NOVEL PRODRUGS FOR SELECTIVE ANTICANCER THERAPY

摘要

The present invention provides a compound having the structure:;whereinX is a therapeutic agent containing at least one amine nitogen and the amine nitrogen on the therapeutic agent covalently bonds directly to carbon α;Z is CH3 or CF3;R1 is —H, —NR2R3, —NH—C(═O)—R4, —NH—C(═O)—OR4, —CH2—C(═O)—NR5R6, —OR7, —CO2R7, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, aryl, or heteroaryl,
wherein R2, R3, R4, R5, R6 and R7 are each, independently, —H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, heteroalkyl, cycloalkyl, heterocyclyl, aryl, alkylaryl, heteroaryl, alkylheteroaryl, an amino acid or an oligopeptide;
wherein an amine of the amino acid or oligopeptide is substituted or unsubstituted; andn is an integer from 0 to 6;

or a diastereomer, enantiomer or pharmaceutically acceptable salt of the compound.

主权项

1. A compound having the structure: wherein X is a therapeutic agent containing at least one amine nitogen and the amine nitrogen on the therapeutic agent covalently bonds directly to carbon α; Z is CH3 or CF3; R1 is —H, —NR2R3, —NH—C(═O)—R4, —NH—C(═O)—OR4, —CH2—C(═O)—NR5R6, —OR7, —CO2R7, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, aryl, or heteroaryl,
wherein R2, R3, R4, R5, R6 and R7 are each, independently, —H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, heteroalkyl, cycloalkyl, heterocyclyl, aryl, alkylaryl, heteroaryl, alkylheteroaryl, an amino acid or an oligopeptide;
wherein an amine of the amino acid or oligopeptide is substituted or unsubstituted; and n is an integer from 0 to 6;or a diastereomer, enantiomer or pharmaceutically acceptable salt of the compound.