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Synthesis, kinase activity and molecular modeling of a resorcylic acid lactone incorporating an amide and a trans-enone in the macrocycle
National University of Ireland, Galway, Ireland.
Örebro University, School of Science and Technology.
National University of Ireland, Galway, Ireland; University of Gothenburg, Göteborg, Sweden.
National University of Ireland, Galway, Ireland.
2012 (English)In: Tetrahedron, ISSN 0040-4020, E-ISSN 1464-5416, Vol. 68, no 27-28, p. 5533-5540Article in journal (Refereed) Published
Abstract [en]

Details for the synthesis of a resorcylic acid lactone (RAL) incorporating a trans-enone and an amide in the macrocyclic ring are provided herein. The sequence included the assembly of three fragments by esterification, olefination, and lactamization. The RAL with the lactam was less potent as an inhibitor of kinases than other RALs investigated. The biological results were rationalized by docking and molecular dynamics simulations of the lactam bound to human ERK2 and comparison with hypothemycin.

Place, publisher, year, edition, pages
Elsevier, 2012. Vol. 68, no 27-28, p. 5533-5540
Keywords [en]
Resorcylic acid lactones, Kinase inhibitors, Olefination, Lactamization
National Category
Chemical Sciences
Research subject
Chemistry
Identifiers
URN: urn:nbn:se:oru:diva-24622DOI: 10.1016/j.tet.2012.04.082ISI: 000306350800026Scopus ID: 2-s2.0-84862017041OAI: oai:DiVA.org:oru-24622DiVA, id: diva2:545848
Available from: 2012-08-21 Created: 2012-08-21 Last updated: 2017-12-07Bibliographically approved

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Palwai, Viraja R.

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