Ontology highlight
ABSTRACT:
SUBMITTER: Xiang J
PROVIDER: S-EPMC5592639 | biostudies-literature | 2016 May
REPOSITORIES: biostudies-literature
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]