Journal article icon

Journal article

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...

Expand abstract
Publication status:
Published

Actions


Access Document


Publisher copy:
10.1021/ml300207a

Authors


Expand authors...
Journal:
ACS medicinal chemistry letters
Volume:
4
Issue:
1
Pages:
22-26
Publication date:
2013-01-01
DOI:
EISSN:
1948-5875
ISSN:
1948-5875
Source identifiers:
375787
Language:
English
Keywords:
Pubs id:
pubs:375787
UUID:
uuid:b21bd950-90be-4383-84dd-268ba016b3ad
Local pid:
pubs:375787
Deposit date:
2013-11-16

Terms of use


Views and Downloads






If you are the owner of this record, you can report an update to it here: Report update to this record

TO TOP