Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India.
J Enzyme Inhib Med Chem. 2011 Aug;26(4):472-9. doi: 10.3109/14756366.2010.528414. Epub 2010 Nov 5.
A new series of pyrazolo[3,4-d]pyrimidine-6-one derivatives (2a-2j) were prepared by using the Biginelli multicomponent cyclocondensation of 3-methyl-1-phenyl-1H-pyrazol-5(4H)-one (1a), different aromatic aldehydes, and urea with a catalytic amount of HCl at reflux temperature. These compounds were characterized by IR, (1)H NMR, (13)C NMR, and Mass spectral data. In vitro antiamoebic activity was performed against HM1:IMSS strain of Entamoeba histolytica. The results showed that the compounds 2b, 2i, and 2j with IC(50) values of 0.37 µM, 0.04 µM, and 0.06 µM, respectively, exhibited better antiamoebic activity than the standard drug metronidazole (IC(50) = 1.33 µM). The toxicological studies of these compounds on human breast cancer MCF-7 cell line showed that the compounds 2b, 2i, and 2j exhibited >80% viability at the concentration range of 1.56-50 µM.
一系列新的吡唑并[3,4-d]嘧啶-6-酮衍生物（2a-2j）是通过使用 3-甲基-1-苯基-1H-吡唑-5(4H)-酮（1a）、不同的芳香醛和脲与催化量的 HCl 在回流温度下进行Biginelli 多组分环缩合反应制备的。这些化合物通过 IR、(1)H NMR、(13)C NMR 和质谱数据进行了表征。对 HM1:IMSS 株溶组织内阿米巴进行了体外抗阿米巴活性测定。结果表明，化合物 2b、2i 和 2j 的 IC(50)值分别为 0.37 µM、0.04 µM 和 0.06 µM，表现出比标准药物甲硝唑（IC(50) = 1.33 µM）更好的抗阿米巴活性。这些化合物对人乳腺癌 MCF-7 细胞系的毒理学研究表明，化合物 2b、2i 和 2j 在 1.56-50 µM 的浓度范围内表现出>80%的活力。
