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作为具有有前途的抗癌作用的强有力的可溶性环氧酶抑制剂的新型triazole-linked indole衍生物

Vijaykumar D Nimbarte^1,2, Shreya S Sonak¹, Sharda A Ishwarkar³

¹Department of Pharmacy, Birla Institute of Technology and Science (BITS) Pilani, Medchal, Telangana, India.

Chemical biology & drug design

|September 3, 2025

概括

通过抑制可溶性环氧化酶 (sEH),新型与三结合的醇衍生物具有强烈的抗癌活性. 化合物9a和9b具有高度有效性,对癌细胞具有显著的细胞毒性作用.

科学领域:

医学化学
药理学
癌症研究

背景情况:

可溶性环氧化酶 (sEH) 是包括癌症在内的各种疾病的潜在治疗点.
开发新的SEH抑制剂对于推进癌症治疗策略至关重要.

研究的目的:

设计,合成和评估与三醇结合的新型醇衍生物作为强大的可溶性环氧化酶抑制剂 (sEHI).
评估这些新型化合物的潜在抗癌活性.
阐明最有前途的候选人的作用机制和结构-活动关系 (SAR).

主要方法:

一系列与三结合的醇衍生物的化学合成.
在体外酶测试以确定sEH抑制活性 (IC50值).
对HeLa癌细胞的细胞毒性测定.
使用1ZD5晶体结构进行分子对接研究.
结构与活动关系 (SAR) 分析.

主要成果:

化合物9a和9b表现出强烈的SEH抑制,其IC50值分别为0. 270±0. 014nM和0. 358±0. 03nM.
这两种化合物对HeLa细胞具有显著的细胞毒性 (IC50值为5. 366 ± 0. 91μM和5. 686 ± 0. 73μM).
分子对接揭示了SEH活性部位内的关键相互作用,类似于AUDA等已知的抑制剂.

结论:

与醇结合的醇衍生物是可溶性环氧化酶的有效抑制剂.
这些化合物显示出有前途的抗癌潜力,需要进一步研究它们的治疗作用.
这些已识别的化合物作为开发新型针对SEH的抗癌药物的有价值的头候选物.

关键词:

抗癌药物化没有疼痛.可溶性环氧酶三醇

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