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Discovery of Novel Tricyclic Thiazepine Derivatives as Anti-Drug-Resistant Cancer Agents by Combining Diversity-Oriented Synthesis and Converging Screening Approach.


ABSTRACT: An efficient discovery strategy by combining diversity-oriented synthesis and converging cellular screening is described. By a three-round screening process, we identified novel tricyclic pyrido[2,3-b][1,4]benzothiazepines showing potent inhibitory activity against paclitaxel-resistant cell line H460TaxR (EC50 < 1.0 ?M), which exhibits much less toxicity toward normal cells (EC50 > 100 ?M against normal human fibroblasts). The most active hits also exhibited drug-like properties suitable for further preclinical research. This redeployment of antidepressing compounds for anticancer applications provides promising future prospects for treating drug-resistant tumors with fewer side effects.

SUBMITTER: Xiang J 

PROVIDER: S-EPMC5592639 | biostudies-literature | 2016 May

REPOSITORIES: biostudies-literature

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Discovery of Novel Tricyclic Thiazepine Derivatives as Anti-Drug-Resistant Cancer Agents by Combining Diversity-Oriented Synthesis and Converging Screening Approach.

Xiang Jinbao J   Zhang Zhuoqi Z   Mu Yan Y   Xu Xianxiu X   Guo Sigen S   Liu Yongjin Y   Russo Daniel P DP   Zhu Hao H   Yan Bing B   Bai Xu X  

ACS combinatorial science 20160415 5


An efficient discovery strategy by combining diversity-oriented synthesis and converging cellular screening is described. By a three-round screening process, we identified novel tricyclic pyrido[2,3-b][1,4]benzothiazepines showing potent inhibitory activity against paclitaxel-resistant cell line H460TaxR (EC50 < 1.0 μM), which exhibits much less toxicity toward normal cells (EC50 > 100 μM against normal human fibroblasts). The most active hits also exhibited drug-like properties suitable for fur  ...[more]

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