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

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Chen CH, Lee O, Yao CN, Chuang MY, Chang YL, Chang MH, Wen YF, Yang WH, Ko CH, Chou NT, Lin MW, Lai CP, Sun CY, Wang LM, Chen YC, Hseu TH, Chang CN, Hsu HC, Lin HC, Chang YL, Shih YC, Chou SH, Hsu YL, Tseng HW, Liu CP, Tu CM, Hu TL, Tsai YJ, Chen TS, Lin CL, Chiou SJ, Liu CC, Hwang CS

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

Bioorg Med Chem Lett. 2010 Oct 15;20(20):6129-32. doi: 10.1016/j.bmcl.2010.08.025. Epub 2010 Aug 10.

PubMed ID
20833039 [ View in PubMed
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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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
SunitinibPlatelet-derived growth factor receptor betaIC 50 (nM)17N/AN/ADetails
SunitinibReceptor-type tyrosine-protein kinase FLT3IC 50 (nM)3N/AN/ADetails
SunitinibReceptor-type tyrosine-protein kinase FLT3IC 50 (nM)16N/AN/ADetails
SunitinibVascular endothelial growth factor receptor 2IC 50 (nM)53N/AN/ADetails