|
|||||
|
|
Isosteric replacement of the Z-enone with haloethyl ketone and E-enone in a resorcylic acid lactone series and biological evaluation |
|
| Authors: | Napolitano Carmela Natoni Alessandro Santocanale Corrado Evensen Lasse Lorens James B Murphy Paul V |
| Affiliation: | a School of Chemistry, National University of Ireland, Galway, University Road, Galway, Ireland b National Centre for Biomedical Engineering Science and Centre for Chromosome Biology, National University of Ireland Galway, University Road, Galway, Ireland c Department of Biomedicine, University of Bergen, Jonas Lies Vei 91, N-5009 Bergen, Norway |
| Abstract: | 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 β-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). |
| Keywords: | Resorcylic acid lactones Photoisomerization Kinase inhibitors Tumor growth |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |