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Green synthesis of α-aminophosphonate derivatives on a solid supported TiO2-SiO2 catalyst and their anticancer activity

机译:固体负载的TiO2-SiO2催化剂上绿色合成α-氨基膦酸酯衍生物及其抗癌活性

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摘要

Syntheses of a new series of biologically potent α-aminophosphonates were accomplished by one-pot Kabachnik-Fields reaction using TiO 2-SiO2 as solid supported catalyst under microwave irradiation conditions. The chemical structures of all the newly synthesized compounds were confirmed by analytical and spectral (IR, 1H, 13C, 31P NMR, and mass) data. Their anticancer nature was evaluated by screening the in vitro activity on two human cancer cell lines, HeLa and SK-BR-3. Compounds 4i and 4o showed the best activity on these cancer cells even though the majority of the compounds, and particularly 4l and 4p, have good cytotoxic activity against them. TiO2-SiO2 was employed as solid supported catalyst for the solvent-free one-pot synthesis of α-aminophosphonates by Kabachnik-Fields reaction under microwave irradiation conditions. The newly synthesized compounds were assessed for in vitro anticancer activity against HeLa and SK-BR-3 cells. The majority of the compounds showed good cytotoxic activity.
机译:通过一锅式Kabachnik-Fields反应,使用TiO 2-SiO2作为固体负载催化剂,在微波辐射条件下,完成了一系列新的具有生物活性的强力α-氨基膦酸酯的合成。通过分析和光谱(IR,1H,13C,31P NMR和质量)数据确认了所有新合成化合物的化学结构。通过筛选两种人类癌细胞系HeLa和SK-BR-3的体外活性,评估了它们的抗癌性质。化合物4i和4o对这些癌细胞显示出最佳活性,尽管大多数化合物,尤其是4l和4p对它们具有良好的细胞毒活性。 TiO2-SiO2用作固体载体催化剂,在微波辐射条件下通过Kabachnik-Fields反应无溶剂一锅合成α-氨基膦酸酯。评估了新合成的化合物对HeLa和SK-BR-3细胞的体外抗癌活性。大多数化合物显示出良好的细胞毒性活性。

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