2-Phenoxy-3-Trichloromethylquinoxalines Are Antiplasmodial Derivatives with Activity against the Apicoplast of Plasmodium falciparum.
Amrane D, Arnold CS, Hutter S, Sanz-Serrano J, Collia M, Azqueta A, Paloque L, Cohen A, Amanzougaghene N, Tajeri S, Franetich JF, Mazier D, Benoit-Vical F, Verhaeghe P, Azas N, Vanelle P, Botté C, Primas N.
Amrane D, et al.
Pharmaceuticals (Basel). 2021 Jul 26;14(8):724. doi: 10.3390/ph14080724.
Pharmaceuticals (Basel). 2021.
PMID: 34451821
Free PMC article.
The biological evaluation highlighted a hit compound (3i) with a potent PfK1 EC(50) value of 0.2 M and a HepG2 CC(50) value of 32 M (Selectivity index = 160). Nitro-containing (3i) was not genotoxic, both in the Ames test and in vitro comet assay. Activity cliffs we …
The biological evaluation highlighted a hit compound (3i) with a potent PfK1 EC(50) value of 0.2 M and a HepG2 CC(50) value of 32 M ( …