Synthesis of N-[trisubstitutedphenyl]-4-methyl Aniline Derivatives as Novel Anti-Breast Cancer Agents

IF 1.7 3区化学 Q3 CHEMISTRY, ORGANIC

Current Organic Chemistry Pub Date : 2024-08-28 DOI:10.2174/0113852728321140240811170956

Fayez Althobaiti

引用次数: 0

Abstract

A series of N-(substituted)-4-methyl aniline derivatives (4a,b, 5a,b, 6, 7, 8, and 9) has been designed and synthesized, and their biological activities were also evaluated as potential anti-tumor and tubulin enzyme inhibitors. Among all compounds, compound (8) showed the most potent tubulin aromatase enzyme inhibitory activity in vitro with an IC50 of 157.3 pg/mL compared to the reference inhibitor Dox (IC50 = 227.4 pg/mL). A docking simulation was performed to insert compound (8) into the crystal structure of human aromatase at the active site to determine the probable binding model. Based on the previous results, compound (8) with potent inhibitory activity on tumor growth could be employed as a potential anticancer agent.

查看原文本刊更多论文

作为新型抗乳腺癌药物的 N-[三取代苯基]-4-甲基苯胺衍生物的合成

设计并合成了一系列 N-（取代）-4-甲基苯胺衍生物（4a,b、5a,b、6、7、8 和 9），并评估了它们作为潜在的抗肿瘤和管壁酶抑制剂的生物活性。在所有化合物中，化合物（8）在体外显示出最强的小管芳香化酶抑制活性，与参考抑制剂 Dox（IC50 = 227.4 pg/mL）相比，IC50 为 157.3 pg/mL。为了确定化合物（8）与人芳香化酶晶体结构活性位点的可能结合模型，对其进行了对接模拟。根据之前的研究结果，化合物（8）对肿瘤生长具有很强的抑制活性，可作为一种潜在的抗癌药物。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

求助全文

约1分钟内获得全文求助全文

来源期刊

Current Organic Chemistry 化学-有机化学

CiteScore

3.70

自引率

7.70%

发文量

审稿时长

1 months

期刊介绍： Current Organic Chemistry aims to provide in-depth/mini reviews on the current progress in various fields related to organic chemistry including bioorganic chemistry, organo-metallic chemistry, asymmetric synthesis, heterocyclic chemistry, natural product chemistry, catalytic and green chemistry, suitable aspects of medicinal chemistry and polymer chemistry, as well as analytical methods in organic chemistry. The frontier reviews provide the current state of knowledge in these fields and are written by chosen experts who are internationally known for their eminent research contributions. The Journal also accepts high quality research papers focusing on hot topics, highlights and letters besides thematic issues in these fields. Current Organic Chemistry should prove to be of great interest to organic chemists in academia and industry, who wish to keep abreast with recent developments in key fields of organic chemistry.