Title of article
[d4U]-butyne-[HI-236] as a non-cleavable, bifunctional NRTI/NNRTI HIV-1 reverse-transcriptase inhibitor
Author/Authors
Roger Hunter، نويسنده , , Clare I. Muhanji، نويسنده , , Ian Hale، نويسنده , , Christopher M. Bailey، نويسنده , , Aravind Basavapathruni، نويسنده , , Karen S. Anderson، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
4
From page
2614
To page
2617
Abstract
The synthesis of bifunctional compound 10 consisting of d4U joined at C-5 to a butynyl spacer attached to HI-236 is reported using a Sonogashira coupling as a key step. As a non-cleavable bifunctional HIV inhibitor incorporating an NRTI with an NNRTI, 10 shows good inhibitory activity (EC50 = 250 nM) against HIV (IIIB) replication in MT-2 cell culture, which is eight times greater than that of d4T and between those of the two component drugs.
Keywords
HIV RT bifunctional inhibitor , NRTI and NNRTI double-drug , Sonogashira coupling , HIV Heterodimer
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798092
Link To Document