Bioorganic & Medicinal Chemistry Letters 2009-08-01

Synthesis and biological evaluation of amide derivatives of diflunisal as potential anti-tumor agents.

Guang-Xiang Zhong, Lu-Lu Chen, Hai-Bo Li, Fu-Jin Liu, Jin-Qing Hu, Wei-Xiao Hu

Index: Bioorg. Med. Chem. Lett. 19(15) , 4399-402, (2009)

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Abstract

To discover the new medicinal activity, the structure of diflunisal has been modified. Forty amide derivatives of diflunisal were synthesized starting from diflunisal in three steps. Their inhibition growth rate of human lung cancer cell (A549) and human endometrial adenocarcinoma cell (Ishikawa) in vitro was evaluated. The preliminary assay results showed that compounds 6j, 7o and 8c exhibited good anti-tumor activities and excellent selectivity for the Ishikawa cell, may be potential anti-tumor agents.