Design, Synthesis, and Biological Testing of Pyrazoline Derivatives of Combretastatin-A4: A Quest for Anticancer, Anti-Inflammatory, and Antioxidant Agents

IF 2.4 3区化学 Q2 CHEMISTRY, ORGANIC

Polycyclic Aromatic Compounds Pub Date : 2024-10-20 DOI:10.1080/10406638.2023.2271113

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引用次数: 0

Abstract

Three groups of novel analogs of combretastatin-A4 (CA-4), viz., the N¹-phenyl-pyrazoline (5a–e), N¹-alkyl acetylated pyrazoline (6a–c), and N¹-phenyl acetylated pyrazoline (7a–g) were designed, and synthesized in good yield. The structure of the compounds was confirmed by spectroscopic techniques. All the compounds were evaluated for their in vitro anticancer (MCF-7 cell line), antioxidant (DPPH, NO, SOR, and H₂O₂), and anti-inflammatory activity. Compounds 5d, 7g, 7f, 7e, 7c, 5b, 6a, 7b, and 7a showed excellent potency with GI₅₀ ranging from 0.1 to 10.9 µM against the MCF-7 cell line. Compounds 7f, 7g, 5c, 5d, 5b, 7e, and 6a exhibited good anti-inflammatory activity. Encouraged by these results, all the compounds were also tested for their antioxidant potency. Compounds 6a, 6c, 7b, 7c, 7f, and 7g were found to be excellent scavengers of all four free radicals (DPPH, NO, SOR, and H₂O₂).

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联合他汀-A4 的吡唑啉衍生物的设计、合成和生物测试：抗癌、抗炎和抗氧化剂的探索

研究人员设计了三组新的考布他丁-A4（CA-4）类似物，即N1-苯基吡唑啉（5a-e）、N1-烷基乙酰化吡唑啉（6a-c）和N1-苯基乙酰化吡唑啉（7a-g）。

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来源期刊

Polycyclic Aromatic Compounds 化学-有机化学

CiteScore

3.70

自引率

20.80%

发文量

412

审稿时长

3 months

期刊介绍： The purpose of Polycyclic Aromatic Compounds is to provide an international and interdisciplinary forum for all aspects of research related to polycyclic aromatic compounds (PAC). Topics range from fundamental research in chemistry (including synthetic and theoretical chemistry) and physics (including astrophysics), as well as thermodynamics, spectroscopy, analytical methods, and biology to applied studies in environmental science, biochemistry, toxicology, and industry. Polycyclic Aromatic Compounds has an outstanding Editorial Board and offers a rapid and efficient peer review process, as well as a flexible open access policy.