Structurally complex compounds exhibiting diverse anticancer activity profiles


Natural products have historically provided a major source of drugs and therapeutic agents; for example, about 50% of anticancer drugs and 60% of antibacterial drugs are natural products or semisynthetic derivatives thereof. Skeletal diversity and high stereochemical content are well-known attributes that endow natural products with the ability to engage a variety of biological molecules with high affinity and specificity, leading to biological and pharmacological activity. Notably, while a number of synthetic strategies have been explored for the generation of natural product-like molecules, none of them utilizes an enzyme-catalyzed C–H oxidation or epoxidation step as a means for generating structurally diverse new molecules from a parent scaffold.

Technology Overview

This technology provides for novel natural product-like molecules obtained through the chemoenzymatic re-elaboration and modification of parthenolide, a plant-derived natural product that has found use for the treatment of pain, migraine, and rheumatoid arthritis, as well as in antitumor, antiviral, and antileishmanial applications. In particular, enzymatic functionalization of parthenolide is combined with a series of molecular rearrangement and editing reactions resulting in a library of new and complex natural product-like molecules. These molecules exhibit potent anticancer activity as well as a diverse anticancer activity profile, including compounds with broad‑spectrum activity against multiple types of cancers as well as compounds with cancer-type specificity


These compounds exhibit high structural and stereochemical complexity akin to that found in natural products and encompass a diverse set of new molecular scaffolds possessing biological activity. In particular, they possess potent and diverse anticancer activity as well as the potential for antimicrobial, antibiotic, antifungal, and anti-inflammatory activity. Owing to the optional presence of an electrophilic ‘warhead’ in their structure, these compounds are also well suited for covalent engagement of their biomolecular target, including their use as molecular glues for targeted protein degradation.


Cancer treatment.

URV Reference Number: 1-22062
Patent Information:
For Information, Contact:
Curtis Broadbent
Licensing Manager
University of Rochester
Rudi Fasan
Andrew Bortz
John Bennett