新型噻唑杂环类化合物的合成及生物评价：潜在的抗癌和抗菌剂。
Synthesis and Biological Evaluation of Some Novel Thiazole-Based Heterocycles as Potential Anticancer and Antimicrobial Agents.
机构信息
Department of Chemistry, Faculty of Science, King Khalid University, Abha 61413, Saudi Arabia.
Department of Organic Chemistry, National Organization for Drug Control and Research (NODCAR), Giza 12311, Egypt.
出版信息
Molecules. 2019 Feb 1;24(3):539. doi: 10.3390/molecules24030539.
A novel series of thiazole-based heterocycles was synthesized using 1,3-dipolar cycloaddition reactions in the presence of chitosan-grafted-poly(vinylpyridine) as an eco-friendly biopolymeric basic catalyst. The molecular structure of the synthesized compounds was illustrated by spectroscopic and elemental analysis. Various in vitro biological assays were performed to explore the potential antitumor, antimicrobial and hepatoprotective activities of the newly synthesized compounds. The cytotoxic activities were assessed against human hepatocellular carcinoma (HepG-2), colorectal carcinoma (HCT-116) and breast cancer (MCF-7) cell lines and results revealed that all compounds displayed antitumor activities with the chlorine-containing derivatives, and , being the most potent. The majority of the tested thiazole derivatives exhibited satisfactory antibacterial activity towards the used gram positive and gram-negative bacterial species. Moreover, many derivatives showed weak hepatoprotective activity against CCl₄-induced hepatotoxicity.
使用壳聚糖接枝聚（4-乙烯吡啶）作为环保型生物高分子碱性催化剂，通过 1,3-偶极环加成反应合成了一系列新型噻唑杂环。通过光谱和元素分析说明了所合成化合物的分子结构。进行了各种体外生物测定，以研究新合成化合物的潜在抗肿瘤，抗菌和保肝活性。用噻唑衍生物对人肝癌（HepG-2），结肠直肠癌细胞（HCT-116）和乳腺癌（MCF-7）细胞系进行了细胞毒性评估，结果表明所有化合物均显示出抗肿瘤活性，含氯衍生物和显示出最强的活性。大多数测试的噻唑衍生物对所使用的革兰氏阳性和革兰氏阴性细菌物种具有令人满意的抗菌活性。此外，许多衍生物对 CCl₄诱导的肝毒性具有弱的保肝活性。
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