RÉSUMÉ
Isomeric oxathiolone fused chalcones were prepared by condensation of appropriate acetylbenzo[1,3]oxathiol-2-ones with benzaldehydes under acidic conditions. The synthesized compounds were screened for cytotoxic activity using HeLa cells, as well as for antibacterial activity against Micrococcus luteus, Staphylococcus aureus, Salmonella typhimurium, Escherichia coli, Proteus vulgaris, antifungal activity against Candida albicans, and tuberculostatic activity against Mycobacterium tuberculosis H(37)Rv and Mycobacterium kansasii strains.
Sujet(s)
Anti-infectieux/synthèse chimique , Anti-infectieux/pharmacologie , Antinéoplasiques/synthèse chimique , Antinéoplasiques/pharmacologie , Composés hétérocycliques bicycliques/composition chimique , Composés hétérocycliques bicycliques/pharmacologie , Chalcones/composition chimique , Chalcones/pharmacologie , Antituberculeux/synthèse chimique , Antituberculeux/pharmacologie , Lignée cellulaire tumorale , Chalcones/isolement et purification , Tests de criblage d'agents antitumoraux , Cellules HeLa , Humains , Isomérie , Spectroscopie par résonance magnétique , Tests de sensibilité microbienne , Sels de tétrazolium , ThiazolesRÉSUMÉ
Biological activity of thioaurones was not tested so far and the group constitute completely unexplored source of new molecules of pharmacological interest. We report synthesis and evaluation of cytotoxic activity of thioaurone derivatives bearing p-hydroquinone system in ring A. Their activity was found to depend strongly on substitution pattern, so eventually both the activity and pharmacokinetic parameters of the molecules could be tailored by further structural modifications.