SUBSTITUTED CHALKONES AS DRUGS

摘要

This invention pertains to substituted chalcones, specifically substituted 1-(4-methoxyphenyl)-3-(3,5-dimethoxyphenyl)prop-1-en-3-ones, which have therapeutic application, for example, as potent antiproliferative agents and antiinflammatory agents, and which have the formula (I) wherein: X is -H, -OH, -OC(=O)R3, -OS(=O)2OH, or -OP(=O)(OH)2; Y is -H or a C1-4alkyl group; Z is -H or -OCH3; R1 is -H, a C1-4alkyl group, or C1-4fluoroalkyl group; R2 is -H, a C1-4alkyl group, or C1-4fluoroalkyl group; and, R3 is -H, a C1-6alkyl group, a C3-20 heterocyclyl group, or a C5-20aryl group; and pharmaceutically acceptable salts, esters, and protected forms thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, for both diagnosis and treatment of, for example, proliferative conditions, such as cancer, and inflammatory conditions.