Patent ID: 6528517
Filing Date: 2003-03-04
Classification: C07D

Abstract:
A method for stabilizing a topoisomerase II-DNA complex comprising the step of contacting a cell containing said complex with a DNA intercalating quinobenzoxazine derivative that has a formula: or a pharmaceutically acceptable salt, ester, or amide thereof, in whichm=0, 1, 2; mâ€²=0, 1, 2; n=0, 1, 2; nâ€²=0, 1, 2; R1=hydrogen or carboxy-protecting group; R2=hydrogen, halogen, or alkyl consisting of 1 to 6 carbon atoms; R3 or R4=alkyl, acyl, amino acids, short peptides, or DNA alkylating, groove binding, intercalating functionalities, or any ligand for nuclear receptors; A=oxygen, sulfur, or carbon; Z=a halogen or nitrogen-containing group consisting of 1 to 6 carbon atoms; X=hydrogen or halogen; W=hydrogen, nitro, amino, alkyl amino, halo-substituted alkyl, or halogen; B=N, O, S, C, CH, CH2; C=N, O, S, C, CH, CH2; whereby said quinobenzoxazine derivative binds to and stabilizes said complex.