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Synthesis and biological evaluation of new bis-indolone-N-oxides.

Abstract：

: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 μgmL(-1)). Of the synthesized bis-indolones, compound 1a had the most potent antiplasmodial activity (IC50=0.763 μmolL(-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.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Najahi E,Valentin A,Téné N,Treilhou M,Nepveu F

doi

10.1016/j.bioorg.2013.03.001

subject

Has Abstract

pub_date

2013-06-01 00:00:00

pages

16-21

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(13)00011-4

journal_volume

48

pub_type

杂志文章

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