Inhibitors of JMJD2C as Anticancer Agents

摘要

The present disclosure provides compounds, pharmaceutical compositions and related methods for the treatment of cancer, e.g., castration-resistant prostate cancer (CRPC). Specifically, the present disclosure provides a series of 8-hydroxyquinoline derivatives which show cytotoxic effects on androgen-independent prostate cancer cells.

主权项

1. A compound of Formula I: wherein
X is CH or a bond;R1 is selected from H, alkyl and substituted alkyl;R2 is selected from H, alkyl, substituted alkyl, amino, substituted amino, cycloalkyl, substituted cycloalkyl, heterocyclyl and substituted heterocyclyl;R3 is selected from H, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, heterocyclyl, substituted heterocyclyl, aryl, substituted aryl, heteroaryl and substituted heteroaryl; andR4 is selected from H, alkyl and substituted alkyl,or a salt or stereoisomer thereof, wherein
if X is a bond, then R2 is H, R3 is absent and R1 is aminoalkyl or substituted aminoalkyl, andif R3 is heteroaryl or substituted aryl, then R4 is alkyl or substituted alkyl.