摘要:
                                Syntheses of several new analogues of lyngbyatoxin A from a single common intermediate are described.  These compounds bear a carbon chain at the 7-position of the indolactam V (ILV) nucleus which contains either a hydrophilic or a lipophilic group.  The effect of these minor structural alterations on the ability of the ILV analogues to activate the enzyme protein kinase C (PKC) was determined by measuring the extent of phosphorylation of calf thymus histone (III-S).  Introduction of a hydroxyl group on the C-7 appendage was found to dramatically decrease compound 3's ability to activate PKC.  This result is interpreted in terms of the decreased ability of 3 to associate with the membrane bilayer.