Synthesis and anticancer activities of thiosemicarbazones derivatives of thiochromanones and related scaffolds

被引：0
作者：
Jiangli Song
Rongkai Pan
Guobi Li
Wenyi Su
Xiumei Song
Jincheng Li
Shenggui Liu
机构：
[1] Lingnan Normal University,School of Chemistry & Chemical Engineering
[2] Key Laboratory of Clean Energy Materials Chemistry of Guangdong Higher Education Institute,Industrial Technology Research Institute
[3] Lingnan Normal University,undefined
来源：
Medicinal Chemistry Research | 2020年 / 29卷
关键词：
Thiosemicarbazone; Thiochromanone; Benzothiazepine; Cytotoxic activity; Apoptosis;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
A series of novel thiosemicarbazone analogs (4a–t, 6a–j) were synthesized and evaluated for their cytotoxic activities. The obtained results showed that thiochromanone-based thiosemicarbazones substituted primarily at the C-8 position exhibited higher cytotoxicity than the corresponding 1,1-dioxo-thiochromanone-, benzothiazepine-, and 1,1-dioxo-benzothiazepine-based analogs. Significantly, compound 4c (8-fluoro thiochromanone thiosemicarbazone) was found to be the most active and exhibited potent cytotoxicity against the MCF-7, SK-mel-2, and DU145 cancer cell lines, with IC50 values of 0.42, 0.58, and 0.43 µM, respectively. In addition, the mechanism of compound 4c induced MCF-7 cell apoptosis was preliminarily investigated through cell cycle, Annexin V-FITC/PI staining, and ROS assays, indicating that compound 4c may exert its anticancer property through ROS-mediated apoptosis.
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页码：630 / 642
页数：12
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