Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1373597 | Bioorganic & Medicinal Chemistry Letters | 2007 | 4 Pages |
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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Roger Hunter, Clare I. Muhanji, Ian Hale, Christopher M. Bailey, Aravind Basavapathruni, Karen S. Anderson,