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新的1,3,4-thiadiazoles作为潜在的抗癌药物:亲细胞亡,细胞循环停止,分子建模和ADMET配置文件

Mohamed H Hekal¹, Paula S Farag¹, Magdy M Hemdan¹

¹Department of Chemistry, Faculty of Science, Ain Shams University Abbassia 11566 Cairo Egypt.

|May 30, 2023

概括

新的1,3,4-thiadiazole衍生物被合成并对抗癌性质进行评估. 化合物6b和19显示出显著的抗增殖活性和选择性,而化合物19显示出作为CDK1抑制剂的潜力.

科学领域:

药用化学医学化学
有机合成有机合成
药理学药理学是指药理学的学科.

背景情况:

1,3,4-thiadiazole支架被认为具有多种生物活动.
开发具有提高疗效和选择性的新型抗癌药物仍然是一个关键的研究领域.

研究的目的:

为了合成和表征新的1,3,4-thiadiazole衍生物.
评估它们对癌细胞的抗增殖活性.
调查它们的作用机制和药物相似性.

主要方法:

通过N-(5-(2-cyanoacetamido)-1,3,4-thiadiazol-2-yl) benzamide与碳电友的反应合成1,3,4-thiadiazole衍生物.
使用光谱和元素分析进行结构阐明.
抗增殖活性评估 (IC50),细胞毒性,细胞周期分析 (Annexin V-PI测定),分子对接,以及利宾斯基五项规则分析.

主要成果:

二十四种新的1,3,4-thiadiazoles被合成.
衍生物6b和19表现出强烈的抗增殖活性 (IC50<10μM) 和对MCF-7乳腺癌细胞的高选择性.
化合物19诱导G2/M细胞循环停止,可能通过CDK1抑制,并显示有利的结合CDK1口袋.
化合物6b诱导了亡和增加了亚G1细胞群.

结论:

化合物6b和19是具有独特作用机制的有前途的抗癌药物.
化合物19是一种潜在的CDK1抑制剂.
这两种化合物都遵循利宾斯基的五项规则,并表现出有利的in silico ADME特性,需要进一步调查.

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