巴比妥酸、硫代巴比妥酸、硫代氨基脲和2-苯基吲哚衍生物异烟肼的光化学合成及其抗癌活性。

Journal of Chemical Biology Pub Date : 2015-11-17 eCollection Date: 2016-04-01 DOI:10.1007/s12154-015-0148-y
S Vijaya Laxmi, G Rajitha, B Rajitha, Asha Jyothi Rao
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引用次数: 16

摘要

在光化学条件下合成了2-苯基- 1h -吲哚-3-乙醛基巴比妥酸、硫代巴比妥酸、硫代氨基脲、异烟肼和丙二腈衍生物。合成的化合物在3种不同的人类癌细胞系(前列腺癌细胞DU145、Dwivedi (DWD)癌细胞系和乳腺癌细胞系MCF7上进行了抗肿瘤活性评价。所有筛选的化合物均具有中等的抗癌活性,其中5-{1[2-(4-氯苯基)2-氧乙基]-2-苯基- 1h -吲哚-3-基亚甲基}-2-硫氧基-二氢嘧啶-4,6-二酮(2b)和5-{1[2-(4-甲氧基苯基)2-氧乙基]-2-苯基- 1h -吲哚-3-基亚甲基}-2-硫氧基-二氢嘧啶-4,6-二酮(2d)对使用的细胞株具有显著的抗肿瘤活性。此外,巴比妥酸衍生物对DWD细胞株和乳腺癌细胞株具有选择性抑制作用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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

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.

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Last issue of journal of chemical biology. JOCB Bulletin. Design, synthesis, and characterization of 2,2-bis(2,4-dinitrophenyl)-2-(phosphonatomethylamino)acetate as a herbicidal and biological active agent. Design and synthesis of an indol derivative as antibacterial agent against Staphylococcus aureus. Amphotericin B potentiates the anticancer activity of doxorubicin on the MCF-7 breast cancer cells.
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