Design and Efficient Synthesis of Novel 4,5-Dimethylthiazole-Hydrazone Derivatives and their Anticancer Activity,Letters in Drug Design & Discovery

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Design and Efficient Synthesis of Novel 4,5-Dimethylthiazole-Hydrazone Derivatives and their Anticancer Activity
Letters in Drug Design & Discovery ( IF 1.2 ) Pub Date : 2021-03-31 , DOI: 10.2174/1570180817999201022192937
Asaf Evrim Evren ₁ , Leyla Yurttaş ₂ , Büşra Ekselli ₃ , Mehmet Onur Aksoy ₃ , Gülşen Akalin-Çiftçi ₃

Affiliation

Background: Recently, researchers have been warning about the increased mortality of the various cancer types. Also, the lung adenocarcinoma and the glioma types are burning issues for world's health due to late or wrong diagnosis and/or insufficient treatment methods. For this purpose, our research group designed and synthesized novel 4,5-dimethyl thiazole-hydrazone derivatives which were tested against cancer and normal cell lines to understand the structureactivity relationship (SAR).

Methods: The lead compounds were obtained by reacting 2-(substituted aryl-2-ylmethylene) hydrazin-1-carbothioamide with 3-chloro-2-butanone derivatives. The structural elucidation of the compounds was performed by 1H-NMR, 13C-NMR, and LC/MS-IT-TOF spectral and elemental analyses. The synthesized compounds were tested in vitro for the anticancer activity against A549 human lung adenocarcinoma and C6 rat glioma cells and investigated for which pathway to induce cell death. Also, the docking study of the active compounds was achieved to understand the SAR.

中文翻译：

新型4,5-二甲基噻唑-zone衍生物的设计，合成及其抗癌活性

背景：最近，研究人员已警告各种癌症类型的死亡率增加。而且，由于晚期或错误的诊断和/或不足的治疗方法，肺腺癌和神经胶质瘤类型是世界健康的迫在眉睫的问题。为此，我们的研究小组设计并合成了新颖的4,5-二甲基噻唑-衍生物，并对其进行了抗癌和正常细胞株测试，以了解其结构活性关系（SAR）。

方法：通过使2-（取代的芳基-2-基亚甲基）肼-1-碳硫酰胺与3-氯-2-丁酮衍生物反应制得先导化合物。通过1 H-NMR，13 C-NMR和LC / MS-IT-TOF光谱和元素分析进行化合物的结构阐明。体外测试了合成的化合物对A549人肺腺癌和C6大鼠神经胶质瘤细胞的抗癌活性，并研究了诱导细胞死亡的途径。此外，完成了对活性化合物的对接研究，以了解SAR。

更新日期：2021-05-05

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