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Discovery of novel pyrazolo[1,5-a]pyrimidines as potent pan-Pim inhibitors by structure- and property-based drug design.

Abstract：

:Pim kinases are promising targets for the development of cancer therapeutics. Among the three Pim isoforms, Pim-2 is particularly important in multiple myeloma, yet is the most difficult to inhibit due to its high affinity for ATP. We identified compound 1 via high throughput screening. Using property-based drug design and co-crystal structures with Pim-1 kinase to guide analog design, we were able to improve potency against all three Pim isoforms including a significant 10,000-fold gain against Pim-2. Compound 17 is a novel lead with low picomolar potency on all three Pim kinase isoforms.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Wang X,Magnuson S,Pastor R,Fan E,Hu H,Tsui V,Deng W,Murray J,Steffek M,Wallweber H,Moffat J,Drummond J,Chan G,Harstad E,Ebens AJ

doi

10.1016/j.bmcl.2013.04.020

subject

Has Abstract

pub_date

2013-06-01 00:00:00

pages

3149-53

issue

11

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(13)00489-7

journal_volume

23

pub_type

杂志文章

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