1. Academic Validation
  2. Synthesis and anti-HIV evaluation of water-soluble calixarene-based bithiazolyl podands

Synthesis and anti-HIV evaluation of water-soluble calixarene-based bithiazolyl podands

  • Bioorg Med Chem. 2010 Jan 1;18(1):36-45. doi: 10.1016/j.bmc.2009.11.016.
Maxime Mourer 1 Nicolas Psychogios Géraldine Laumond Anne-Marie Aubertin Jean-Bernard Regnouf-de-Vains
Affiliations

Affiliation

  • 1 SRSMC, UMR 7565 Nancy Université, CNRS, Equipe Groupe d'Etude des Vecteurs Supramoléculaires du Médicament, Faculté de Pharmacie, 5 rue Albert Lebrun, 54001 Nancy Cedex, France.
Abstract

Nine anionic water-soluble calix[4]arene species, incorporating sulfonate, carboxylate or phosphonate groups, six of them incorporating two 2,2'-bithiazole subunits in alternate position at the lower rim, have been synthesised and evaluated as anti-HIV agents on various HIV strains and cells of the lymphocytic lineage (HIV-1 III B/MT4, HIV-1 LAI/CEM-SS, HIV-1 Bal/PBMC), using AZT as reference compound. A toxicity was detected for a minority of compounds on PBMC whereas for the Others no cellular toxicity was measured at concentrations up to 100 microM. Most of the compounds have an Antiviral activity in a 10-50 microM range, and one of them, sulfonylated, displays its activity, whatever the tropism of the virus, at a micromolar concentration.

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