含有不同碱胺末端的喹唑啉衍生物的设计、合成及抗肿瘤活性评价

IF 2.6 4区医学 Q3 CHEMISTRY, MEDICINAL

Medicinal Chemistry Research Pub Date : 2024-11-04 DOI:10.1007/s00044-024-03320-1

Shihao Wang, Zichen Yang, Dongling Gu, JiaHui Han, Hongjing Chen, Hao Wang, JiaXin Zheng, Hongmin Liu, Yu Ke, Qiurong Zhang

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引用次数: 0

摘要

在本研究中，我们设计并合成了41种不同碱胺末端的喹唑啉衍生物。化合物15n对4种癌细胞（MGC-803、PC-3、A549和Eca-109）的抗增殖活性最好，IC50值为1.91 μM。在集落、划痕和凋亡实验中，化合物15n对A549细胞的增殖、迁移和凋亡均呈浓度依赖性，并将细胞周期阻断在G0/G1期。总之，我们的研究表明化合物15n具有开发抗肿瘤药物的先导化合物的潜力。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Design, synthesis, and evaluation of antitumor activity of quinazoline derivatives containing different terminal segments of basic amine groups

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Design, synthesis, and evaluation of antitumor activity of quinazoline derivatives containing different terminal segments of basic amine groups

In this study, we designed and synthesized 41 quinazoline derivatives with different base amine termini. Compound 15n showed the best antiproliferation activity against A549 cells with IC₅₀ value of 1.91 μM in four cancer cell lines (MGC-803, PC-3, A549, and Eca-109). In colony, scratch, and apoptosis experiments, compound 15n inhibited proliferation, migration, and apoptosis of A549 cells in a concentration-dependent manner and blocked the cell cycle in the G0/G1 phase. Overall, our study suggests that compound 15n has potential as a lead compound for the development of antitumor drugs.

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来源期刊

Medicinal Chemistry Research 医学-医药化学

CiteScore

4.70

自引率

3.80%

发文量

162

审稿时长

5.0 months

期刊介绍： Medicinal Chemistry Research (MCRE) publishes papers on a wide range of topics, favoring research with significant, new, and up-to-date information. Although the journal has a demanding peer review process, MCRE still boasts rapid publication, due in part, to the length of the submissions. The journal publishes significant research on various topics, many of which emphasize the structure-activity relationships of molecular biology.