A series of sulphonyl acetamide analogues were generated on the quinazoline ring through a multistep reaction starting from 2-mercapto-3H-quinazolin-4-one. The library of synthesised analogues was screened for in vitro cytotoxic activity against various human cancer cell lines such as HCT-1 and HT-15 (colon), MCF-7(Breast), PC-3 (Prostrate), SF268 (CNS) using MTT method. From the bioassay results, it was observed that even though most of the synthesised derivatives exhibited a good potency against various screened cancer cell lines, but compound 10d, 10k, and 10n were found to show very potent anticancer activity on all tested cancer cell lines with compound 10d showing IC50 value of 0.08, 0.3 and 0.55 µM on HT-29, MCF-7 and PC-3 cell lines, respectively, compound 10k showing IC50 value of 0.12, 0.03 and 0.08 µM on HCT-15, HT-29 and PC-3 cell lines, respectively, and compound 10n showing IC50 values of 0.1, 0.34, 0.52 and 0.26 on HCT-15, HT-29, MCF-7 and PC-3 cell lines, respectively.
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Authors thank University of Pretoria for providing postdoctoral fellowship to JK. We also thank Department of Biotechnology, Govt. of India, New Delhi for Providing Energy Bioscience Overseas Fellowship to BAM.
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Khazir, J., Mir, B.A., Pandita, M. et al. Design and synthesis of sulphonyl acetamide analogues of quinazoline as anticancer agents. Med Chem Res 29, 916–925 (2020). https://doi.org/10.1007/s00044-020-02533-4