Coumarin-based inhibitors of HIV integrase.

  title={Coumarin-based inhibitors of HIV integrase.},
  author={Hui Ming Zhao and Nouri Neamati and H Hong and Amitabha Mazumder and Shaomeng Wang and Sham Sunder and Garth W. Milne and Yves Pommier and Terrence R. Burke},
  journal={Journal of medicinal chemistry},
  volume={40 2},
The structures of a large number of HIV-1 integrase inhibitors have in common two aryl units separated by a central linker. Frequently at least one of these aryl moieties must contain 1,2-dihydroxy substituents in order to exhibit high inhibitory potency. The ability of o-dihydroxy-containing species to undergo in situ oxidation to reactive quinones presents a potential limitation to the utility of such compounds. The recent report of tetrameric 4-hydroxycoumarin-derived inhibitor 5 provided a… CONTINUE READING
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