设计和合成不对称苯并芘、喹喔啉类化合物，并评估其对人类非小肺癌细胞的抗癌活性。

IF 3.6 4区医学 Q2 CHEMISTRY, MEDICINAL

ChemMedChem Pub Date : 2024-11-26 DOI:10.1002/cmdc.202400847

Ping-Chih Hsu, Yu-Hsin Hsu, Chuan-Hsin Chang, Tzenge-Lien Shih

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引用次数: 0

摘要

喹喔啉及其衍生物具有广谱的生物活性，因此在各种治疗应用中具有重要价值。然而，由于喹喔啉类化合物在自然界中的稀缺性，大多数喹喔啉类化合物都是人工合成的。本文合成了一系列不对称的苯并芘，随后与 1,2-二氨基苯缩合生成了不对称的喹喔啉类化合物。研究人员评估了这些新合成的苯并吡啶和喹喔啉类化合物对携带不同基因突变的人类非小细胞肺癌（NSCLC）细胞的抗癌活性，以探索它们作为抗癌剂的潜力。在这些合成分子中，化合物 5g 的抑制作用与顺铂相当。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Design and Synthesis of Unsymmetric Benzils, Quinoxalines, and Evaluations of their Anticancer Activities against Human Non-Small Lung Cancer Cells.

Quinoxaline and its derivatives exhibit a broad spectrum of biological activity, making them valuable for various therapeutic applications. However, most quinoxalines are synthetically produced due to their scarcity in nature. In this article, a series of unsymmetric benzils were synthesized and subsequently condensed with 1,2-diaminobenzene to produce unsymmetric quinoxalines. The novel synthetic benzils and quinoxalines were evaluated for their anticancer activities against human non-small-cell lung cancer (NSCLC) cells harboring different gene mutations, to explore their potential as anticancer agents. Among these synthesized molecules, compound 5 g demonstrated inhibitory effects comparable to those of cisplatin.

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来源期刊

ChemMedChem 医学-药学

CiteScore

6.70

自引率

2.90%

发文量

280

审稿时长

1 months

期刊介绍： Quality research. Outstanding publications. With an impact factor of 3.124 (2019), ChemMedChem is a top journal for research at the interface of chemistry, biology and medicine. It is published on behalf of Chemistry Europe, an association of 16 European chemical societies. ChemMedChem publishes primary as well as critical secondary and tertiary information from authors across and for the world. Its mission is to integrate the wide and flourishing field of medicinal and pharmaceutical sciences, ranging from drug design and discovery to drug development and delivery, from molecular modeling to combinatorial chemistry, from target validation to lead generation and ADMET studies. ChemMedChem typically covers topics on small molecules, therapeutic macromolecules, peptides, peptidomimetics, and aptamers, protein-drug conjugates, nucleic acid therapies, and beginning 2017, nanomedicine, particularly 1) targeted nanodelivery, 2) theranostic nanoparticles, and 3) nanodrugs. Contents ChemMedChem publishes an attractive mixture of: Full Papers and Communications Reviews and Minireviews Patent Reviews Highlights and Concepts Book and Multimedia Reviews.