Abstract

A novel series of 4,5-dihydroisoxazole-5-carboxamide derivatives were designed, synthesized and evaluated for their anti-cancer activity against two different human cancer cell lines. Most of the synthesized compounds showed anti-cancer activity with IC₅₀ values ranging from 4.03 to 104.45 μM. Further, compounds 17h, 17i, 17e, and 18e were showed potent inhibitory activity against two cancer cell lines, with IC₅₀ values close to that of standard drug. It is important to note that compound 17h was more potent than the standard drug cisplatin with IC₅₀ values of 4.11 and 4.03 μM against Hela cell line and MCF-7 cell line respectively.

摘要

设计、合成了一系列新的 4,5-dihydroisoxazole-5-carboxamide 衍生物，并评估了它们对两种不同人类癌细胞系的抗癌活性。大多数合成的化合物显示出抗癌活性，IC ₅₀值范围为4.03至104.45 μM。此外，化合物17h、17i、17e和18e对两种癌细胞系均显示出有效的抑制活性，IC ₅₀值接近标准药物的IC ₅₀值。重要的是要注意，化合物17h比标准药物顺铂更有效，对 Hela 细胞系和 MCF-7 细胞系的IC ₅₀值分别为 4.11 和 4.03 μM。