Synthesis of unsymmetrical biphenyls as potent cytotoxic agents

…, KF Bastow, SL Morris-Natschke, KH Lee, L Xie

Index: Wu, Gang; Guo, Huan-Fang; Gao, Kun; Liu, Yi-Nan; Bastow, Kenneth F.; Morris-Natschke, Susan L.; Lee, Kuo-Hsiung; Xie, Lan Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 19 p. 5272 - 5276

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Citation Number: 22

Abstract

Twenty-six unsymmetrical biphenyls were synthesized and evaluated for cytotoxic activity against DU145, A549, KB and KB-Vin tumor cell lines. Three compounds 27, 35 and 40 showed very potent activity against the HTCL panel with an IC50 value range of 0.04–3.23 μM. In addition, fourteen active compounds were all more potent against the drug-resistant KB-Vin cell line than the parental KB cell line. Preliminary SAR analysis indicated that two ...