1,4-Naphthoquinones are a group of natural and synthetic substances that participate
in various biochemical functions in most plants and animals, being involved in energy
production, electron transport, blood coagulation, and generation of reactive oxygen species
(ROS), among others. The performance of such biochemical functions is directly related to the
functional groups linked to the 1,4-naphthoquinone scaffold, and the introduction of nitrogencontaining
groups into this nucleus may amplify its biological activity against numerous targets.
Therefore, several methods have been developed in the last decades for preparing these
compounds, especially from 1,4-naphthoquinone derivatives. Considering these concepts, in
this review, we aim to provide insights into the chemistry, chemical synthesis, semi-synthesis,
pharmacological effects, and reactivity of low molecular weight mono- and bis(aminonaphthoquinones);
we start by discussing the use of some of the most important 1,4-naphthoquinones as starting materials
for the synthesis of amino-1,4-naphthoquinones (ANQs), examine the modification of ANQ derivatives, and conclude
by providing an outlook on this field.