Synthesis, Characterization and Preliminary Screening of New N-Substi-tuted -8-Methyl-4-Hydroxy-2-Quinolone -3-Carboxamides as Potential An-ticancer Agents

IF 1.7 4区化学 Q3 CHEMISTRY, ORGANIC Current organic synthesis Pub Date : 2024-04-19 DOI:10.2174/0115701794291133240327044308

Dania Altaher, Hiba Zalloum, Kamal Sweidan, Dima A. Sabbah, Husam AlSalamat, Mahmoud Sunjuk, Reem Isleem

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Abstract

Introduction: A new series of 4-hydroxy-8-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide derivatives has been synthesized in good yields, followed by complete characteri-zation using 1D-NMR, 2D-NMR, and IR techniques. Methods:: The final products contain amide, hydroxyl, and aromatic functional groups that usu-ally show significant bioactivity. The target products have been examined towards three cancer cell lines, namely colorectal cancer cell line (HCT116), breast cancer cell line (MCF-7), and leukemia cell line (K562) in addition to the fibroblast cells, that were used as a model for normal human tissue. Results:: The anticancer results signified that compound 6 showed the most activity in the series accomplished with IC50 values of 14.6, 5.3 and 12.8 μM, Conclusion:: Other compounds exhibited considerable activity, such as compounds 9 (IC50 3.5 and 19.0 μM), 10 (IC50 12.6 μM), and 11 (IC50 10.3 μM) against the three cancer cell lines HCT116, MCF-7 and K562, respectively.

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作为潜在抗癌剂的新型 N-取代基-8-甲基-4-羟基-2-喹啉酮-3-羧酰胺的合成、表征和初步筛选

简介：以良好的产率合成了一系列新的 4-羟基-8-甲基-2-氧代-1,2-二氢喹啉-3-甲酰胺衍生物，随后使用一维-核磁共振、二维-核磁共振和红外技术进行了完整的表征。方法：：最终产物含有酰胺、羟基和芳香官能团，通常具有显著的生物活性。除了用作正常人体组织模型的成纤维细胞外，还对三种癌细胞系，即结直肠癌细胞系（HCT116）、乳腺癌细胞系（MCF-7）和白血病细胞系（K562）进行了目标产物检测。结果抗癌结果表明，化合物 6 在完成的系列研究中表现出最强的活性，其 IC50 值分别为 14.6、5.3 和 12.8 μM：其他化合物也表现出相当高的活性，如化合物 9（IC50 值为 3.5 和 19.0 μM）、10（IC50 值为 12.6 μM）和 11（IC50 值为 10.3 μM），它们分别对三种癌细胞系 HCT116、MCF-7 和 K562 具有抗癌活性。

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来源期刊

Current organic synthesis 化学-有机化学

CiteScore

3.40

自引率

5.60%

发文量

审稿时长

6-12 weeks

期刊介绍： Current Organic Synthesis publishes in-depth reviews, original research articles and letter/short communications on all areas of synthetic organic chemistry i.e. asymmetric synthesis, organometallic chemistry, novel synthetic approaches to complex organic molecules, carbohydrates, polymers, protein chemistry, DNA chemistry, supramolecular chemistry, molecular recognition and new synthetic methods in organic chemistry. The frontier reviews provide the current state of knowledge in these fields and are written by experts who are internationally known for their eminent research contributions. The journal is essential reading to all synthetic organic chemists. Current Organic Synthesis should prove to be of great interest to synthetic chemists in academia and industry who wish to keep abreast with recent developments in key fields of organic synthesis.