The synthesis of indolo[2,3-b]quinoline derivatives with a guanidine group: Highly selective cytotoxic agents

作者: Katarzyna Sidoryk , Marta Świtalska , Anna Jaromin , Piotr Cmoch , Iwona Bujak

DOI: 10.1016/J.EJMECH.2015.10.022

关键词:

摘要: The synthesis of indolo[2,3-b]quinoline derivatives containing guanidine, amino acid or guanylamino substituents as well their in vitro evaluation for the cytotoxic and antifungal activity are reported. influence guanidine group on selective hemolytic properties was investigated. Most compounds displayed a high two most promising (3 12) exhibited selectivity between normal cancer cell-lines. compound 3 about 600-fold lower against fibroblasts than A549 MCF-7 cell lines. Novel entities acted DNA-intercalators when tested using DNA-methyl green assay but demonstrated zero low in comparison to unsubstituted analogs. mechanism action studied 12 both were found be very effective inducers apoptosis.

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