ORBi: Hale K. J. - Synthesis of a simplified bryostatin C-ring analogue that binds to the CRD2 of human PKC-alpha and construction of a novel BC-analogue by an unusual Julia olefination process

Reference : Synthesis of a simplified bryostatin C-ring analogue that binds to the CRD2 of human PKC...


	Document type :	Scientific journals : Article
	Discipline(s) :	Physical, chemical, mathematical & earth Sciences : Chemistry
	To cite this reference:	http://hdl.handle.net/2268/77941

Title :	Synthesis of a simplified bryostatin C-ring analogue that binds to the CRD2 of human PKC-alpha and construction of a novel BC-analogue by an unusual Julia olefination process
Language :	English
Author, co-author :	Hale, K. J. [> > > >]
	Frigerio, M. [ > > ]
	Manaviazar, S. [> > > >]
	Hummersone, M. G. [> > > >]
	Fillingham, I. J. [> > > >]
	Barsukov, I. G. [> > > >]
	Damblon, Christian [Université de Liège - ULg > Département de chimie (sciences) > Chimie biologique structurale >]
	Gescher, A. [> > > >]
	Roberts, G. C. K. [> > > >]
Publication date :	2003
Journal title :	Organic Letters
Publisher :	American Chemical Society
Volume :	5
Issue/season :	4
Pages :	499-502
Peer reviewed :	Yes (verified by ORBi)
ISSN :	1523-7060
e-ISSN :	1523-7052
Abstract :	[en] [GRAPHICS] The synthesis of two truncated bryostatin analogues 2 and 3 is described. High-field NMR measurements on the C-ring analogue 3 in (CH3CN)-H-2 containing 25% (H2O)-H-2 have shown that it binds to the CRD2 of human PKC-alpha at virtually the same position as phorbol-13-acetate (PA) and bryostatin 1 (1). NMR titration studies have also revealed that 3 binds to the CRD2 with a potency similar in magnitude to PA but much less potently than 1.
Permalink :	http://hdl.handle.net/2268/77941
DOI :	10.1021/ol027392u

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