Novel quinoline-based oxadiazole derivatives induce G2/M arrest and apoptosis in human breast cancer MCF-7 cell line

作者：Dofe Vidya S^*; Sarkate Aniket P; Azad Rajaram; Gill Charansingh H

来源：Research on Chemical Intermediates, 2017, 43(12): 7331-7345.

DOI：10.1007/s11164-017-3078-1

• Quinoline
• 1,3,4-Oxadiazole
• Anticancer activity
• Apoptosis

In the search for novel anticancer agents, we designed and synthesized a series of quinoline-based oxadiazole derivatives and assayed their in vitro cytotoxic efficacy against human breast cancer MCF-7 cell line. The most promising compounds in the present series (Q8, S3, S6) showed excellent activity and inhibited growth of breast cancer cell MCF-7 with 50% inhibitory concentration (IC50) of 8.31, 9.81, and 9.96 A mu M, respectively. The results of the present study reveal reduced IC50 values in a time- and dose-dependent mode with high specificity for MCF-7 (IC50 of 10 mu M at 24 h) versus normal breast cells. Apoptosis assay using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) also suggested that this compound induced cell death by apoptosis.
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• 出版日期2017-12