2-Benzyl and 2-phenyl-3-hydroxypropyl pivalates as protein kinase C ligands

…, NA Perry, NE Lewin, JA Ayres, PM Blumberg

Index: Lee, Jeewoo; Lee, Ju-Hyun; Kim, Su Yeon; Perry, Nicholas A.; Lewin, Nancy E.; Ayres, Jolene A.; Blumberg, Peter M. Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 6 p. 2022 - 2031

Full Text: HTML

Citation Number: 13

Abstract

A series of 2-benzyl and 2-phenyl-3-hydroxypropyl pivalates designed to incorporate the principal pharmacophores of phorbol esters have been synthesized and tested as PKC-α ligands. Among the analogues, 13c exhibited the most potent binding affinity with a Ki= 0.7 μM. The synthesized analogues were subjected to molecular modeling analysis based on two alternative models of the phorbol pharmacophore and a docking study of 13c was ...