Synthesis of novel pyrazolo[3,4-d]pyrimidine derivatives as potential anti-breast cancer agents

被引：49

作者：

Abd El Hamid, Mohammed K. ^{[1
]}

Mihovilovic, Marko D. ^{[2
]}

El-Nassan, Hala B. ^{[1
]}

机构：

[1] Cairo Univ, Dept Organ Pharmaceut Chem, Fac Pharm, Cairo 11562, Egypt

[2] Vienna Univ Technol, Inst Appl Synthet Chem, A-1040 Vienna, Austria

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 57卷

关键词：

Pyrazolo[3,4-d]pyrimidine; Antitumor activity; MCF7; INHIBITORS; ANTICANCER;

D O I：

10.1016/j.ejmech.2012.09.031

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

A series of new 1-aryl-4-benzylidenehydrazinyl-3-methylsulphanyl-pyrazolo[3,4-d]pyrimidines 6a-p was synthesized. The cytotoxic activity of the newly synthesized compounds against human breast cancer cell line, MCF7 was investigated. Most of the test compounds showed potent antitumor activity comparable to that of doxorubicin. The 1-phenyl series (6a-i) exhibited better antitumor activity than 1-(4-methoxyphenyl) series (6j-p). 4-[2-(4-Fluorobenzylidene)hydrazinyl]-3-(methylsulphanyl)-1-phenyl-1H-pyrazolo[3,4-d]pyrimidine (6d) was the most active compound in this study with IC50 equal to 7.5 nM. (C) 2012 Elsevier Masson SAS. All rights reserved.

引用

页码：323 / 328

页数：6

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