Diadenylated polyols as new non-isopolar analogues of diadenosine tri- and tetraphosphates
摘要:
A series of diadenosine polyphosphate-mimics were prepared based upon phosphorothioylation of the hydroxyl functions of polyols 1 and 1,3,2-oxathiaphospholane ring-opening condensation methodology. (C) 1999 Elsevier Science Ltd. All rights reserved.
Inhibition of ADP-triggered blood platelet aggregation by diadenosine polyphosphate analogues
作者:Bogdan Walkowiak、Janina Baraniak、Czeslaw S. Cierniewski、Wojciech Stec
DOI:10.1016/s0960-894x(02)00318-9
日期:2002.8
The synthesis and biological evaluation of new diadenosine polyphosphateanalogues on blood platelet aggregation are reported. The most active are compounds with a sulfur atom replacing one or both non-bridging oxygens at phosphorus bound to adenosyl residues and hydroxymethyl groups of bis(hydroxymethyl)phosphinic acid.
nucleosides based on a bis(hydroxymethyl)phosphinicacid (BHPA) backbone were obtained by condensation of the bis(4,4′-dimethoxytrityl) derivative of BHPA with N-1- or N-3-(2-hydroxyethyl)thymine in the presence of MSNT, or by an Appel reaction with N-1- or N-3-(2-aminoethyl)thymine. After selective deprotection and phosphitylation they were used as monomers for automated solid support synthesis of short oligomers