220867-48-1Relevant articles and documents
Synthesis and biological activity of (2'-5')oligoadenylate trimers containing a 5'-terminal 5'-amino-5'-deoxy- or 5'-amino-3',5'- dideoxyadenosine derivative
Kvasyuk, Evgeny I.,Mikhailopulo, Igor A.,Homan, Joseph W.,Iacono, Kathryn T.,Muto, Nicholas F.,Suhadolnik, Robert J.,Pfleiderer, Wolfgang
, p. 19 - 29 (2007/10/03)
The new (2'-5')oligoadenylate trimers 26-34 containing 5'-amino-5'- deoxyadenosine or 5'-amino-3',5'-dideoxyadenosine or their lipophilic 5'- deoxy-5'-(hexadecanoylamino) derivatives at the 5'-terminus, and adenosine or 3'-deoxyadenosine (=cordycepin) at the penultimate and T-end position of the trimers were synthesized by the phosphoramidite method. The newly synthesized trimers 26-34 inhibited, at 100 μM concentration, HIV-1-induced syncytia formation (SYN) by 19-96% and reverse-transcriptase activity (RT) by 27-100% (see Table). The two hexadecanoylamino derivatives 27 and 30 which were found to be potent inhibitors of SYN and RT showed also a 73 and 49% inhibition, respectively, of expression of HIV-1 p24 antigen (p24-EX). The same compounds 27 and 30 inhibited also, with a 100% efficacy, an amplification of HIV-1 partial reverse transcripts (PCR) and HIV-1 integrase activity (INT), respectively.