Record number :
1104667
Title of article :
Synthesis, kinase activity and molecular modeling of a resorcylic acid lactone incorporating an amide and a trans-enone in the macrocycle
Author/Authors :
Carmela Napolitano، نويسنده , , Viraja R. Palwai، نويسنده , , Leif A. Eriksson، نويسنده , , Paul V. Murphy، نويسنده ,
Issue Information :
هفته نامه با شماره پیاپی سال 2012
Pages :
8
From page :
5533
To page :
5540
Abstract :
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.
Keywords :
Kinase inhibitors , Olefination , Resorcylic acid lactones , lactamization
Journal title :
Tetrahedron
Serial Year :
2012
Link To Document :
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