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Photochemical synthesis and anticancer activity of barbituric acid thiobarbituric acid thiosemicarbazide and isoniazid linked to 2-phenyl indole derivatives

机译:与2-苯基吲哚衍生物连接的巴比妥酸硫代巴比妥酸硫代氨基脲和异烟肼的光化学合成和抗癌活性

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摘要

2-Phenyl-1H-indole-3-carbaldehyde-based barbituric acid, thiobarbituric acid, thiosemicarbazide, isoniazid, and malononitrile derivatives were synthesized under photochemical conditions. The antitumor activities of the synthesized compounds were evaluated on three different human cancer cell lines representing prostate cancer cell line DU145, Dwivedi (DWD) cancer cell lines, and breast cancer cell line MCF7. All the screened compounds possessed moderate anticancer activity, and out of all the screened compounds, 5-{1[2-(4-chloro-phenyl)2-oxo-ethyl]-2-phenyl-1H-indole-3-ylmethylene}-2-thioxo-dihydro-pyrimidine-4,6-dione (2b) and 5-{1[2-(4-methoxy-phenyl)2-oxo-ethyl]-2-phenyl-1H-indole-3-ylmethylene}-2-thioxo-dihydro-pyrimidine-4,6-dione (2d) exhibited marked antitumor activity against used cell lines. Additionally, barbituric acid derivatives were selective to inhibit cell line DWD and breast cancer cell lines.Electronic supplementary materialThe online version of this article (doi:10.1007/s12154-015-0148-y) contains supplementary material, which is available to authorized users.
机译:在光化学条件下合成了基于2-苯基-1H-吲哚-3-甲醛的巴比妥酸,硫代巴比妥酸,硫代氨基脲,异烟肼和丙二腈衍生物。在代表前列腺癌细胞系DU145,Dwivedi(DWD)癌细胞系和乳腺癌细胞系MCF7的三种不同的人类癌细胞系上评估了合成化合物的抗肿瘤活性。所有被筛选的化合物都具有中等的抗癌活性,在所有被筛选的化合物中,5- {1 [2-(4-氯-苯基)2-氧代乙基] -2-苯基-1H-吲哚-3-基亚甲基} -2-硫代-二氢-嘧啶-4,6-二酮(2b)和5- {1 [2-(4-甲氧基-苯基)2-氧代乙基] -2-苯基-1H-吲哚-3-基亚甲基} -2-硫代-二氢-嘧啶-4,6-二酮(2d)对使用的细胞系表现出显着的抗肿瘤活性。此外,巴比妥酸衍生物具有选择性抑制DWD细胞和乳腺癌细胞系的作用。电子补充材料本文的在线版本(doi:10.1007 / s12154-015-0148-y)包含补充材料,授权用户可以使用。

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