Design and synthesis of sulphonyl acetamide analogues of quinazoline as anticancer agents

AbstractA 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 compound10d, 10k, and10n were found to show very potent anticancer activity on all tested cancer cell lines with compound10d showing IC50 value of 0.08, 0.3 and 0.55  µM on HT-29, MCF-7 and PC-3 cell lines, respectively, compound10k showing IC50 value of 0.12, 0.03 and 0.08  µM on HCT-15, HT-29 and PC-3 cell lines, respectively, and compound10n 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.
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research