The stilbene scaffold is a basic element for a number of biologically
active natural and synthetic compounds, and it is considered as a privileged structure.
Stilbenes exemplified by resveratrol, combretastatin A-4 and pterostilbene
are of significant interest for drug research and development because of their
potential in therapeutic and preventive application. Resveratrol, present in grapes
and other food products, plays a role in the prevention of several human
pathological processes and has been suggested as an anticancer agent. Moreover,
recent evidence has revealed its potential effect on the aging process, diabetes and
neurological dysfunction. Combretastatin A-4, from the bark of South African
bush willow Combretum caffrum, also shows significant antitumor activity.
Pterostilbene is closely related to resveratrol, sharing the same unique therapeutic
potential as anti-inflammatory, antineoplastic and antioxidant agent.
Therefore, research and development of stilbene-based medicinal chemistry have
become rapidly evolving and increasingly active topics covering almost the whole
range of therapeutic fields.
In the present review, we provide an overview of the role of stilbenes in medicinal
chemistry. In this context, we highlight the chemical methodologies adopted for
the synthesis of stilbene derivatives, and outline the successful design of novel
stilbene based hybrids in the field of cancer, Alzheimer’s and other relevant
diseases. This information may be useful in further design of stilbene-based
molecules as new leads for the development of novel agents with clinical potential
or as effective chemical probes to dissect biological processes.