Design and synthesis of diarylamines and diarylethers as cytotoxic antitumor agents

…, PC Wu, MJ Hour, HY Hung, K Qian, R Huang…

Index: Wang, Xiao-Feng; Tian, Xing-Tao; Ohkoshi, Emika; Qin, Bingjie; Liu, Yi-Nan; Wu, Pei-Chi; Hour, Mann-Jen; Hung, Hsin-Yi; Qian, Keduo; Huang, Rong; Bastow, Kenneth F.; Janzen, William P.; Jin, Jian; Morris-Natschke, Susan L.; Lee, Kuo-Hsiung; Xie, Lan Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 19 p. 6224 - 6228

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Citation Number: 18

Abstract

Based on a shared structural core of diarylamine in several known anticancer drugs as well as a new cytotoxic hit 6-chloro-2-(4-cyanophenyl) amino-3-nitropyridine (7), 30 diarylamines and diarylethers were designed, synthesized, and evaluated for cytotoxic activity against A549, KB, KB-vin, and DU145 human tumor cell lines (HTCL). Four new leads 11e, 12, 13a, and 13b were discovered with GI50 values ranging from 0.33 to 3.45 μM. Preliminary SAR ...