Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.
Bioorg Med Chem Lett
; 17(10): 2886-9, 2007 May 15.
Article
in En
| MEDLINE
| ID: mdl-17350837
ABSTRACT
A novel class of selective Tie-2 inhibitors was derived from a multi-kinase inhibitor 1. By reversing the amide connectivity and incorporating aminotriazine or aminopyridine hinge-binding moieties, excellent Tie-2 potency and KDR selectivity could be achieved with 3-substituted terminal aryl rings. X-ray co-crystal structure analysis aided inhibitor design. This series was evaluated on the basis of potency, selectivity, and rat pharmacokinetic parameters.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Triazines
/
Receptor, TIE-2
Limits:
Animals
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2007
Document type:
Article
Affiliation country:
United States