Next Article in Journal
2-C-Alkynyl and 2-C-cis-Alkenyl β-Mannosides with Acetal Protected γ-Aldehyde Functionality via 2-Uloside Alkynylation and Lindlar Hydrogenation
Previous Article in Journal
4,4′-Bis[4-(4′-hydroxyphenyl)phenylazo]diphenyl Ether
Open AccessShort Note

(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
Molbank 2016, 2016(4), M915; https://doi.org/10.3390/M915
Received: 28 September 2016 / Revised: 29 October 2016 / Accepted: 8 November 2016 / Published: 10 November 2016
(This article belongs to the Section Organic Synthesis)
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
Show Figures

Graphical abstract

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.

Show more citation formats Show less citations formats
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop