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Thiazolidine derivatives as potent and selective inhibitors of the PIM kinase family.

Abstract:

The PIM family of serine/threonine kinases have become an attractive target for anti-cancer drug development, particularly for certain hematological malignancies. Here, we describe the discovery of a series of inhibitors of the PIM kinase family using a high throughput screening strategy. Through a combination of molecular modeling and optimization studies, the intrinsic potencies and molecular properties of this series of compounds was significantly improved. An excellent pan-PIM isoform inh...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1016/j.bmc.2017.02.056

Authors


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Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Organic Chemistry
Role:
Author
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Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Organic Chemistry
Role:
Author
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Funding agency for:
Fedorov, O
Grant:
1097737
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Funding agency for:
Knapp, S
Grant:
1097737
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Funding agency for:
Huber, K
Grant:
C17468/A9332
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Funding agency for:
Quevedo, C
Grant:
C17468/A9332
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Funding agency for:
Russell, A
Grant:
Fellowship
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Publisher:
Elsevier Publisher's website
Journal:
Bioorganic & Medicinal Chemistry Journal website
Volume:
25
Issue:
9
Pages:
2657-2665
Publication date:
2017-02-01
Acceptance date:
2017-02-25
DOI:
ISSN:
0968-0896 and 1464-3391
Source identifiers:
687672
Language:
English
Keywords:
Pubs id:
pubs:687672
UUID:
uuid:7b0cdcdc-22cb-46f9-9a3a-f3e33a8b468d
Local pid:
pubs:687672
Deposit date:
2017-05-16

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