Novel 1, 3, 4-oxadiazole thioether derivatives targeting thymidylate synthase as dual anticancer/antimicrobial agents

…, J Sun, F Fang, WQ Zhong, HB Gong, HL Zhu

Index: Du, Qian-Ru; Li, Dong-Dong; Pi, Ya-Zhou; Li, Jing-Ran; Sun, Jian; Fang, Fei; Zhong, Wei-Qing; Gong, Hai-Bin; Zhu, Hai-Liang Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 8 p. 2286 - 2297

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Citation Number: 27

Abstract

A series of novel 1, 3, 4-oxadiazole thioether derivatives (compounds 9–44) were designed and synthesized as potential inhibitors of thymidylate synthase (TS) and as anticancer agents. The in vitro anticancer activities of these compounds were evaluated against three cancer cell lines by the MTT method. Among all the designed compounds, compound 18 bearing a nitro substituent exhibited more potent in vitro anticancer activities with IC50 ...