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Bioorganic & medicinal chemistry letters

Novel azulene-based derivatives as potent multi-receptor tyrosine kinase inhibitors.


PMID 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.

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A97203
Azulene, 99%
C10H8