Kozikowski A P, Ma D, Du L, Lewin N E, Bumberg P M
Mayo Foundation for Medical Education and Research, Jacksonville, Florida 32224, USA.
Farmaco. 1995 Jun;50(6):425-30.
A palladium catalyzed route for the preparation of several benzofuran analogues of the PKC activator indolactam V (ILV) is described together with the ability of these compounds to activate the isoforms of PKC. The benzofuran analogues of ILV are shown to activate PKC with a slightly different pattern of isotype selectivity than ILV or 7-n-octyl-ILV. Moreover, in an examination of the effect of stereochemistry at the C-14 center of the teleocidins on PKC binding activity, a clear preference for R-stereochemistry at the C-14 center was found, thus providing additional verification of previously published structural correlations between the families of PKC activators.
描述了一种钯催化的路线，用于制备蛋白激酶C（PKC）激活剂吲哚内酰胺V（ILV）的几种苯并呋喃类似物，以及这些化合物激活PKC亚型的能力。结果表明，ILV的苯并呋喃类似物激活PKC的同型选择性模式与ILV或7-正辛基-ILV略有不同。此外，在研究teleocidins的C-14中心立体化学对PKC结合活性的影响时，发现C-14中心对R-立体化学有明显偏好，从而为先前发表的PKC激活剂家族之间的结构相关性提供了额外验证。
