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含有阿里里丁基基因的印丁-2-的双重活性:DNA和BSA相互作用

Syed Nasir Abbas Bukhari¹, Tariq G Alsahli², Hasan Ejaz³

¹Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf University Sakaka Al Jouf 72388 Saudi Arabia sbukhari@ju.edu.sa.

|September 27, 2023

概括

新的印-2- (IND) 被合成并测试其生物活性. 化合物4d表现出双重抗微生物和抗癌特性,表明其在药物发现方面的潜力.

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:

印度-2- (IND) 是一种具有多种生物活性的异环化合物.
阿里利丁基因图案经常被纳入候选药物中,以调节它们的特性.

研究的目的:

为了合成新型的带有阿里利丁部分的印丁-2- (IND).
评估合成的化合物对抗微生物和细胞毒性活动的评估.
研究有前途的化合物与DNA和牛血清白蛋白 (BSA) 的相互作用.

主要方法:

新型印度-2-一衍生物的多步合成.
针对细菌 (如B. cereus) 和真菌的抗微生物测试.
使用MCF-7癌细胞系进行细胞毒性测定.
谱学研究以确定DNA和BSA的结合亲缘关系.

主要成果:

合成的印度-2-具有不同程度的抗微生物和抗真菌活性.
化合物4h对B. cereus有很好的活性.
化合物4d和4g表现出强大的抗真菌活性和对MCF-7细胞有前途的抗癌作用.
化合物4d表现出适度的DNA结合和强大的结合亲和力与BSA.

结论:

具有m-aminobenzylidene片段的indolin-2-one衍生物4d具有显著的双重生物活性.
化合物4d是进一步研究传染病和癌症治疗药物发现的有希望的候选物.

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