymerization inhibitors

被引：47

作者：

Kamal, Ahmed ^{[1
,3
]}

Reddy, M. Kashi ^{[1
]}

Shaik, Thokhir B. ^{[2
]}

Rajender ^{[1
]}

Srikanth, Y. V. V. ^{[1
]}

Reddy, V. Santhosh ^{[1
]}

Kumar, G. Bharath ^{[1
]}

Kalivendi, Shasi V. ^{[2
]}

机构：

[1] Indian Inst Chem Technol, Div Organ Chem, Hyderabad 500607, Andhra Pradesh, India

[2] Indian Inst Chem Technol, Ctr Chem Biol, Hyderabad 500607, Andhra Pradesh, India

[3] King Saud Univ, Coll Sci, Dept Chem, Catalyt Chem Chair, Riyadh 11451, Saudi Arabia

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 50卷

关键词：

Terphenyls; Suzuki coupling; Benzimidazoles; Anticancer agents; Tubulin polymerization; ANTICANCER AGENTS; DERIVATIVES; POTENT; MICROTUBULES; APOPTOSIS; IDENTIFICATION; ATROMENTIN; DISCOVERY; KINASES; BINDING;

D O I：

10.1016/j.ejmech.2012.01.004

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of new terphenyl benzimidazoles (3a-z and 3aa-ad) were synthesized and evaluated for their anticancer activity. All the 30 compounds have shown moderate to good anticancer potency, however some of the compounds (3j, 3m-t and 3aa-ad) exhibited prominent anticancer potency with GI(50) values ranging from <0.1 to 9.72 mu M. These compounds exhibit G2/M phase arrest and the analysis of tubulin by Western blot experiments in case of 3t and 3ad shows the disturbances that are caused in the ratio of soluble versus polymerized tubulin in cells. Compounds 3t and 3ad are the most promising candidates amongst the series and has the potential to be taken up for further detailed studies either alone or in combination with the existing therapies. (C) 2012 Elsevier Masson SAS. All rights reserved.

引用

页码：9 / 17

页数：9

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