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设计,合成和抗瘤活动评价新型多洛特格拉维尔衍生物的设计,合成和抗瘤活动评价

Xi-Xi Hou¹, Long-Fei Mao², Yajie Guo³

¹Department of Pharmacy, The First Affiliated Hospital, and College of Clinical Medicine of Henan University of Science and Technology, Luoyang, China.

Frontiers in pharmacology

|August 23, 2023

概括

具有1,2,3-triazole部分的新型杜洛特格拉维尔衍生物对A549肺癌细胞表现出显著的抗癌活性. 化合物4b和4g有效地抑制了细胞生长,4g诱导了细胞亡,并激活了自和DNA损伤途径.

科学领域:

药用化学医学化学
有机合成有机合成
癌症生物学癌症生物学

背景情况:

多卢特格拉维尔是一种整合酶抑制剂,作为新型抗癌药物的结构基础.
1,2,3-二醇部分因其多样化的生物活性而得到认可.
肺腺癌 (A549细胞系) 仍然是癌症治疗的一个重大挑战.

研究的目的:

合成新型的杜洛特格拉维尔衍生物,其中包含1,2,3-三醇组.
为了评估这些衍生物对A549细胞的体外抗癌活性.
阐明潜在的强效化合物的活性背后的分子机制.

主要方法:

通过点击化学合成新型杜洛特格拉维尔衍生物.
在体外细胞毒性测定使用A549细胞系.
流细胞测量以评估亡诱导.
西方模糊分析LC3和γ-H2AX信号通路.

主要成果:

一系列新的杜洛特格拉维尔-1,2,3-三醇衍生物已经成功合成.
化合物4b和4g表现出A549细胞生长的强烈抑制,IC50值分别为8.72 ± 0.11 μM和12.97 ± 0.32 μM.
化合物4g在A549细胞中显著诱导了亡,克隆抑制,自 (LC3通路激活) 和DNA损伤 (γ-H2AX通路激活).

结论:

合成的杜洛特格拉维尔衍生物代表着有前途的抗癌药物.
化合物4g显示出作为肺癌治疗方法进一步发展的巨大潜力.
观察到的抗癌效应是通过亡,自和DNA损伤诱导进行的.

关键词:

一,二,三-三醇是一种造成的DNA损伤是DNA损伤.这是一种抗瘤药物.自自是自的过程.杜洛特格拉维尔 (Dolutegravir) 是一种严重的病毒.

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