| Literature DB >> 17317163 |
Roger Hunter1, Clare I Muhanji, Ian Hale, Christopher M Bailey, Aravind Basavapathruni, Karen S Anderson.
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 (EC(50)=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.Entities:
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Year: 2007 PMID： 17317163 DOI： 10.1016/j.bmcl.2007.01.107
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823