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Discovery of potent and highly selective thienopyridine Janus kinase 2 inhibitors.

Abstract：

:Developing Janus kinase 2 (Jak2) inhibitors has become a significant focus for small molecule drug discovery programs in recent years due to the identification of a Jak2 gain-of-function mutation in the majority of patients with myeloproliferative disorders (MPD). Here, we describe the discovery of a thienopyridine series of Jak2 inhibitors that culminates with compounds showing 100- to >500-fold selectivity over the related Jak family kinases in enzyme assays. Selectivity for Jak2 was also observed in TEL-Jak cellular assays, as well as in cytokine-stimulated peripheral blood mononuclear cell (PBMC) and whole blood assays. X-ray cocrystal structures of 8 and 19 bound to the Jak2 kinase domain aided structure-activity relationship efforts and, along with a previously reported small molecule X-ray cocrystal structure of the Jak1 kinase domain, provided structural rationale for the observed high levels of Jak2 selectivity.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Schenkel LB,Huang X,Cheng A,Deak HL,Doherty E,Emkey R,Gu Y,Gunaydin H,Kim JL,Lee J,Loberg R,Olivieri P,Pistillo J,Tang J,Wan Q,Wang HL,Wang SW,Wells MC,Wu B,Yu V,Liu L,Geuns-Meyer S

doi

10.1021/jm200911r

subject

Has Abstract

pub_date

2011-12-22 00:00:00

pages

8440-50

issue

24

eissn

0022-2623

issn

1520-4804

journal_volume

54

pub_type

杂志文章

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