Synthesis of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates and evaluation of their Src kinase inhibitory and anticancer activities

被引：104

作者：

Kumar, Anil ^{[1
,2
]}

Ahmad, Israr ^{[1
]}

Chhikara, Bhupender S. ^{[2
]}

Tiwari, Rakesh ^{[2
]}

Mandal, Deendayal ^{[2
]}

Parang, Keykavous ^{[2
]}

机构：

[1] Birla Inst Technol & Sci, Dept Chem, Pilani 333031, Rajasthan, India

[2] Univ Rhode Isl, Dept Biomed & Pharmaceut Sci, Kingston, RI 02881 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 05期

基金：

美国国家科学基金会;

关键词：

Anticancer activity; Click reaction; Phenylpyrazolopyrimidine; Src kinase; 1,2,3-Triazole; Tyrosine kinase; CONSTRAINED PEPTIDE ANALOGS; TYROSINE KINASE; BREAST-CANCER; POTENT INHIBITORS; DISCOVERY; GROWTH; LCK; INVASION; RECEPTOR; SKI-606;

D O I：

10.1016/j.bmcl.2011.01.047

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 two classes of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates were synthesized using click chemistry approach. All compounds were evaluated for inhibition of Src kinase and human ovarian adenocarcinoma (SK-Ov-3), breast carcinoma (MDA-MB-361), and colon adenocarcinoma (HT-29). Hexyl triazolyl-substituted 3-phenylpyrazolopyrimidine exhibited inhibition of Src kinase with an IC50 value of 5.6 mu M. 4-Methoxyphenyl triazolyl-substituted 3-phenylpyrazolopyrimidine inhibited the cell proliferation of HT-29 and SK-Ov-3 by 73% and 58%, respectively, at a concentration of 50 mu M. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：1342 / 1346

页数：5

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