Discovery of N-substituted 7-azaindoles as Pan-PIM kinase inhibitors - Lead series identification - Part II

被引：4

作者：

Barberis, Claude ^{[1
]}

Moorcroft, Neil ^{[1
,6
]}

Pribish, James ^{[1
]}

Tserlin, Elina ^{[1
]}

Gross, Alexandre ^{[1
]}

Czekaj, Mark ^{[1
]}

Barrague, Matthieu ^{[1
]}

Erdman, Paul ^{[1
]}

Majid, Tahir ^{[1
]}

Batchelor, Joseph ^{[5
]}

Levit, Mikhail ^{[2
]}

Hebert, Andrew ^{[2
]}

Shen, Liduo ^{[4
]}

Moreno-Mazza, Sandra ^{[3
]}

Wang, Anlai ^{[2
]}

机构：

[1] Sanofi Genzyme, IDD Med Chem, 153 Second Ave, Waltham, MA 02451 USA

[2] Sanofi, Oncol Biol, 270 Albany St, Cambridge, MA 02139 USA

[3] Sanofi, Oncol Biochem, 270 Albany St, Cambridge, MA 02139 USA

[4] Sanofi Genzyme, DSAR, 211 Second Ave, Waltham, MA 02451 USA

[5] Sanofi, IDD Vitro Biol, 153 Second Ave, Waltham, MA 02451 USA

[6] Maxsar Biopharma, 18 Roberts Rd, Warren, NJ 07059 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2017年 / 27卷 / 20期

关键词：

Pan-PIM kinases; X-ray crystallography; AML; PK/PD; Hit-to-Lead; Small molecule inhibitor; Cancer; SELECTIVE INHIBITORS; POTENT; PROTEIN; DERIVATIVES; EXPRESSION; BINDING; HIT; BAD; OPTIMIZATION; ACTIVATION;

D O I：

10.1016/j.bmcl.2017.08.068

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

N-Substituted azaindoles have been discovered as pan-PIM kinase inhibitors. Initial SAR, early ADME and PK/PD data of a series of compounds is described and led to the identification of promising pan-PIM inhibitors which validated our interest in the 7-azaindole scaffold and led us to pursue the identification of a clinical candidate. (C) 2017 Elsevier Ltd. All rights reserved.

引用

页码：4735 / 4740

页数：6

共 16 条

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