2,3-Substituted quinoxalin-6-amine analogs as antiproliferatives: A structure-activity relationship study

被引：36

作者：

Chen, Qianyi ^{[1
,3
]}

Bryant, Vashti C. ^{[1
,3
]}

Lopez, Hernando ^{[1
]}

Kelly, David L. ^{[1
]}

Luo, Xu ^{[1
]}

Natarajan, Amarnath ^{[1
,2
,3
]}

机构：

[1] Univ Nebraska Med Ctr, Eppley Inst Res Canc, Omaha, NE 68198 USA

[2] Univ Nebraska Med Ctr, Dept Genet Cell Biol & Anat, Omaha, NE 68198 USA

[3] Univ Texas Med Branch, Dept Pharmacol & Toxicol, Chem Biol Program, Galveston, TX 77555 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 07期

基金：

美国国家卫生研究院;

关键词：

Quinoxaline urea; Antiproliferative; Mcl-1 dependent apoptosis; SMALL-MOLECULE INHIBITORS; HIGH-THROUGHPUT SCREEN; CYCLOPHILIN-A; DERIVATIVES;

D O I：

10.1016/j.bmcl.2011.02.055

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The quinoxaline core is considered a privileged scaffold as it is found in a variety of biologically relevant molecules. Here we report the synthesis of a quinoxalin-6-amine library, screening against a panel of cancer cell lines and a structure-activity relationship (SAR). This resulted in the identification of a bisfuranylquinoxalineurea analog (7c) that has low micromolar potency against the panel of cancer cell lines. We also show that cells treated with quinoxalineurea 7c results in caspase 3/7 activation, PARP cleavage and Mcl-1 dependent apoptosis. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：1929 / 1932

页数：4

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