Wisconsin Alumni Research Foundation

Therapeutics & Vaccines
Therapeutics Vaccines
Library of Glycosylated Chlorambucil Analogs for Cancer Treatment
WARF: P110076US02

Inventors: Jon Thorson, Randal Goff

The Wisconsin Alumni Research Foundation (WARF) is seeking commercial partners interested in developing a set of glycosylated chlorambucil molecules that are potentially useful as anti-tumor or anti-metastatic agents.
Many of the compounds used in drug discovery by pharmaceutical companies consist of a central core structure (aglycon) and various sugar (glycosyl) attachments. Because the sugar moieties of many of these compounds define their biological activities, altering the carbohydrate ligands can lead to valuable new pharmaceuticals.  A UW–Madison researcher previously developed a glycorandomization method for rapidly generating a diverse library of novel glycosylated compounds for use in drug discovery (see WARF reference number P04020US). 

Chlorambucil currently is used as a leukemia treatment. This compound, which was first synthesized more than 50 years ago, acts by prohibiting DNA replication and transcription, ultimately killing cells. However, it is not specific to tumor cells, resulting in adverse side effects such as decreasing bone marrow function.
The Invention
UW–Madison researchers have used glycorandomization to develop a set of 63 glycosylated chlorambucil molecules. Several of these novel compounds are efficacious against various types of cancer cells. They could be developed into cancer therapeutics.
  • Cancer treatment
Key Benefits
  • Provides novel compounds for use as cancer therapeutics
  • Some of the analogs show greater anti-cancer activity than the parent chlorambucil molecule.
Additional Information
  • Goff R.D. and Thorson J.S. 2010. Assessment of Chemoselective Neoglycosylation Methods Using Chlorambucil as a Model. J. Med. Chem. 53, 8129-8139.
For current licensing status, please contact Rafael Diaz at [javascript protected email address] or 608-960-9847