取代嘧啶的自由基清除和细胞毒活性

Qurat-ul-ain, S. Hussain, M. I. Coudhary, K. Khan
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引用次数: 1

摘要

合成了一个取代嘧啶文库,并对3T3细胞的自由基清除和体外细胞毒活性进行了评价。化合物的IC50值为42.9 + 0.31 ~ 438.3 3.3 {\mu}M,与标准丁基羟基甲苯的IC50值为128.83 2相比,具有良好的自由基清除能力。1}{\μM。并建立了结构-活性关系。选择1、2、3、5、6、7、8、9、10、12、13、15、19、20、21、24、25、26和28个类似物,采用MTT法对小鼠成纤维细胞3T3细胞株进行细胞毒性检测,结果表明,大部分类似物具有细胞毒性。本研究发现了一些具有自由基清除活性的细胞毒性新型取代嘧啶,可作为抑制由活性氧介导的癌细胞生长的化合物。
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Free Radical Scavenging and Cytotoxic Activities of Substituted Pyrimidines
A library of substituted pyrimidines was synthesized and evaluated for free radical scavenging, and in vitro cytotoxic activity in 3T3 cells. All compounds showed good free radical scavenging activity with IC50 values in the range of 42.9 + 0.31 to 438.3 3.3 {\mu}M as compared to the standard butylated hydroxytoluene having IC50 value of 128.83 2. 1 {\mu}M. The structure activity-relationship was also established. Selected analogues 1, 2, 3, 5, 6, 7, 8, 9, 10, 12, 13, 15, 19, 20, 21, 24, 25, 26 and 28 were tested for cytotoxicity in mouse fibroblast 3T3 cell line using MTT assay, and most of the analogues showed cytotoxicity. This study has identified a number of cytotoxic novel substituted pyrimidines having free radical scavenging activities that can be used as inhibitory compounds for those cancer cells whose growth is mediated by reactive oxygen species.
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