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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.
Authors: Hale, KJ
Frigerio, M
Manaviazar, S
Hummersone, MG
Fillingham, IJ
Barsukov, IG
Damblon, CF
Gescher, A
Roberts, GC
First Published: 20-Feb-2003
Citation: ORG LETT, 2003, 5 (4), pp. 499-502
Abstract: [structure: see text] The synthesis of two truncated bryostatin analogues 2 and 3 is described. High-field NMR measurements on the C-ring analogue 3 in C(2)H(3)CN containing 25% (2)H(2)O 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.
DOI Link: 10.1021/ol027392u
ISSN: 1523-7060
Type: Journal Article
Appears in Collections:Published Articles, Dept. of Biochemistry

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