Antileukemic Properties and Structure-Activity Relationships of O- and S- Glycosylated Derivatives of Juglone and Related 1,4-Naphthoquinones

Glycosylated derivatives of physiologically active natural compound juglone and related 1,4naphthoquinones are known as antifungal, immunomodulatory, and antitumor substances. However, their antileukemic properties and structure-activity relationships have been studied insufficiently. Antileukemic effects and structure-activity relationships (SAR) of the 50 1,4naphthoquinone 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 antileukemic activity of the compounds studied. In conclusion, Oor Sglycosylated derivatives of juglone and related 1,4naphthoquinones have potential for development of the new antileukemic agents and should be further investigated.