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Synthesis and antitumor activity of tetrahydrocarbazole hybridized with dithioate derivatives

机译:四氢咔唑与二硫代酸酯衍生物的合成及其抗肿瘤活性

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The present study reported the synthesis of tetrahydrocarbazoles hybridized with dithioate derivatives. Three series were synthesized namely alkyl dithiocarbonates (4a–d), heterocyclic dithiocarbamates (6a–g) and dialkyl dithiocarbamate (7). The synthesized compounds were tested in vitro on human breast adenocarcinoma cell line (MCF7) and the human colon tumor cell line (HCT116). Most of the synthesized compounds exploited potent antitumor activity, especially compound 6f [4-chlorophenylpiperazine derivative], which showed cytotoxic activity against MCF7 superior to doxorubicin with IC50 value of 7.24?nM/mL.
机译:本研究报道了与二硫代酸酯衍生物杂交的四氢咔唑的合成。合成了三个系列,即烷基二硫代碳酸酯(4a–d),杂环二硫代氨基甲酸酯(6a–g)和二烷基二硫代氨基甲酸酯(7)。在人乳腺癌细胞系(MCF7)和结肠癌细胞系(HCT116)上对合成的化合物进行了体外测试。大多数合成的化合物都具有强大的抗肿瘤活性,尤其是化合物6f [4-氯苯基哌嗪衍生物],其对MCF7的细胞毒活性优于阿霉素,IC 50 值为7.24?nM / mL。

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