An Intramolecular Heck Approach To Obtain 17-Membered Macrocyclic Diversity and the Identification of an Antiangiogenesis Agent from a Zebrafish Assay
2013 (English)In: European Journal of Organic Chemistry, ISSN 1434-193X, E-ISSN 1099-0690, no 19, 3955-3958 p.Article in journal (Refereed) Published
We report a practical and modular approach to obtain two different types of 17-membered ring macrocyclic compounds through an intramolecular Heck reaction. These macrocyclic compounds are functionalized, that is, they contain two contiguous stereogenic hydroxy functional groups and an amino acid moiety in the macrocyclic ring skeleton. The macrocycles were then screened against a zebrafish assay to determine the antiangiogenesis activity of these small molecules. Macrocyclic compound 2.2a was identified as a potent inhibitor at 2.5 M, whereas its acyclic precursor and the other related macrocyclic compounds did not show any effect.
Place, publisher, year, edition, pages
2013. no 19, 3955-3958 p.
IdentifiersURN: urn:nbn:se:sh:diva-19539DOI: 10.1002/ejoc.201300408ISI: 000320720100002ScopusID: 2-s2.0-84879246191OAI: oai:DiVA.org:sh-19539DiVA: diva2:642657