Synthesis and anticancer activity of novel 5-(indole-2-yl)-3-substituted 1,2,4-oxadiazoles.
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.
Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Ji'nan, Shandong, China.
Peng
P
Wang
Jianzhen
J
Liu
Hualu
H
Xing
Yang
Y
Liu
Wencheng
W
Xie
Guisen
G
Zhao
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D005260:Female; D006801:Humans; D008297:Male; D010069:Oxadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D010069:Oxadiazoles