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Napolitano, C,Natoni, A,Santocanale, C,Evensen, L,Lorens, JB,Murphy, PV
2011
February
Bioorganic & Medicinal Chemistry Letters
Isosteric replacement of the Z-enone with haloethyl ketone and E-enone in a resorcylic acid lactone series and biological evaluation
Published
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Resorcylic acid lactones Photoisomerization Kinase inhibitors Tumor growth IN-VITRO KINASE HYPOTHEMYCIN PHOSPHORYLATION ACTIVATION POTENT TRANSFORMATION SPECIFICITY INHIBITORS RADICICOL
21
1167
1170
The synthesis of a small library of resorcylic acid lactones and evaluation of their biological properties as kinase inhibitors is described. Within the series E-enones were found more active than corresponding Z-enones as inhibitors of a subset of kinases containing a conserved cysteine. Replacement of the enone moiety with a beta-haloketone group led to compounds with an interesting kinase selectivity profile and also antiproliferative activity against Jurkat cells. An E-enone derivative also showed activity against capillary tube formation based on a co-culture of primary human umbilical cord endothelial cells (HUVECs) and vascular smooth muscle cells (vSMCs). (c) 2010 Elsevier Ltd. All rights reserved.
DOI 10.1016/j.bmcl.2010.12.100
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