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含苯并二恶烷部分的具有 EGFR 抑制活性的硫脲衍生物的合成及抗癌活性，凋亡检测及分子对接研究。

Synthesis and anticancer activity of thiourea derivatives bearing a benzodioxole moiety with EGFR inhibitory activity, apoptosis assay and molecular docking study.

机构信息

Organometallic and Organometalloid Chemistry Department, National Research Centre, Cairo, Egypt.

Department of Chemistry, Faculty of Science, Taibah University, Almadinah Almunawarrah, Saudi Arabia.

出版信息

Eur J Med Chem. 2020 Jul 15;198:112363. doi: 10.1016/j.ejmech.2020.112363. Epub 2020 Apr 23.

DOI:10.1016/j.ejmech.2020.112363
PMID:32361329
Abstract

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, IC values of N,N-disubstituted-thiosemicarbazone 7 were 1.11, 1.74 and 7.0 μM for HCT116, HepG2 and MCF7, respectively; IC values of doxorubicin were 8.29, 7.46 and 4.56 μM, respectively. The anticancer mechanisms were studied via EGFR inhibition and apoptosis assessments, as well as molecular docking.

摘要

合成了一系列含有苯并二氧杂环结构的新型硫脲衍生物，其通过 5-异硫氰酸基苯并二氧杂环与芳胺、磺胺类药物、杂环胺、肼和酰肼等氨基化合物反应得到。对合成的硫脲衍生物进行了体外抗 HCT116、HepG2 和 MCF-7 癌细胞系的活性测试。大多数硫脲衍生物表现出显著的细胞毒性作用，在某些情况下比阿霉素更强。例如，N,N-二取代硫代缩氨基脲 7 对 HCT116、HepG2 和 MCF7 的 IC 值分别为 1.11、1.74 和 7.0 μM；阿霉素的 IC 值分别为 8.29、7.46 和 4.56 μM。通过 EGFR 抑制和细胞凋亡评估以及分子对接研究了抗癌机制。

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