Efficient synthesis of novel disubstituted pyrido[3,4-b]pyrazines for the design of protein kinase inhibitors

被引：4

作者：

Antoine, Maud ^{[1
,3
]}

Schuster, Tilmann ^{[2
]}

Seipelt, Irene ^{[2
]}

Aicher, Babette ^{[2
]}

Teifel, Michael ^{[2
]}

Guenther, Eckhard ^{[2
]}

Gerlach, Matthias ^{[2
]}

Marchand, Pascal ^{[1
]}

机构：

[1] Univ Nantes, Nantes Atlantic Univ, Lab Chim Therapeut Cibles & Medicaments Infect &, UFR Sci Pharmaceut & Biol, 1 Rue Gaston Veil, F-44035 Nantes, France

[2] AEterna Zentaris GmbH, Weismuellerstr 50, D-60314 Frankfurt, Germany

[3] AtlanChim Pharma, 3 Rue Aronnax, F-44821 St Herblain, France

来源：

MEDCHEMCOMM | 2016年 / 7卷 / 02期

关键词：

BIOLOGICAL EVALUATION; SER/THR KINASES; DUAL INHIBITORS; CANCER-THERAPY; ANALOGS; AGENTS; DISCOVERY; ETHYL; PYRIDO;

D O I：

10.1039/c5md00424a

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A novel family of disubstituted pyrido [3,4-b] pyrazine-based compounds was discovered as valuable series for the design of promising protein kinase inhibitors. SAR study allowed the identification of 4-(piperidin-1-yl) aniline moiety as pharmacophoric group, in C-5 or C-8 positions of the pyrido [3,4-b] pyrazine ring, for binding to the selected therapeutic targets. Several analogues were active at low micromomolar IC50 values against a panel of seven cancer-related protein kinases providing an excellent starting point for further drug discovery optimization.

引用

页码：224 / 229

页数：6

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