23751-23-7

Upstream product

• 98447-30-4 2-bromo-4-methoxy-1-nitrobenzene 
• 43192-31-0 2-bromo-4-methoxybenzaldehyde 
• 768-60-5 4-methoxyphenylacetylen 
• 3989-14-8 (4-methoxyphenylethynyl)trimethylsilane 
• 1133204-83-7 5-methoxy-2-(4-methoxyphenyl)-3-oxo-3H-indole 1-oxide 

Relevant academic research and scientific papers

2-Aryl-3H-indol-3-ones: Synthesis, electrochemical behaviour and antiplasmodial activities

The synthesis of indolone derivatives and their antiplasmodial activity in vitro against Plasmodium falciparum at the blood stage are described. The 2-aryl-3H-indol-3-ones were synthesized via deoxygenation of indolone-N-oxides. Electrochemical behaviour, antiplasmodial activity and cytotoxicity on human tumor cell lines were compared to those of indolone-N-oxides. The antiplasmodial IC50 (concentrations at 50% inhibition) of these compounds ranged between 49 and 1327 nM. Among them, the 2-(4-dimethylaminophenyl)-5-methoxy- indol-3-one, 7, had the best antiplasmodial activity in vitro (IC50 = 49 nM; FcB1 strain) and selectivity index (SI (CC50 MCF7/IC 50 FcB1) = 423.4). Thus, the hits identified in this deoxygenated series correspond to their structural homologs in the N-oxide series with comparable electrochemical behaviour at the nitrogen-carbon double bond.