Antileukemic Properties and Structure-Activity Relationships of O- and SGlycosylatedDerivatives of Juglone and Related 1,4-Naphthoquinones

Abstract

Glycosylated derivatives of physiologically active natural compound juglone and related 1,4- naphthoquinones are known as antifungal, immunomodulatory, and antitumor substances. However, their antileukemic properties and struc- ture-activity relationships have been studied insufficiently. Antileukemic effects and structure-activity relationships (SAR) of the 50 1,4- naphthoquinone derivatives were examined using HL-60 human promyelocytic leukemia cells and MTS method of the study of cell viability. As was shown, the substances inhibited viability of HL-60 cells at the wide range of concentrations. SAR study revealed the structure peculiarities which lead to increase or decrease of the antileu- kemic activity of the compounds studied. In conclusion, O- or S- glycosylated derivatives of juglone and related 1,4- naphthoquinones have potential for development of the new antileukemic agents and should be further investigated.