Abstract Ten new pyridine linked various substituted thiazole hybrids through (hydrazonomethyl)phenoxy-acetamide spacer were synthesized. The synthetic strategy was based on the reaction of the precursor 2-(4-((2-carbamothioylhydrazono)methyl)phenoxy)-N-(pyridin-2-yl)acetamide (3) with various α-halogenated carbonyl compounds (namely; phenacyl bromides, ethyl bromoacetate, diethyl bromomalonate and 3-chloropentane-2,4-dione). Moreover, the cytotoxicity properties of the synthesized compounds have been studied against liver carcinoma (HepG2), laryngeal carcinoma (Hep-2), prostate cancer (PC3), breast cancer (MCF-7) and normal fibroblast cells (WI38). The pyridine-thiazole compounds 7 and 10 revealed promising anticancer activity against MCF-7 and HepG2 cell lines with IC50 values in the range 5.36-8.76 μM compared to the activity of 5-fluorouracil. Docking study provided valuable insights for binding sites of the synthesized compounds with Rho-associated protein kinase (ROCK-1).

中文翻译：

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新型官能化吡啶连接噻唑衍生物的合成和抗增殖活性研究

摘要 合成了十个通过（腙甲基）苯氧基-乙酰胺间隔基连接各种取代噻唑杂化物的新型吡啶。合成策略基于前体 2-(4-((2-carbamothioylhydrazono)methyl)phenoxy)-N-(pyridin-2-yl) 乙酰胺 (3) 与各种 α-卤代羰基化合物（即;苯甲酰溴、溴乙酸乙酯、溴丙二酸二乙酯和 3-氯戊烷-2,4-二酮）。此外，已研究合成化合物对肝癌 (HepG2)、喉癌 (Hep-2)、前列腺癌 (PC3)、乳腺癌 (MCF-7) 和正常成纤维细胞 (WI38) 的细胞毒性特性。吡啶-噻唑化合物 7 和 10 显示出对 MCF-7 和 HepG2 细胞系的有希望的抗癌活性，与 5-氟尿嘧啶的活性相比，IC50 值在 5.36-8.76 μM 范围内。