Title:Natural-derived Polyphenols as Potential Anticancer Agents
Volume: 12
Issue: 8
Author(s): Carmela Spatafora and Corrado Tringali
Affiliation:
Keywords:
Polyphenols, Flavonoids, Stilbenoids, Structure-activity relationship, Anticancer agents, chemopreventive, therapeutic index, antiproliferative, coumarins, depolymerising agent
Abstract: In this short review we report selected examples from recent literature to show the potential of natural-derived, low molecular
weight polyphenols as antitumor agents. The two major groups of polyphenol analogues have been reviewed here, namely flavonoids and
stilbenoids. Notwithstanding these limitations, we listed 75 compounds, many of them representing only the most potent member in a
library. In addition, many studies afforded useful SARs which may be the basis for future optimization. In this regard, it is worth
highlighting the close structural relationships connecting some families of tubulin inhibitors, namely analogues of chalcones,
combretastatin A-4, and resveratrol. Some interesting hybrid molecules have already been obtained, such as chalcone-combretastatin and
chalcone-resveratrol hybrids. The optimization of natural polyphenols reputed to be anticarcinogenic has also been addressed to improve
their metabolic stability and a number of analogues, which are more stable to metabolic conversion and display comparable or higher
antitumor activity than the parent compound, have been obtained. In some cases analogues with higher lipophilicity showed higher
activity than the parent compound, in particular stilbenoids, flavanols, and flavone derivatives. Table 1 summarizes the main biological
data on the natural-derived polyphenols cited within this review.
As a whole, this survey of recently reported, natural-derived polyphenols, though not exhaustive, clearly indicates that intensive research
is being carried out in the area of antitumor polyphenol analogues and suggests that in the near future some polyphenolic leads may
become useful anticancer drugs or adjuvants in cancer therapy.
