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合成,抗癌活性和新型1,2,3-triazole链接甲基库衍生物的分子对接

Meitao Duan^1,2,3, Ahmed Mahal⁴, Anas Alkouri⁵

¹School of Pharmacy, Xiamen Medical College, Xiamen 361023, China.

Molecules (Basel, Switzerland)

|July 13, 2024

概括

合成和测试了13种新型四基库明衍生物的抗癌活性. 化合物4g对结肠癌细胞表现出强烈的细胞毒性作用,抑制细胞循环的进展,并为新的癌症药物开发提供了有希望的线索.

科学领域:

药用化学医学化学
有机合成有机合成
癌症研究癌症研究

背景情况:

癌症仍然是导致死亡的主要原因,需要开发新的治疗药物.
现有治疗方法面临挑战,推动对新药候选药物的研究.
氨酸库尔库明衍生物为抗癌药物发现提供了潜在的支架.

研究的目的:

为了合成新型的1,2,3-triazole相关的四水库衍生物.
评估这些化合物的体外抗癌活性与各种人类癌症细胞系相对应.
为了研究最强效化合物的作用机制.

主要方法:

通过点击反应合成13种与1,2,3-二醇相关的四水库衍生物.
通过MTT测定对HeLa,A549,HepG2和HCT-116细胞系进行体外抗癌活性评估.
使用NMR,HRMS和IR光谱学进行结构阐明;细胞周期分析;以及分子对接研究.

主要成果:

所有合成的化合物都进行了表征,并取得了良好的结果.
化合物4g和4k对测试的癌症细胞系表现出显著的细胞毒性活性.
化合物4g对HCT-116 (IC50 = 1.09 ± 0.17μM) 和A549 (IC50 = 45.16 ± 0.92μM) 细胞表现出强烈的活性,在G1阶段停止细胞周期,并可能抑制APC-Asef结合.

结论:

新型四水库衍生物成功合成和表征.
化合物4g显示出显著的抗癌潜力,特别是针对结肠癌.
化合物4g代表了一种有前途的化合物,用于开发新的抗癌疗法.

关键词:

这是一种抗癌药物.点击反应点击反应反应发现药物的发现.水库尔库四水库尔库.三醇三醇的使用方法

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