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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and anticancer activity of thiourea derivatives bearing a benzodioxole moiety with EGFR inhibitory activity, apoptosis assay and molecular docking study
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Synthesis and anticancer activity of thiourea derivatives bearing a benzodioxole moiety with EGFR inhibitory activity, apoptosis assay and molecular docking study

机译：含有EGFR抑制活性，凋亡测定和分子对接研究含有苯并二奇氧氧氧源性部分的硫脲衍生物的合成与抗癌活性及分子对接研究

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摘要

New thiourea derivatives bearing a benzodioxole moiety were synthesized via the reaction of 5-isothiocyanatobenzodioxole with amino compounds such as aromatic amines, sulfa drugs, heterocyclic amines, hydrazines and hydrazides. The anticancer activity of the synthesized thiourea derivatives was examined against HCT116, HepG2 and MCF-7 cancer cell lines. Most of thiourea derivatives revealed significant cytotoxic effect, in some cases greater than the doxorubicin. As example, IC50 values of N-1,N-3-disubstituted-thiosemicarbazone 7 were 1.11, 1.74 and 7.0 mu M for HCT116, HepG2 and MCF7, respectively; IC50 values of doxorubicin were 8.29, 7.46 and 4.56 mu M, respectively. The anticancer mechanisms were studied via EGFR inhibition and apoptosis assessments, as well as molecular docking. (C) 2020 Elsevier Masson SAS. All rights reserved.
机译：通过5-异硫氰酸二苯并二氧唑与氨基化合物如芳族胺，磺胺类药物，杂环胺，肼和酰肼来合成含有苯二氧辛杂辛杂唑部分的新硫脲衍生物。 检查合成的硫脲衍生物的抗癌活性针对HCT116，HepG2和MCF-7癌细胞系。 大多数硫脲衍生物揭示了显着的细胞毒性效应，在某些情况下大于多柔比星。 作为实施例，对于HCT116，HepG2和MCF7，N-1，N-3-二取代 - 硫代硫代苯滴虫的IC 50值分别为1.11,1.74和7.0μm; 多柔比蛋白的IC 50值分别为8.29,7.46和4.56 mu m。 通过EGFR抑制和细胞凋亡评估以及分子对接研究抗癌机制。 （c）2020 Elsevier Masson SAS。 版权所有。

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