887577-27-7Relevant academic research and scientific papers
Discovery of Novel Tricyclic Thiazepine Derivatives as Anti-Drug-Resistant Cancer Agents by Combining Diversity-Oriented Synthesis and Converging Screening Approach
Xiang, Jinbao,Zhang, Zhuoqi,Mu, Yan,Xu, Xianxiu,Guo, Sigen,Liu, Yongjin,Russo, Daniel P.,Zhu, Hao,Yan, Bing,Bai, Xu
, p. 230 - 235 (2016)
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 50 > 100 μM 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.
