The synthesis of novel bisphosphonates as inhibitors of phosphoglycerate kinase (3-PGK)
A series of conformationally-restrained analogues of 1,3-bisphospho-D-glyceric acid (1,3-BPG) 1 has been synthesised for use as inhibitors of 3-PGK (E.C. 2.7.2.3). These compounds have non-scissile phosphonate linkages and also incorporate α-halogen substituents to make them isopolar and isosteric mimics of the natural substrate. A monocyclic aryl core between the two phosphoryl centres provides both a rigid framework linking these moieties and loci for further substitution. The compounds were tested against human 3-PGK and found to be good competitive inhibitors. α-Fluorination of the phosphonic acids increased the affinity for the enzyme into the submicromolar range. Correlation of IC50 data with pKa. and pKa, values indicates that the acidity of the phosphoryl group exerts a strong influence on protein binding. The Royal Society of Chemistry 2000.
Caplan, Neil A.,Pogson, Christopher I.,Hayes, David J.,Blackburn, G. Michael
p. 421 - 437
(2007/10/03)
Stilbenoid dendrimers
The first five generations of the stilbenoid dendrimers 1(n) (n = 1-5) have been prepared by a combined coupled synthesis (between the generations of the dendrons 8-12) and convergent synthesis. Wittig-Horner reactions together with a protecting group tec
Meier, Herbert,Lehmann, Matthias,Kolb, Ute
p. 2462 - 2469
(2007/10/03)
Stilbenoid dendrimers
A convergent synthesis in which all trans double bonds were constructed by Wittig-Horner reactions produces dendrimers of the general structure 1. With long-chain alkoxy residues on the periphery of the benzene rings, the first two generations display liq
Meier, Herbert,Lehmann, Matthias
p. 643 - 645
(2007/10/03)
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