Design, Synthesis, and Antitumor Evaluation of Novel Pyrazolo[3,4-d]pyrimidine Derivatives
Open Access
- 1 January 2012
- journal article
- Published by MDPI AG in Scientia Pharmaceutica
- Vol. 80 (3), 531-545
- https://doi.org/10.3797/scipharm.1204-23
Abstract
A new series of pyrazolo[3,4-d]pyrimidines has been synthesized. The new compounds were tested for their antitumor activity on 60 different cell lines, and some of the compounds were found to have potent antitumor activity. In particular, 2-hydroxybenzaldehyde [1-(4-chlorophenyl)-3-methyl-1H-pyrazolo-[3,4-d]pyrimidin-4-yl]hydrazone (VIIa) was found to be the most effective among the other derivatives, showing IC50 values of 0.326 to 4.31 μM on 57 different cell lines.This publication has 16 references indexed in Scilit:
- A Facile One-pot Synthesis of 1-Arylpyrazolo[3,4-d]Pyrimidin- 4-onesMolecules, 2010
- Pyrazolopyrimidines as highly potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): Optimization of the 1-substituentBioorganic & Medicinal Chemistry Letters, 2010
- Synthesis of some new pyrazolo[3,4-d]pyrimidine derivatives of expected anticancer and radioprotective activityEuropean Journal of Medicinal Chemistry, 2010
- Pyrazolo[3,4-d]pyrimidines as potent inhibitors of the insulin-like growth factor receptor (IGF-IR)Bioorganic & Medicinal Chemistry Letters, 2007
- 3D-QSAR and molecular docking studies on pyrazolopyrimidine derivatives as glycogen synthase kinase-3β inhibitorsJournal of Molecular Graphics and Modelling, 2007
- Synthesis and evaluation of novel heterocyclic inhibitors of GSK-3Bioorganic & Medicinal Chemistry Letters, 2006
- Synthesis and Biological Evaluation of 1-Aryl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-one Inhibitors of Cyclin-Dependent KinasesJournal of Medicinal Chemistry, 2004
- Novel pyrazolopyrimidine derivatives as GSK-3 inhibitorsBioorganic & Medicinal Chemistry Letters, 2004
- Synthesis and biological evaluations of pyrazolo[3,4-d]pyrimidines as cyclin-dependent kinase 2 inhibitorsEuropean Journal of Medicinal Chemistry, 2003
- New Colorimetric Cytotoxicity Assay for Anticancer-Drug ScreeningJNCI Journal of the National Cancer Institute, 1990