Anti-proliferation evaluation of new derivatives of indole-6-carboxylate ester as receptor tyrosine kinase inhibitors.

IF 3.2 4区医学 Q3 CHEMISTRY, MEDICINAL Future medicinal chemistry Pub Date : 2024-07-02 Epub Date: 2024-05-10 DOI:10.1080/17568919.2024.2347084

Mustafa M Allawi, Ammar A Razzak Mahmood, Lubna H Tahtamouni, Abdulrahman M Saleh, Sana I Kanaan, Khaled M Saleh, Mai F AlSakhen, Nisreen Himsawi, Salem R Yasin

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引用次数: 0

Abstract

Aim: The main goal was to create two new groups of indole derivatives, hydrazine-1-carbothioamide (4a and 4b) and oxadiazole (5, and 6a-e) that target EGFR (4a, 4b, 5) or VEGFR-2 (6a-e). Materials & methods: The new derivatives were characterized using various spectroscopic techniques. Docking studies were used to investigate the binding patterns to EGFR/VEGFR-2, and the anti-proliferative properties were tested in vitro. Results: Compounds 4a (targeting EGFR) and 6c (targeting VEGFR-2) were the most effective cytotoxic agents, arresting cancer cells in the G2/M phase and inducing the extrinsic apoptosis pathway. Conclusion: The results of this study show that compounds 4a and 6c are promising cytotoxic compounds that inhibit the tyrosine kinase activity of EGFR and VEGFR-2, respectively.

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作为受体酪氨酸激酶抑制剂的吲哚-6-羧酸酯新衍生物的抗增殖评估。

目的：主要目标是创造两组新的吲哚衍生物，即针对表皮生长因子受体（EGFR）（4a、4b、5）或血管内皮生长因子受体-2（VEGFR-2）（6a-e）的肼-1-硫代甲酰胺（4a 和 4b）和噁二唑（5 和 6a-e）。材料与方法：使用各种光谱技术对新衍生物进行表征。利用对接研究调查了与表皮生长因子受体/血管内皮生长因子受体-2的结合模式，并在体外测试了其抗增殖特性。结果：化合物 4a（靶向表皮生长因子受体）和 6c（靶向血管内皮生长因子受体-2）是最有效的细胞毒剂，能使癌细胞停滞在 G2/M 期，并诱导细胞外凋亡途径。结论本研究结果表明，化合物 4a 和 6c 是很有前途的细胞毒性化合物，可分别抑制表皮生长因子受体和血管内皮生长因子受体-2 的酪氨酸激酶活性。

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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来源期刊

Future medicinal chemistry CHEMISTRY, MEDICINAL-

CiteScore

5.80

自引率

2.40%

发文量

118

审稿时长

4-8 weeks

期刊介绍： Future Medicinal Chemistry offers a forum for the rapid publication of original research and critical reviews of the latest milestones in the field. Strong emphasis is placed on ensuring that the journal stimulates awareness of issues that are anticipated to play an increasingly central role in influencing the future direction of pharmaceutical chemistry. Where relevant, contributions are also actively encouraged on areas as diverse as biotechnology, enzymology, green chemistry, genomics, immunology, materials science, neglected diseases and orphan drugs, pharmacogenomics, proteomics and toxicology.