N-Aryltriazole ribonucleosides with potent antiproliferative activity against drug-resistant pancreatic cancer

被引：25

作者：

Liu, Yang ^{[2
]}

Xia, Yi ^{[1
]}

Fan, Yuting ^{[2
]}

Maggiani, Alain ^{[1
]}

Rocchi, Palma ^{[3
]}

Qu, Fanqi ^{[2
]}

Iovanna, Juan L. ^{[3
]}

Peng, Ling ^{[1
]}

机构：

[1] CNRS, Dept Chim, UPR CINaM 3118, F-13288 Marseille, France

[2] Wuhan Univ, Coll Chem & Mol Sci, State Key Lab Virol, Wuhan 430072, Peoples R China

[3] INSERM, U624, F-13288 Marseille, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 08期

基金：

美国国家科学基金会;

关键词：

Nucleosides; N-Arylated triazole nucleoside; Triazole nucleosides; Pancreatic cancer; N-Arylation; TOBACCO-MOSAIC-VIRUS; SHOCK-PROTEIN; 27; BITRIAZOLYL COMPOUNDS; THERAPEUTIC TARGETS; ANDROGEN ABLATION; HUISGEN REACTION; PROSTATE-CANCER; ACYCLONUCLEOSIDES; GEMCITABINE; HEAT-SHOCK-PROTEIN-27;

D O I：

10.1016/j.bmcl.2010.02.104

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel N-aryltriazole nucleosides were synthesized via Cu-mediated C-N cross-coupling reaction starting with 3-aminotriazole ribonucleoside and various boronic acids. Two of them exhibited potent apoptosis-related antiproliferative activity against the drug-resistant pancreatic cancer cell line MiaPaCa-2, with an increased potency compared to gemcitabine, the reference treatment for pancreatic cancer. A preliminary SAR study suggests that the appended N-aryl moiety and the substituent at its para-position, as well as the ribose sugar component, contribute considerably to the observed antiproliferative activity. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：2503 / 2507

页数：5

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