Najahi E., Valentin A., Tene N., Treilhou M., Nepveu Françoise. (2013). Synthesis and biological evaluation of new bis-indolone-N-oxides. Bioorganic Chemistry, 48, p. 16-21. ISSN 0045-2068.
Titre du document
Synthesis and biological evaluation of new bis-indolone-N-oxides
Najahi E., Valentin A., Tene N., Treilhou M., Nepveu Françoise
Source
Bioorganic Chemistry, 2013,
48, p. 16-21 ISSN 0045-2068
A series of bis-indolone-N-oxides, 1a-f, was prepared from bis(ethynyl)benzenes and o-halonitroaryls and studied for their in vitro antiplasmodial activities against Plasmodium falciparum and representative strains of bacteria and candida as well as for their cytotoxicity against a human tumor cell line (MCF7). They did not cause any haemolysis (300 mu g mL(-1)). Of the synthesized bis-indolones, compound 1a had the most potent antiplasmodial activity (IC50 = 0.763 mu mol L-1 on the FcB1 strain) with a selectivity index (CC50 MCF7/IC50 FcB1) of 35.6. No potency against the tested microbial strains was observed.
Plan de classement
Sciences fondamentales / Techniques d'analyse et de recherche [020]
;
Entomologie médicale / Parasitologie / Virologie [052]
