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作为抗癌药物的一些 3-取代-4-氧代-2-(1H)-噻唑烷-2-硫酮衍生物的细胞毒性筛选。

cytotoxicity screening of some 3-substituted-4-oxo-imidazolidin-2-(1H)-thione derivatives as anticancer drug.

机构信息

Department of Chemistry (The Division of Organic Chemistry), Faculty of Science, Port Said University, Port Said, Egypt.

Department of Chemistry, Faculty of Science, Suez Canal University, Ismailia, Egypt.

出版信息

Future Med Chem. 2024;16(14):1379-1393. doi: 10.1080/17568919.2024.2350925. Epub 2024 May 24.

Abstract

This study aimed to investigate the antitumor activity of new series of 2-thiohydanotin derivatives ( and ) against two cancer cell lines. A new series of 2-thioxoimidazolidine derivatives () were synthesized and investigated for its structure through spectral analysis and also tested against (HepG-2) and (HCT-116) cell line. Among the synthesized compounds, compound halted liver cancer cells at the G0/G1 phase and triggered apoptosis of liver cancer. Contrarily, compound caused colon cancer cells to be arrested at the S phase and trigger apoptosis. Also, they had a good inhibitory effect on (Nrf2). Both compounds had attractive lead molecules for the creation of colon and liver cancer medications.

摘要

本研究旨在探讨一系列新型 2-硫代海因衍生物(和)对两种癌细胞系的抗肿瘤活性。合成了一系列新的 2-硫代恶唑烷衍生物(),通过光谱分析对其结构进行了研究,并对(HepG-2)和(HCT-116)细胞系进行了测试。在所合成的化合物中,化合物使肝癌细胞停滞在 G0/G1 期,并引发肝癌细胞凋亡。相反,化合物使结肠癌细胞停滞在 S 期并引发细胞凋亡。此外,它们对(Nrf2)有很好的抑制作用。这两种化合物都是用于开发结肠癌和肝癌药物的有吸引力的先导分子。

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