(3,5-Dimethylpyrazol-1-yl)-[4-(1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ylamino)phenyl]methanone

• Published in: MolBank Vol. 2016; no. 4; p. M915
• Main Authors: Bakr, Rania, Mehany, Ahmed
• Format: Journal Article
• Language: English
• Published: Basel MDPI AG 01-12-2016
• Subjects: Acetylacetone; anticancer; Apoptosis; Breast cancer; Chemistry; Colon; Cytotoxicity; Epidermal growth factor; Growth factors; Insulin; Kinases; Liver; Liver cancer; Pharmacy; protein kinases; Proteins; pyrazole; pyrazolo[3,4-d]pyrimidine; United States > US; Cairo Egypt; Egypt
• ISSN: 1422-8599; 1422-8599
• DOI: 10.3390/M915

In an attempt to enhance cytotoxic activity of pyrazolo[3,4-d]pyrimidine core, we synthesized (3,5-dimethylpyrazol-1-yl)-[4-(1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ylamino)phenyl]methanone (4) by reacting 4-(1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ylamino)benzohydrazide (3) with acetylacetone. Antiproliferative activity of this compound was screened against breast (MCF-7), colon (HCT-116), and liver (HEPG-2) cancer cell lines. The tested compound exhibited cytotoxic activity with IC50 = 5.00–32.52 μM. Moreover, inhibitory activity of this compound was evaluated against the epidermal growth factor receptor (EGFR), the fibroblast growth factor receptor (FGFR), the insulin receptor (IR), and the vascular endothelial growth factor receptor (VEGFR). This target compound showed potent inhibitory activity, especially against FGFR with IC50 = 5.18 μM.