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Molbank 2016, 2016(4), M915; doi:10.3390/M915

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

1
Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Beni Suef University, Beni Suef 62514, Egypt
2
Department of Pharmaceutical Chemistry, College of Pharmacy, Al Jouf University, Sakaka, Al Jouf 2014, Saudi Arabia
3
Department of Zoology, Faculty of Science, Al-Azhar University, Cairo 11884, Egypt
*
Author to whom correspondence should be addressed.
Academic Editor: Norbert Haider
Received: 28 September 2016 / Revised: 29 October 2016 / Accepted: 8 November 2016 / Published: 10 November 2016
(This article belongs to the Section Organic Synthesis)
View Full-Text   |   Download PDF [476 KB, uploaded 22 November 2016]   |  

Abstract

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. View Full-Text
Keywords: pyrazole; pyrazolo[3,4-d]pyrimidine; anticancer; protein kinases pyrazole; pyrazolo[3,4-d]pyrimidine; anticancer; protein kinases
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Bakr, R.B.; Mehany, A.B.M. (3,5-Dimethylpyrazol-1-yl)-[4-(1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ylamino)phenyl]methanone. Molbank 2016, 2016, M915.

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