Patent ID: 6391884
Filing Date: 2002-05-21
Classification: A61K,A61P,C07H,C12Q,G01N

Abstract:
A method for inhibiting the proliferation of a hyperproliferative cell, comprising contacting the cell with a prodrug that is selectively converted to a toxin in the cell by endogenous, intracellular thymidylate synthase, wherein the prodrug is an L- or D-compound of the formula: wherein R1 is a toxic metabolite extractable from the pyrimidine ring by thymidylate synthase and wherein R1 is selected from the group consisting of â€”Br, â€”I, â€”O-alkyl, â€”O-aryl, O-heteroaryl, â€”S-alkyl, â€”S-aryl, â€”S-heteroaryl, â€”CN, â€”OCN, â€”SCN, â€”NH2, â€”NH-alkyl, â€”N(alkyl)2, â€”NHCHO, â€”NHOH, â€”NHO-alkyl, NH2CONHOâ€”, NHNH2, and â€”N3; and wherein Q is selected from the group consisting of sugar groups, thio-sugar groups, carbocyclic groups and salts thereof.