Synthesis and in vitro anticancer and antitubercular activity of diarylpyrazole ligated dihydropyrimidines possessing lipophilic carbamoyl group

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• 作者：Rama Krishna Yadlapalli^a ; O.P. Chourasia^a ; Kiranmayi Vemuri^b ; Manjula Sritharan^b ; Ramu Sridhar Perali^c ; ^{prssc@uohyd.ernet.in}
• 关键词：Dihydropyrimidines ; 1 ; 3-Diarylpyrazoles ; Multicomponent Reaction ; Anticancer ; Antitubercular
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 April, 2012
• 卷：22
• 期：8
• 页码：2708-2711
• 文件大小：574 K

摘要

A series of dihydropyrimidine derivatives were synthesized by utilizing Biginelli reaction and evaluated for their in vitro anticancer activity against MCF-7 human breast cancer (HBC) cell line using sulforhodamine B (SRB) assay and antitubercular activity against Mycobacterium tuberculosis (MTB) H₃₇Rv using Microplate Alamar Blue Assay (MABA). Compounds 13p, 13t were exhibited 70.6%and 63.7%of HBC cell growth inhibition at 10 渭M concentration. Interestingly compound 13p was also found to be the most potent in the series against MTB H₃₇Rv with MIC value of 0.125 渭g/mL.