Menadione (Vitamin K3) comprises of 1,4-naphthoquinone (NQ) moiety that can form
redox isomers such as napthosemiquinone (NSQ) and catechol by accepting one or two electrons,
respectively. The quinone redox cycling ability leads to the generation of "reactive oxygen species"
(ROS) as well as arylation reactions, which are of biological relevance. This ability can be
modulated with the help of suitable derivatization. A pharmacophore can be appended at suitable
position of Vitamin K3 to have a synergistic or additive effect. In the present review, an attempt has
been made to accrue such derivatives modified at 1 or 2 position and evaluated for their
cytotoxicity activity on different series of human cancer cell lines such as HeLa, HL-60 and MCF-
7 etc. Production of reactive oxygen species (ROS) and mitochondrial dysfunction caused by
Vitamin K3 derivatives leads to apoptosis and tumor inhibition. Recently, the CR-108 compound
has shown to exhibit oxidative path together with non-oxidative phosphorylation of p38 MAP
kinase in human breast cancer cells. Thus the chemical-biological interactions have been discussed
which can be further extrapolated for the development of a potent anticancer drug.
Keywords: Anticancer activity, antioncogenic activity, chemical biology, mechanism, polymorph, redox isomers, QSAR.
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