Resveratrol, phenstatin and combretastatin A-4 are molecules belonging to the classes of stilbenes or benzophenones. Resveratrol is known to possesst a variety of useful biological properties, i.e. antileukemic and antibacterial properties, and has displayed cancer cell growth inhibition in vitro. Combretastatin A-4 has anti-mitotic activity and is now in phase III clinical trials to study its effectiveness in treating a variety of cancers. Early structure-activity work demonstrated that phenstatin, a benzophenone, retained most of the cytotoxic properties of combretastatin A-4.
Further structure-activity relationship efforts resulted in the discovery of other novel stilbenes and benzophenones possessing anti-neoplastic and/or anti-microbial activities.
Examples of the novel compounds are (Z)- and (E)- 3,4’,5-trimethoxystibene; (Z)- and (E)- 3,5-dimethoxy-4’-hydroxystilbene; (Z)- and (E)- 3-hydroxy-4’,5-dimethoxystilbene; (Z)- and (E)- 3,5-dihydroxy-4’-methoxystilbene; sodium resverastatin dibenzyl phosphate and sodium resverastatin phosphate.
Since these novel compounds have comparable results to their previously known structural analogs they have applications as:
- Anti-neoplasic and anti-cancer therapeutic agents
- Anti-microbial and anti-fungal agents
Benefits and Advantages
- Diversity – Numerous compounds have been synthesized and their effects have been analyzed on variety of human tumor cell lines, showing a panel of diverse inhibitory profiles. Compounds also present anti-microbial/anti-fungal activities.
- Synthesis – The syntheses for the new compound are well described.
- Efficacy – Testing results demonstrate improved activities in comparison with the resveratrol.
For more information about the inventor(s) and their research, please see
Dr. Pettit's departmental webpage