Quinoline and thiazolopyridine allosteric inhibitors of MALT1

被引：13

作者：

Scott, David A. ^{[1
,2
]}

Hatcher, John M. ^{[1
,2
]}

Liu, Hongyan ^{[5
]}

Fu, Mingpeng ^{[5
]}

Du, Guangyan ^{[1
,2
]}

Fontan, Lorena ^{[3
]}

Us, Ilkay ^{[3
]}

Casalena, Gabriella ^{[3
]}

Qiao, Qi ^{[4
]}

Wu, Hao ^{[4
]}

Melnick, Ari ^{[3
]}

Gray, Nathanael S. ^{[1
,2
]}

机构：

[1] Dana Farber Canc Inst, Dept Canc Biol, Boston, MA 02115 USA

[2] Harvard Med Sch, Dept Biol Chem & Mol Pharmacol, 360 Longwood Ave, Boston, MA 02115 USA

[3] Cornell Univ, Div Hematol & Oncol, Dept Med, Weill Cornell Med, New York, NY 10021 USA

[4] Harvard Med Sch, Program Cellular & Mol Med, Boston Childrens Hosp, Boston, MA 02115 USA

[5] PepTech Shanghai Pharmaceut Corp, 388 Yindu Rd, Shanghai 200231, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2019年 / 29卷 / 14期

关键词：

MALT1; Protease inhibitors; Allosteric; B-cell lymphomas; PROTEASE;

D O I：

10.1016/j.bmcl.2019.05.040

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Quinolines and thiazolopyridines were developed as allosteric inhibitors of MALT1, with good cellular potency and exquisite selectivity. Mouse pharmacokinetic (PK) profiling showed these to have low in vivo clearance, and moderate oral exposure. The thiazolopyridines were less lipophilic than the quinolines, and one thiazolopyridine example was active in our hIL10 mouse pharmacodynamic (PD) model upon oral dosing.

引用

页码：1694 / 1698

页数：5

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