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Microwave-assisted synthesis and in vitro antiproliferative activity of some novel 1,2,3-triazole-based pyrazole aldehydes and their benzimidazole derivatives
Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2020-01-31 , DOI: 10.1007/s00044-020-02515-6
Dongamanti Ashok , M. Ram Reddy , Nalaparaju Nagaraju , Ravinder Dharavath , Katta Ramakrishna , Srinivas Gundu , P. Shravani , M. Sarasija

A series of new 3-(5-methyl-1-aryl-1H-1,2,3-triazol-4-yl)-1-phenyl-1H-pyrazole-4-carbaldehydes 4(a–g) and their benzimidazole derivatives 6(ag) were synthesized under both conventional and microwave irradiation methods. However, we successfully achieved good yields in shorter reaction times under microwave irradiation. All the synthesized scaffolds were characterized by 1H NMR, 13C NMR, IR and mass spectral analyses. The synthesized compounds have been evaluated as potential antiproliferative agents. The antiproliferative activity of the synthesized compounds was studied against two cancer cell lines C6 (nerve cells) and MCF-7 (human breast adenocarcinoma cells) and among them, compounds 4g and 6b exhibited highly potent activity against C6 cell line and 6b–c exhibited highly potent activity against MCF-7 cell line.

中文翻译:

新型1,2,3-三唑基吡唑醛及其苯并咪唑衍生物的微波辅助合成及体外抗增殖活性

一系列新的3-(5-甲基-1-芳基-1 H -1,2,3-三唑-4-基)-1-苯基-1 H-吡唑-4-甲醛4(a–g)和它们的苯并咪唑衍生物6ag)是在常规和微波辐射方法下合成的。但是,我们在较短的微波辐射反应时间内成功地获得了良好的收率。所有合成的支架均通过1 H NMR,1313 C NMR,IR和质谱分析。合成的化合物已被评估为潜在的抗增殖剂。合成的化合物的抗增殖活性进行了研究针对两种癌细胞系C6(神经细胞)和MCF-7(人乳腺癌细胞)和它们之间,化合物4克6B表现出对C6细胞系和高度有效的活性图6b-C显示出针对MCF-7细胞系的高效活性。
更新日期:2020-01-31
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