2-Phenylaminonaphthoquinones and related compounds: synthesis, trypanocidal and cytotoxic activities.

作者: Ivan Sieveking , Pablo Thomas , Juan C Estévez , Natalia Quiñones , Mauricio A Cuéllar

DOI: 10.1016/J.BMC.2014.07.030

关键词:

摘要: A series of new 2-aminonaphthoquinones and related compounds were synthesized evaluated in vitro as trypanocidal cytotoxic agents. Some tested inhibited epimastigote growth trypomastigote viability. Several showed similar or higher activity selectivity compared with current drug, nifurtimox. Compound 4l exhibit than nifurtimox against Trypanosoma cruzi comparison Vero cells. the quinones cancer cells normal fibroblasts, showing that certain chemical modifications on naphthoquinone moiety induce excellent increase index cytotoxicity (4g 10). The results presented here show anti-T. derivatives can be improved by replacement benzene ring a pyridine moiety. Interestingly, presence chlorine atom at C-3 highly lipophilic alkyl group aromatic are newly observed elements should lead to discovery more selective compounds.

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