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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

Journal article
Authors C. Napolitano
V. R. Palwai
Leif A Eriksson
P. V. Murphy
Published in Tetrahedron
Volume 68
Issue 27-28
Pages 5533-5540
ISSN 0040-4020
Publication year 2012
Published at Department of Chemistry and Molecular Biology
Pages 5533-5540
Language en
Keywords Resorcylic acid lactones, Kinase inhibitors, Olefination, Lactamization, methoxybenzyl pmb ethers, force-field, secondary alcohols, tyrosine, kinases, in-vitro, inhibitors, phosphorylation, activation, cancer, potent, ss db, 1991, journal of the american chemical society, v113, p7277, ss db, 1983, journal of organic chemistry, v48, p4155
Subject categories Biochemistry and Molecular Biology, Chemical Sciences, Organic Chemistry, Physical Chemistry, Theoretical Chemistry, Biophysical chemistry


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. (c) 2012 Elsevier Ltd. All rights reserved.

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