1.
Bioorg Med Chem Lett
; 20(20): 6129-32, 2010 Oct 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-20833039
RESUMO
A series of azulene-based derivatives were synthesized as potent inhibitors for receptor tyrosine kinases such as FMS-like tyrosine kinase 3 (FLT-3). Systematic side chain modification of prototype 1a was carried out through SAR studies. Analogue 22 was identified from this series and found to be one of the most potent FLT-3 inhibitors, with good pharmaceutical properties, superior efficacy, and tolerability in a tumor xenograft model.