N-亚硝基-3-（取代苯基亚氨基）-吲哚-2-酮衍生物的致癌作用
Carcinogenic effects of N-nitroso-3-(substituted phenylimino)-indolin-2-one derivatives.
作者信息
Kumarasamy Murali, Theivendren Panneerselvam, Govindarajan Rousso, Franzblau Scott G, Ramalingam Kirthiga
机构信息
Department of Chemical Engineering, University of Rovira i Virgili, 26, Av. Paisos Catalans, Tarragona, Spain.
出版信息
J Pharm Bioallied Sci. 2012 Jul;4(3):207-11. doi: 10.4103/0975-7406.99035.
AIM
A novel series of N-nitroso-3-(substituted phenylimino)-indolin-2-one 3a-h was synthesized and tested for carcinogenic effects.
MATERIALS AND METHODS
The synthesized pyrazole derivatives' chemical structures were proved by means of their infra red (IR), proton nuclear magnetic resonance ((1)H-NMR), and mass,and confirmed by elemental analyses. The carcinogenic activity was assessed by 3-(4,5dimethyl thiazole-2yl)-2,5-diphenyltetrazoliumbromide (MTT) cell-viability assay.
RESULTS
The results show that most of the synthesized compounds exhibit significant carcinogenic activities. Among the synthesized compounds, N-nitroso-3-(2,4-dinitrophenylimino)-indolin-2-one 3h exhibited the most potent carcinogenic activity.
CONCLUSION
The structure-activity relationship (SAR) studies show that the nature as well as the position of the amine are important for deciding the activity profile of the indolin-2-one derivatives, which reiterates the need for further experimental investigations.
目的
合成了一系列新型的N-亚硝基-3-（取代苯基亚氨基）-吲哚啉-2-酮3a-h，并测试其致癌作用。
材料与方法
通过红外光谱（IR）、质子核磁共振（(1)H-NMR）和质谱对合成的吡唑衍生物的化学结构进行了验证，并通过元素分析加以确认。采用3-（4,5-二甲基噻唑-2-基）-2,5-二苯基四氮唑溴盐（MTT）细胞活力测定法评估致癌活性。
结果
结果表明，大多数合成化合物表现出显著的致癌活性。在合成化合物中，N-亚硝基-3-（2,4-二硝基苯基亚氨基）-吲哚啉-2-酮3h表现出最强的致癌活性。
结论
构效关系（SAR）研究表明，胺的性质和位置对于确定吲哚啉-2-酮衍生物的活性特征很重要，这再次强调了进一步进行实验研究的必要性。
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