喹啉和磺酰胺的分子杂化物:设计、合成和体外抗癌研究。

IF 2.5 4区 化学 Q2 CHEMISTRY, MULTIDISCIPLINARY
Padyala Panduranga, Parameshwar Makam, Naresh Kumar Katari, Rambabu Gundla, Sreekantha Babu Jonnalagadda, Bharat Kumar Tripuramallu
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引用次数: 0

摘要

设计出了多种官能化喹啉和磺酰胺的分子杂交体。合成过程采用了多步合成策略。针对各种癌细胞系,包括 HCT116、A549、U2OS、CCRF-CEM、Jurkat、MOLT-4、RAMOS 和 K562,对其抗癌特性进行了评估。非癌细胞株 MRC-5 和 BJ 也被纳入比较范围。在研究对 A549、HCT116 和 U2OS 细胞的影响时,所有测试化合物都表现出有限的效力,IC50 值超过 50 μM,表明对这些细胞株的活性很弱。对于高 ITK 细胞(即 Jurkat、CCRF-CEM 和 MOLT-4),9 e、9 p 和 9 j 是最强效的化合物,IC50 值分别为 7.43±7.40μM、13.19±1.25μM 和 5.57±7.56 μM。同样,在 BTK 高细胞筛选中,9 个 n 和 9 个 e 分子对 RAMOS 和 K562 的 IC50 值分别为 2.76±0.79 μM 和 5.47±1.71 μM,具有很高的效力。有趣的是,所有分子对非癌细胞(MRC-5 和 BJ)的 IC50 值均大于 50 μM,这表明这些分子具有良好的无毒性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Molecular Hybrids of Quinoline and Sulfonamide: Design, Synthesis and in Vitro Anticancer Studies

Molecular Hybrids of Quinoline and Sulfonamide: Design, Synthesis and in Vitro Anticancer Studies

Molecular hybrids of diversely functionalized quinoline and sulfonamide have been designed. Multistep synthetic strategies have been used for the synthesis. The anti-cancer properties have been evaluated against various cancer cell lines including HCT116, A549, U2OS, CCRF-CEM, Jurkat, MOLT-4, RAMOS, and K562. Non-cancer cell lines MRC-5 and BJ were also included for comparison. When examining the effects on A549, HCT116, and U2OS cells, all tested compounds exhibited limited potency with IC50 values exceeding 50 μM, indicating weak activity against these cell lines. Against the ITK high cells Viz. are Jurkat, CCRF-CEM and MOLT-4, 9 e, 9 p and 9 j found to the maximum potent compounds with IC50 values of 7.43±7.40 μM, 13.19±1.25 μM and 5.57±7.56 μM respectively. Similarly, in the BTK high cells screenings, 9 n and 9 e molecules with an IC50 value of 2.76±0.79 μM and 5.47±1.71 μM against RAMOS and K562 respectively are highly potent. Interestingly, all the molecules have exhibited IC50 value >50 μM against the non-cancer cells (MRC-5 and BJ), which indicates the promising non-cytotoxic nature of the molecules.

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来源期刊
ChemistryOpen
ChemistryOpen CHEMISTRY, MULTIDISCIPLINARY-
CiteScore
4.80
自引率
4.30%
发文量
143
审稿时长
1 months
期刊介绍: ChemistryOpen is a multidisciplinary, gold-road open-access, international forum for the publication of outstanding Reviews, Full Papers, and Communications from all areas of chemistry and related fields. It is co-owned by 16 continental European Chemical Societies, who have banded together in the alliance called ChemPubSoc Europe for the purpose of publishing high-quality journals in the field of chemistry and its border disciplines. As some of the governments of the countries represented in ChemPubSoc Europe have strongly recommended that the research conducted with their funding is freely accessible for all readers (Open Access), ChemPubSoc Europe was concerned that no journal for which the ethical standards were monitored by a chemical society was available for such papers. ChemistryOpen fills this gap.
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