Organic compounds -- part of the class 532-570 series – Organic compounds – Phosphorus esters
Patent
1991-12-13
1993-12-28
Higel, Floyd D.
Organic compounds -- part of the class 532-570 series
Organic compounds
Phosphorus esters
514118, 514553, 514603, 514114, 558169, 558170, 558171, 558172, 562 67, 564 85, 564 94, A01N 4716, A01N 4102, A01N 3734, A61K 31445, C07F 902
Patent
active
052741621
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.
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