SYNTHESIS OF A PENTASACCHARIDE-OLIGONUCLEOTIDE CONJUGATE - A NOVEL ANTITHROMBOTIC AGENT

Authors
BUIJSMAN RC KUIJPERS WHA BASTEN JEM KUYLYEHESKIELY E VANDERMAREL GA VANBOECKEL CAA VANBOOM JH
Citation
Rc. Buijsman et al., SYNTHESIS OF A PENTASACCHARIDE-OLIGONUCLEOTIDE CONJUGATE - A NOVEL ANTITHROMBOTIC AGENT, Chemistry, 2(12), 1996, pp. 1572-1577
Citations number
28
Categorie Soggetti
Chemistry
Journal title
Chemistry → ACNP
ISSN journal
09476539
Volume
2
Issue
12
Year of publication
1996
Pages
1572 - 1577
Database
ISI
SICI code
0947-6539(1996)2:12<1572:SOAPC->2.0.ZU;2-3
Abstract
Derivatization of the octadecathymidylate derivative 18 (T-18 ODN) con taining a free amine function with sulfo-SIAB(R) gave the correspondin g iodoacetyl ODN 21. Conjugation of the latter with the thiol-containi ng pentasaccharide 17c gave pentasaccharide-ODN conjugate III, which e xhibited anti-Xa and antithrombin activities of 173 U mg(-1) and 5 U m g(-1), respectively.