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Synthesis and Cytotoxicity Evaluation of Novel Asymmetrical Mono-Carbonyl Analogs of Curcumin (AMACs) against Vero, HeLa, and MCF7 Cell Lines

机译:姜黄素(AMACs)新的姜黄素,Hela和MCF7细胞系的新型不对称单羰基类似物的合成与细胞毒性评价

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摘要

A series of novel asymmetrical mono-carbonyl analogs of curcumin (AMACs) were synthesized and evaluated for cytotoxic activity using BSLT and MTT assay against Vero, HeLa, and MCF7 cell lines. The structures of the synthesized compounds were confirmed by FTIR, 1H-NMR, 13C-NMR, and mass spectral data. The results of the cytotoxicity evaluation showed that the synthesized compounds exhibited moderate to very high toxic activity in BSLT (LC50 value 29.80–1704.23 µM); most of the compound exhibited cytotoxic activity against HeLa cell lines, which is comparable to the activity of cisplatin (IC50 value 40.65–95.55 µM), and most of the compound tested against MCF7 cell lines exhibited moderate to very high cytotoxic activity (IC50 value 7.86–35.88 µM). However, the selectivity index (SI) of the compounds was low (<1–1.96). Among the synthesized compounds, compound 1b was the most cytotoxic and selective against MCF7 cell lines. It could be considered for further development to obtain the more active and selective chemotherapeutic agents against breast cancer.
机译:合成了姜黄素(AMACs)的一系列新的非对称单羰基类似物,并使用BSLT和MTT测定对Vero,Hela和MCF7细胞系评估细胞毒性活性。通过FTIR,1H-NMR,13C-NMR和质谱数据证实合成化合物的结构。细胞毒性评价的结果表明,合成化合物在BSLT中表现出中等至非常高的毒性活性(LC50值29.80-1704.23μm);大多数化合物表现出对HeLa细胞系的细胞毒性活性,其与顺铂的活性相当(IC50值40.65-95.55μm),并且对MCF7细胞系测试的大多数化合物表现出中等至非常高的细胞毒性活性(IC50值7.86 -35.88μm)。然而,化合物的选择性指数(Si)低(<1-1.96)。在合成化合物中,化合物1b是最多的细胞毒性和针对MCF7细胞系的选择性。可以考虑进一步发展以获得更活跃和选择性化学治疗剂免受乳腺癌。

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