Drug Discov Ther. 2012;6(3):133-139. (DOI: 10.5582/ddt.2012.v6.3.133)

Synthesis and anticancer activity of novel 5-(indole-2-yl)-3-substituted 1,2,4-oxadiazoles.

Wang P, Liu JZ, Xing HL, Liu Y, Xie WC, Zhao GS


A new series of 5-(indole-2-yl)-3-substituted 1,2,4-oxadiazoles were synthesized and evaluated for their anticancer activities. Structures of the compounds were confirmed by spectroscopic methods. Structural modifications were done to improve the antiproliferative activity of compound 1. The results indicated that a benzyloxyl substituent on the C-4 position was better than a methyl substituent on the C-6 position of the indole component. Compounds 10a, 10b, 10g, 10i, 10l, 10n, 10o, and 10p were found to be more active than lead compound 1 in the PC-3 cell line. These compounds may serve as lead candidates in the development of novel chemotherapeutics for cancer treatment.

KEYWORDS: Indole, 1,2,4-oxadiazole, anticancer

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