Synthesis, Characterization and In Vitro Antitumor Evaluation of New Pyrazolo[3,4-d]Pyrimidine Derivatives
Open Access
- 1 January 2017
- journal article
- research article
- Published by Scientific Research Publishing, Inc. in Open Journal of Medicinal Chemistry
- Vol. 07 (01), 1-17
- https://doi.org/10.4236/ojmc.2017.71001
Abstract
A new series of 3-(methylthio)-1-phenyl-1H-pyrazolo[3,4-d]pyrimidine derivatives was synthesized. The structures of the new derivatives were confirmed by the spectral data and elemental analyses. The antitumor activity of this series against human breast adenocarcinoma cell line MCF7 was evaluated. Out of twenty new derivatives, ten were revealed mild to moderate activity compared with doxorubicin as a reference antitumor. Among this new series N-(2-chlorophenyl)-2-(3-(methylthio)-4-oxo-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-5(4H)-yl)acetamide (13a) was found the most active one with IC50 equal to 23 μM.Keywords
This publication has 21 references indexed in Scilit:
- Synthesis of novel pyrazolo[3,4-d]pyrimidine derivatives as potential anti-breast cancer agentsEuropean Journal of Medicinal Chemistry, 2012
- Design, Synthesis, and Antitumor Evaluation of Novel Pyrazolo[3,4-d]pyrimidine DerivativesScientia Pharmaceutica, 2012
- Synthesis of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates and evaluation of their Src kinase inhibitory and anticancer activitiesBioorganic & Medicinal Chemistry Letters, 2011
- Synthesis and antitumor activity of novel 6-aryl and 6-alkylpyrazolo[3,4-d]pyrimidin-4-one derivativesEuropean Journal of Medicinal Chemistry, 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
- It Is Time to Include Cancer and Other Noncommunicable Diseases in the Millennium Development GoalsCA: A Cancer Journal for Clinicians, 2009
- Synthesis of pyrazolo[4,3-e][1,2,4]triazolo[4,3-c]pyrimidinesMonatshefte für Chemie / Chemical Monthly, 2008
- Novel 3-alkoxy-1H-pyrazolo[3,4-d]pyrimidines as EGFR and erbB2 receptor tyrosine kinase inhibitorsBioorganic & Medicinal Chemistry Letters, 2008
- 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