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

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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Mourer M,Psychogios N,Laumond G,Aubertin AM,Regnouf-de-Vains JB

doi

10.1016/j.bmc.2009.11.016

subject

Has Abstract

pub_date

2010-01-01 00:00:00

pages

36-45

issue

1

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(09)01024-4

journal_volume

18

pub_type

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