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Synthesis and Cytotoxic Evaluation of Novel Dimethyl [1,1′-Biphenyl]-2,2′-dicarboxylates Bearing 1,3,4-Thiadiazole Moieties

✍ Scribed by Xiang-Wen Kong; Yi-Hua Zhang; Tao Wang; Yi-Sheng Lai; Si-Xun Peng


Publisher
John Wiley and Sons
Year
2008
Tongue
English
Weight
193 KB
Volume
5
Category
Article
ISSN
1612-1872

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✦ Synopsis


Abstract

In search of novel anticancer agents, two series of dimethyl [1,1′‐biphenyl]‐2,2′‐dicarboxylate derivatives, 8a8k and 9a9k, containing both methylenedioxy and 1,3,4‐thiadiazole moieties were designed and synthesized. Cytotoxicity of these compounds was evaluated in vitro against five human tumor cell lines, i.e., HepG2, KB, A549, K562, and MCF‐7. The results indicated that 8h, 8j, 8k, 9d, 9g, 9h, 9j, and 9k showed notable anticancer activities comparable to or stronger than that of 5‐fluorouracil, a canonical anticancer drug. Structure–activity relationships were also discussed based on the experimental data obtained.


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