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.

中文翻译：

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喹唑啉磺酰乙酰胺类似物作为抗癌剂的设计与合成

通过2-巯基-3H-喹唑啉-4-酮的多步反应，在喹唑啉环上生成了一系列磺酰基乙酰胺类似物。使用以下方法筛选合成的类似物文库对各种人类癌细胞系（例如HCT-1和HT-15（结肠），MCF-7（乳腺癌），PC-3（Prostrate），SF268（CNS））的体外细胞毒活性MTT方法。从生物测定结果中观察到，即使大多数合成的衍生物对各种筛选的癌细胞系均显示出良好的效力，但发现化合物10d，10k和10n对所有测试的癌细胞系均显示出非常强的抗癌活性。化合物10d显示IC ₅₀在HT-29，MCF-7和PC-3细胞系上分别为0.08、0.3和0.55 µM，化合物10k在HCT-15，HT-29和PC-3上的IC ₅₀值分别为0.12、0.03和0.08 µM分别在HCT-15，HT-29，MCF-7和PC-3细胞株上显示的IC ₅₀值为0.1、0.34、0.52和0.26的化合物10n和化合物10n。