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吲哚-6-羧酸酯类新型衍生物作为受体酪氨酸激酶抑制剂的抗增殖活性评价。

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

机构信息

Department of Pharmaceutical Chemistry, College of Pharmacy, Uruk university, Baghdad, Iraq.

Department of Pharmaceutical Chemistry, College of Pharmacy, University of Baghdad, Bab-Al-Mouadam, 10001, Baghdad, Iraq.

出版信息

Future Med Chem. 2024 Jul 2;16(13):1313-1331. doi: 10.1080/17568919.2024.2347084. Epub 2024 May 10.

DOI:10.1080/17568919.2024.2347084
PMID:39109434
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11318749/
Abstract

The main goal was to create two new groups of indole derivatives, hydrazine-1-carbothioamide ( and ) and oxadiazole (, and ) that target EGFR (, , ) or VEGFR-2 (). 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 . Compounds (targeting EGFR) and (targeting VEGFR-2) were the most effective cytotoxic agents, arresting cancer cells in the G2/M phase and inducing the extrinsic apoptosis pathway. The results of this study show that compounds and are promising cytotoxic compounds that inhibit the tyrosine kinase activity of EGFR and VEGFR-2, respectively.

摘要

主要目标是创建两个新的吲哚衍生物组,肼-1-碳硫酰胺(和)和恶二唑(,和),分别针对 EGFR(,,)或 VEGFR-2()。使用各种光谱技术对新衍生物进行了表征。对接研究用于研究与 EGFR/VEGFR-2 的结合模式,并测试了抗增殖特性。化合物(针对 EGFR)和(针对 VEGFR-2)是最有效的细胞毒性剂,将癌细胞阻滞在 G2/M 期并诱导细胞外凋亡途径。这项研究的结果表明,化合物和是有前途的细胞毒性化合物,分别抑制 EGFR 和 VEGFR-2 的酪氨酸激酶活性。