Abstract
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 µM, 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 μM 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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Acknowledgements
V.S.D. is very grateful to the Council of Scientific and Industrial Research (CSIR), New Delhi, India, for providing Senior Research Fellowship and Sophisticated Analytical Instrumentation Facility (SAIF), Panjab University, Chandigarh for providing spectral data. We are grateful to Head, Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad, Maharashtra, for providing laboratory facility. We are grateful to Dean, School of Life Sciences, University of Hyderabad, for providing the FACS facility.
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Dofe, V.S., Sarkate, A.P., Azad, R. et al. Novel quinoline-based oxadiazole derivatives induce G2/M arrest and apoptosis in human breast cancer MCF-7 cell line. Res Chem Intermed 43, 7331–7345 (2017). https://doi.org/10.1007/s11164-017-3078-1
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DOI: https://doi.org/10.1007/s11164-017-3078-1