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1,3-Dipolar Cycloaddition Reactions for the Synthesis of Novel Oxindole Derivatives and Their Cytotoxic Properties
ACS Combinatorial Science ( IF 3.903 ) Pub Date : 2017-09-07 00:00:00 , DOI: 10.1021/acscombsci.7b00044
Prakash R. Mali 1, 2 , Prashishkumar K. Shirsat 1, 2 , Navnath Khomane 1, 2 , Lakshama Nayak 1 , Jagadeesh Babu Nanubolu 3 , H. M. Meshram 1
Affiliation  

The multicomponent reaction between isatin, amino acid, but-2-ynedioates, and phenacyl bromide has been developed using microwave irradiation under catalyst and base-free conditions in aqueous medium. This synthetic protocol is useful for the synthesis of various functionalized spirooxindole derivatives. This MCR exhibits a broad substrate scope with excellent yields and shorter reaction time. Additionally the synthesized spirooxindole derivatives were evaluated for their anticancer activity against three human cancer cell lines: MCF-7 (breast), A549 (lung), and HeLa cervical. Most of the compounds showed moderate to potent cytotoxic activity against the tested cell lines.

中文翻译:

1,3-偶极环加成反应合成新型羟吲哚衍生物及其细胞毒性

靛红,氨基酸,丁-2-炔基和苯甲酰溴之间的多组分反应已经在含水介质中在催化剂和无碱条件下使用微波辐射进行了开发。该合成方案可用于合成各种功能化的螺氧杂吲哚衍生物。该MCR显示出广泛的底物范围,具有优异的产率和较短的反应时间。另外,评估了合成的螺并吲哚衍生物对三种人类癌细胞系的抗癌活性:MCF-7(乳腺癌),A549(肺)和HeLa宫颈癌。大多数化合物对测试的细胞系显示出中度至强力的细胞毒活性。
更新日期:2017-09-07
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