期刊
JOURNAL OF SAUDI CHEMICAL SOCIETY
卷 26, 期 4, 页码 -出版社
ELSEVIER
DOI: 10.1016/j.jscs.2022.101488
关键词
Anticancer; EGFR; ARO; Hydrazinyl-thiazole; Antibacterial; Cell cycle; Apoptosis
资金
- ASU
- AlMaarefa University
The synthesis and screening of a series of 5-hydrazinyl-2-(2-(1-(thien-2-yl)ethylidene)hydrazinyl)thiazole derivatives with dual anticancer and antimicrobial properties were conducted. The compounds showed promising in-vitro cytotoxic and enzyme inhibitory activity, as well as significant antimicrobial activity. Compounds 5h, 5j, and 5m demonstrated dual anticancer and antimicrobial effects, making them potential lead compounds for further modification and development of more potent and selective agents.
Increase in the number of infections caused by pathogenic microbes in cancer patients has prompted the searcher to invest in the development of agents having dual anticancer and antimicrobial properties. The present study is concerned with synthesis and screening for anticancer and antimicrobial activity of a series of 5-hydrazinyl-2-(2-(1-(thien-2-yl)ethylidene)hydrazinyl)thia zole derivatives. The structure elucidation of the synthesized hydrazinyl thiazole derivatives was illustrated by spectroscopic and elemental analysis. All the newly synthesized compounds 5a-p were evaluated for in-vitro cytotoxic activity against breast carcinoma (MCF-7 cell line), hepatocellular carcinoma (HePG-2) and colorectal cancer (HCT-116) cell lines using MTT assay method. Compounds 5 g, 5h showed broad spectrum activity against three cancer cell lines with IC50 ranged from 3.81 to 11.34 mM in compared to the reference drug Roscovitine (IC50 = 9.32 to 13.82 mM), while compounds 5 l and 5 m were found to be more selective against HePG-2 and HCT-116 cell line (IC50 = 9.29 and 8.93 mM respectively) and compound 5j was more selective against HePG-2 and MCF-7 cell lines (IC50 = 6.73 and 10.87 mM respectively). The inhibitory activity of the most promising compounds was tested against the EGFR and ARO enzymes and were further tested for apoptosis and Annexin V/PI staining. The results of enzyme-based tests revealed that the tested compound 5j has a dual inhibitory effect on the EGFR and ARO enzymes with IC50 = 82.8 and 98.6 nM respectively in compared to the reference drugs Erlotinib and Letrozole (IC50 = 62.4 and 79 nM respectively). Furthermore, the majority of the tested hydrazinyl thiazole derivatives exhibited significant antimicrobial activity against the used pathogenic microbes species. Compounds 4b, 5h, 5j and 5 m exerted a good antibacterial and antifungal activity against all tested pathogenic microbes. Therefore, it was concluded that compounds 5 h, 5j and 5 m proved to possess dual anticancer and antimicrobial agent and may serves as a useful lead compounds in search for further modification or derivatization to give more potent and selective agents. (c) 2022 The Authors. Published by Elsevier B.V. on behalf of King Saud University. This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/).
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据