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Synthesis and Bioactivity of Thiosemicarbazones Containing Adamantane Skeletons

机译:含金刚烷骨架的硫代半氨基甲酮的合成及生物活性

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摘要

Reaction of 4-(1-adamantyl)-3-thiosemicarbazide ( ) with numerous substituted acetophenones and benzaldehydes yielded the corresponding thiosemicarbazones containing adamantane skeletons. The synthesized compounds were evaluated for their in vitro activities against some Gram-positive and Gram-negative bacteria, and the fungus , and cytotoxicity against four cancer cell lines (Hep3B, HeLa, A549, and MCF-7). All of them showed good antifungal activity against . Compounds , , , and , , displayed significant inhibitory activity against . Compounds , , , and had moderate inhibitory potency against . Compounds , and found so good inhibitory effect on . Compounds and , which contain ( ) hydroxyl groups on the phenyl ring, were shown to be good candidates as potential agents for killing the tested cancer cell lines, i.e., Hep3B, A549, and MCF-7. Compounds – , , , , , , and were moderate inhibitors against MCF-7.
机译:4-(1-金刚烷基)-3-硫代氨基脲()与大量取代的苯乙酮和苯甲醛的反应产生了相应的含金刚烷骨架的硫代半氨基甲酮。评估了合成的化合物对某些革兰氏阳性和革兰氏阴性细菌以及真菌的体外活性,以及​​对四种癌细胞系(Hep3B,HeLa,A549和MCF-7)的细胞毒性。它们均显示出良好的抗真菌活性。化合物,和和表现出显着的抑制作用。化合物,,和对乙肝有中等抑制作用。复方,并发现有很好的抑制作用。已显示在苯环上含有()羟基的化合物和可能是杀死被测癌细胞系(Hep3B,A549和MCF-7)的潜在药物的良好候选者。化合物–,,,,,和是对MCF-7的中度抑制剂。

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