The Koch research group is currently focused on the development of doxazolidine prodrugs for the treatment of primary liver cancer and pancreatic cancer. Doxazolidine, discovered in the Koch group, is a formaldehyde conjugate of the broad spectrum anti-tumor drug doxorubicin. Doxazolidine is orders of magnitude more effective for induction of tumor cell apoptosis than doxorubicin and works by a different mechanism. Doxazolidine is very short lived under physiological conditions and requires prodrug delivery. A prodrug is inactive and robust in vivo and transformed to the active drug at the disease site. The group is designing and evaluating strategies for selective prodrug delivery of doxazolidine to tumors through activation of the prodrug by enzymes highly abundant at the tumor.
keywords
drug discovery and development for cancer, drug mechanism, primary liver cancer, pancreatic cancer, non small cell lung cancer, drug formulation, drug pharmacology, drug toxicology, drug efficacy, doxorubicin, doxazolidine, prodrug design, carboxylesterases, plasmin, cathepsin B, RGD peptides, SELEX, PhotoSELEX, aptamers, protein nucleic acid photocrosslinking, medical diagnostics
A PREFERRED METHOD FOR IMIDE PREPARATION.
Synthetic Communications: an international journal for rapid communication of synthetic organic chemistry.
447-454.
1981
