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Bioorg Med Chem Lett ; 20(20): 6129-32, 2010 Oct 15.
Article in English | MEDLINE | ID: mdl-20833039

ABSTRACT

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.


Subject(s)
Antineoplastic Agents/chemistry , Antineoplastic Agents/therapeutic use , Azulenes/chemistry , Azulenes/therapeutic use , Leukemia, Myeloid, Acute/drug therapy , Receptor Protein-Tyrosine Kinases/antagonists & inhibitors , Animals , Antineoplastic Agents/blood , Antineoplastic Agents/pharmacology , Azulenes/blood , Azulenes/pharmacology , Cell Line, Tumor , Cell Proliferation , Humans , Mice , Mice, Inbred BALB C , Mice, Nude , Rats , Receptor Protein-Tyrosine Kinases/metabolism , fms-Like Tyrosine Kinase 3/antagonists & inhibitors
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