El-Serwy Walaa S, A Mohamed Neama, M M Kassem Emad, Mahmoud Khaled, Mounier M M
Therapeutical Chemistry Department, National Research Center, Dokki, Cairo, Egypt.
Department of Pharmacognosy, National Research Center, Cairo, Egypt.
Iran J Pharm Res. 2016 Winter;15(1):179-96.
Different acid chlorides (2a-d) reacted with anthranilic acid to produce 2-substituted-3, 1-benzoxazin-4-one (3a-d) which was used as starting material to synthesize some condensed and non-condensed heterocyclic compounds by reaction with nitrogen nucleophiles e.g., hydrazine hydrate, and formamide. Some of the newly synthesized analogues were chosen to evaluate their cytotoxic activity against human carcinoma cell lines (HePG2- MCF7- A549). The docking and the cytotoxic activity results revealed that nearly all of the compounds containing N-phenyl aniline showed significant inhibition for the three cell lines.
不同的酰氯(2a - d)与邻氨基苯甲酸反应生成2 - 取代 - 3,1 - 苯并恶嗪 - 4 - 酮(3a - d),该产物用作起始原料,通过与亲核氮试剂如水合肼和甲酰胺反应来合成一些稠合和非稠合的杂环化合物。选择一些新合成的类似物评估它们对人癌细胞系(HePG2 - MCF7 - A549)的细胞毒性活性。对接和细胞毒性活性结果表明,几乎所有含N - 苯基苯胺的化合物对这三种细胞系均表现出显著抑制作用。