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

被引：15

作者：

Bakr, Rania B. ^{[1
,2
]}

Mehany, Ahmed B. M. ^{[3
]}

机构：

[1] Beni Suef Univ, Fac Pharm, Pharmaceut Organ Chem Dept, Bani Suwayf 62514, Egypt

[2] Al Jouf Univ, Coll Pharm, Dept Pharmaceut Chem, Sakaka, Al Jouf, Saudi Arabia

[3] Al Azhar Univ, Fac Sci, Dept Zool, Cairo 11884, Egypt

来源：

MOLBANK | 2016年 / 04期

关键词：

pyrazole; pyrazolo[3,4-d] pyrimidine; anticancer; protein kinases;

D O I：

10.3390/M915

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

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 mu M. 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 mu M.

引用

页数：6

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