新型噻唑啉-四氢萘衍生物的合成及生物活性评价。

New Thiazoline-Tetralin Derivatives and Biological Activity Evaluation.

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskisehir, Turkey.

Department of Chemistry, Faculty of Sciences, Mentouri University, 25000 Constantin, Algeria.

出版信息

Molecules. 2018 Jan 10;23(1):135. doi: 10.3390/molecules23010135.

In this study, novel '-(3-cyclohexyl/phenyl-4-(substituted phenyl)thiazole-2(3)-ylidene)-2-[(5,6,7,8-tetrahydronaphthalen-2-yl)oxy]acetohydrazide (-) derivatives were synthesized and their anticancer potency were evaluated on human breast adenocarcinoma cell line (MCF-7), human lung carcinoma cell line (A549) and mouse embryoblast cell line (NIH/3T3) using the MTT method, DNA synthesis inhibition and flow cytometric analysis. Compound bearing 4-methoxyphenyl moiety exhibited the highest antitumor efficiency against MCF-7 cell line with higher DNA synthesis inhibition and apoptotic cell percentages (ealy+late apoptotic cell). On the other hand, compounds , , and bearing 4-bromo, 4-chloro and 4-florophenyl moieties, respectively caused excellent apoptosis levels against A549 cell line when treated with lower concentration even than cisplatin. Anticholinesterase activity of the compounds were also tested, compound showed 49.92% inhibition of acetylcholinesterase (AChE).

在这项研究中，我们合成了新型的‘-(3-环己基/苯基-4-(取代苯基)噻唑-2(3)-基)-2-[(5,6,7,8-四氢萘-2-基)氧基]乙酰胺(-)衍生物，并通过 MTT 法、DNA 合成抑制和流式细胞术分析，评估了它们对人乳腺癌腺癌细胞系 (MCF-7)、人肺癌细胞系 (A549) 和小鼠胚胎成纤维细胞系 (NIH/3T3) 的抗癌活性。带有 4-甲氧基苯基部分的化合物对 MCF-7 细胞系表现出最高的抗肿瘤效率，具有更高的 DNA 合成抑制和凋亡细胞百分比（早期+晚期凋亡细胞）。另一方面，带有 4-溴、4-氯和 4-氟苯基部分的化合物、和，在较低浓度下对 A549 细胞系产生了极好的凋亡水平，甚至比顺铂的效果还要好。我们还测试了这些化合物的乙酰胆碱酯酶抑制活性，结果表明化合物对乙酰胆碱酯酶 (AChE) 的抑制率为 49.92%。