Discovery of Novel 2-Aryl-4-benzoyl-imidazole (ABI-III) Analogues Targeting Tubulin Polymerization As Antiproliferative Agents

被引：102

作者：

Chen, Jianjun ^{[1
]}

Ahn, Sunjoo ^{[2
]}

Wang, Jin ^{[1
]}

Lu, Yan ^{[1
]}

Dalton, James T. ^{[2
]}

Miller, Duane D. ^{[1
,2
]}

Li, Wei ^{[1
]}

机构：

[1] Univ Tennessee, Ctr Hlth Sci, Dept Pharmaceut Sci, Coll Pharm, Memphis, TN 38163 USA

[2] GTx Inc, Memphis, TN 38163 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 55卷 / 16期

关键词：

ANTICANCER AGENTS; MULTIDRUG-RESISTANCE; DRUG-RESISTANCE; BINDING AGENTS; IN-VIVO; CANCER; POTENT; MECHANISMS; INHIBITORS; INDIBULIN;

D O I：

10.1021/jm300564b

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel ABI-III compounds were designed and synthesized based on our previously reported ABI-I and ABI-II analogues. ABI-III compounds are highly potent against a panel of melanoma and prostate cancer cell lines, with the best compound having an average IC50 value of 3.8 nM. They are not substrate of Pgp and thus may effectively overcome Pgp-mediated multidrug resistance. ABI-III analogues maintain their mechanisms of action by inhibition of tubulin polymerization.

引用

页码：7285 / 7289

页数：5

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