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Novel Inverse Binding Mode of Indirubin Derivatives Yields Improved Selectivity for DYRK Kinases.

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...

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Publication status:
Published

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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

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