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

Bioorganic & Medicinal Chemistry
Maxime MourerJean-Bernard Regnouf-de-Vains

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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Citations

May 10, 2011·Chemical Communications : Chem Comm·Florent Perret, Anthony W Coleman
Mar 1, 2012·Drug and Chemical Toxicology·Bahram Mokhtari, Kobra Pourabdollah
Aug 14, 2020·Polymers·Miriam Trigo-LópezJosé M García
Jan 23, 2020·Angewandte Chemie·Yu-Chen PanDong-Sheng Guo
Nov 11, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Dmitriy N ShurpikPeter J Cragg
Dec 15, 2016·Organic Letters·Maria Koyioni, Panayiotis A Koutentis

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