2. Academic Validation
  3. [d4U]-butyne-[HI-236] as a non-cleavable, bifunctional NRTI/NNRTI HIV-1 reverse-transcriptase inhibitor

[d4U]-butyne-[HI-236] as a non-cleavable, bifunctional NRTI/NNRTI HIV-1 reverse-transcriptase inhibitor

  • Bioorg Med Chem Lett. 2007 May 1;17(9):2614-7. doi: 10.1016/j.bmcl.2007.01.107.
Roger Hunter 1,  Clare I Muhanji,  Ian Hale,  Christopher M Bailey,  Aravind Basavapathruni,  Karen S Anderson
Affiliations

Affiliation

  • 1 Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa. Roger.Hunter@uct.ac.za
PMID: 17317163 DOI: 10.1016/j.bmcl.2007.01.107
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.

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