期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 4, 页码 1167-1170出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.12.100
关键词
Resorcylic acid lactones; Photoisomerization; Kinase inhibitors; Tumor growth
资金
- Science Foundation Ireland [PI/IN1/B966, 08/IN.1/B2064]
- COST Action (Angiokem) [CM0602]
- Science Foundation Ireland (SFI) [08/IN.1/B2064] Funding Source: Science Foundation Ireland (SFI)
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.
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