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Synthesis of Derivatives of the 2-Arylquinoline Alkaloid Dubamine and their Cytotoxicity
Chemistry of Natural Compounds ( IF 0.8 ) Pub Date : 2020-05-01 , DOI: 10.1007/s10600-020-03074-3
A. R. Niyazmetov , E. O. Terent’eva , U. B. Khamidova , Z. S. Khashimova , Sh S. Azimova , V. I. Vinogradova

5′-Nitro- ( 2 ) and 5′-aminodubamine ( 3 ) were sequentially synthesized from the alkaloid dubamine. Condensation of 3 with 15 aldehydes gave imines, reduction of which produced secondary amines. Studies of the cytotoxicities for HeLa and HEp-2 cells of the compounds at a concentration of 100 μM revealed several trends. The activity decreased significantly or disappeared at lower concentrations although compound 5o at concentrations of 1–10 μM was active for HEp-2 cells at the level of cisplatin.

中文翻译:

2-芳基喹啉生物碱杜巴明衍生物的合成及其细胞毒性

5'-硝基-(2)和5'-氨基杜巴明(3)是由生物碱杜巴明依次合成的。3与15个醛缩合得到亚胺,其还原产生仲胺。对浓度为 100 μM 的化合物对 HeLa 和 HEp-2 细胞的细胞毒性研究揭示了几种趋势。尽管浓度为 1-10 μM 的化合物 5o 在顺铂水平下对 HEp-2 细胞有活性,但活性在较低浓度下显着降低或消失。
更新日期:2020-05-01
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