Benzothiazoles exhibit broad-spectrum antitumor activity: Their potency, structure-activity and structure-metabolism relationships

被引：41

作者：

Xie, Xilei ^{[1
,2
]}

Yan, Yu ^{[1
,2
]}

Zhu, Ning ^{[1
,2
]}

Liu, Gang ^{[1
,2
,3
,4
]}

机构：

[1] Chinese Acad Med Sci, Inst Mat Med, Beijing 100050, Peoples R China

[2] Peking Union Med Coll, Beijing 100050, Peoples R China

[3] Tsinghua Univ, Sch Med, Tsinghua Peking Ctr Life Sci, Beijing 100084, Peoples R China

[4] Tsinghua Univ, Sch Med, Dept Pharmacol & Pharmaceut Sci, Beijing 100084, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 76卷

基金：

中国国家自然科学基金;

关键词：

Benzothiazole; Antitumor activity; Structure-activity relationships; Structure-metabolism relationship; POTENTIAL ANTICANCER AGENTS; TUMOR-CELL LINES; BIOLOGICAL EVALUATION; IN-VITRO; ALZHEIMERS-DISEASE; INHIBITORS; DERIVATIVES; DESIGN; BENZIMIDAZOLE; DISCOVERY;

D O I：

10.1016/j.ejmech.2014.02.007

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

An antitumor activity oriented benzothiazole sublibrary was constructed from a hit compound 3 via a five stepwise procedure. All target compounds were screened for their antitumor activity against 60 human cancer cell lines. Compounds 9p, 12d and 12i, showing higher potency than hit 3, were identified. Particularly, the compound 9p gave its average 50% growth inhibition (GI(50)) at 0.38 mu M. Furthermore, incubation in human liver microsome primarily proved their metabolic stability in vitro. General structure-activity and structure-metabolism relationships were both summarized, which provides information on further strategically optimization. (C) 2014 Elsevier Masson SAS. All rights reserved.

引用

页码：67 / 78

页数：12

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