Benzothiazoles exhibit broad-spectrum antitumor activity: their potency, structure-activity and structure-metabolism relationships.
Benzothiazoles exhibit broad-spectrum antitumor activity: their potency, structure-activity and structure-metabolism relationships.
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DOI：
10.1016/j.ejmech.2014.02.007
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发表时间：
2014-04
影响因子：
6.7
通讯作者：
Xilei Xie;Yu Yan;N. Zhu;Gang Liu
中科院分区：
文献类型：
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作者：
Xilei Xie;Yu Yan;N. Zhu;Gang Liu
An antitumor activity oriented benzothiazole sublibrary was constructed from a hit compound3via a five stepwise procedure. All target compounds were screened for their antitumor activity against 60 human cancer cell lines. Compounds9p,12dand12i, showing higher potency than hit3, were identified. Particularly, the compound9pgave its average 50% growth inhibition (GI50) at 0.38 μM. Furthermore, incubation in human liver microsome primarily proved their metabolic stabilityin vitro. General structure–activity and structure–metabolism relationships were both summarized, which provides information on further strategically optimization.
