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
收藏
页码：2503 / 2507
页数：5
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