Antineoplastic drugs with bipolar toxification/detoxification functionalities
US5274162A · kind A · utility
Inventor
Key dates
| Filing date | Dec 13, 1991 |
| Grant date | Dec 28, 1993 |
| Priority date | — |
| Expiry date | Dec 13, 2011 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07F9/2429
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The composition, methods of synthesis, and applications of a new class of tumor selective antineoplastic drugs is described. These novel antineoplastic agents are of the general structure: A-C-B. The agents are designed with two key functionalities: a trigger which toxifies the drug; (A) and a deactivator which detoxifies the drug (B) The trigger is selected such that it is activated by an enzyme which is present in elevated levels in the tumor. The deactivator is selected such that it is actuated by an enzyme ubiquitous to all tissues. The fate of the drug in a given cell is then determined by the ratio of the enzymatic activity that triggers toxication to the enzymatic activity which detoxifies the drug. The partitioning of the drug between toxic metabolite and nontoxic metabolite defines the resulting specificity of cytotoxic effect. The application of this invention is exemplified by a new class of antineoplastic drugs which are designed to be selectively toxic for tumor cells bearing the enzyme guanidinobenzoatase.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.