Journal article
Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.
- Abstract:
-
The bromodomain protein module, which binds to acetylated lysine, is emerging as an important epigenetic therapeutic target. We report the structure-guided optimization of 3,5-dimethylisoxazole derivatives to develop potent inhibitors of the BET (bromodomain and extra terminal domain) bromodomain family with good ligand efficiency. X-ray crystal structures of the most potent compounds reveal key interactions required for high affinity at BRD4(1). Cellular studies demonstrate that the phenol a...
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- Publication status:
- Published
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- Publisher copy:
- 10.1021/jm301588r
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Authors
Bibliographic Details
- Journal:
- Journal of medicinal chemistry
- Volume:
- 56
- Issue:
- 8
- Pages:
- 3217-3227
- Publication date:
- 2013-04-01
- DOI:
- EISSN:
-
1520-4804
- ISSN:
-
0022-2623
- Source identifiers:
-
390906
Item Description
- Language:
- English
- Keywords:
- Pubs id:
-
pubs:390906
- UUID:
-
uuid:0e7f0389-b43f-425a-8884-39502b8e63dd
- Local pid:
- pubs:390906
- Deposit date:
- 2013-11-16
Terms of use
- Copyright date:
- 2013
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