- Abstract:
-
DYRK kinases are involved in alternative pre-mRNA splicing as well as in neuropathological states such as Alzheimer's disease and Down syndrome. In this study, we present the design, synthesis, and biological evaluation of indirubins as DYRK inhibitors with enhanced selectivity. Modifications of the bis-indole included polar or acidic functionalities at positions 5' and 6' and a bromine or a trifluoromethyl group at position 7, affording analogues that possess high activity and pronounced spe...
Expand abstract - Publication status:
- Published
- Publisher copy:
- 10.1021/ml300207a
-
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- Journal:
- ACS medicinal chemistry letters
- Volume:
- 4
- Issue:
- 1
- Pages:
- 22-26
- Publication date:
- 2013-01-05
- DOI:
- EISSN:
-
1948-5875
- ISSN:
-
1948-5875
- URN:
-
uuid:b21bd950-90be-4383-84dd-268ba016b3ad
- Source identifiers:
-
375787
- Local pid:
- pubs:375787
- Language:
- English
- Keywords:
- Copyright date:
- 2013
Journal article
Novel Inverse Binding Mode of Indirubin Derivatives Yields Improved Selectivity for DYRK Kinases.
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