Substituted chalcones as therapeutic compounds

A method of treating a proliferative condition in a patient comprising administering to said patient a therapeutically-effective amount of a compound having the formula:

• 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 C3-20heterocyclyl group, or a C5-20aryl group;
• or a pharmaceutically acceptable salt, ester, or protected form thereof.

A method of prophylactically treating a proliferative condition in a patient comprising administering to said patient a therapeutically-effective amount of a compound having the formula:

• 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 C3-20heterocyclyl group, or a C5-20aryl group;
• or a pharmaceutically acceptable salt, ester, or protected form thereof.

A method of treating a inflammatory condition in a patient comprising administering to said patient a therapeutically-effective amount of a compound having the formula:

• 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 C3-20heterocyclyl group, or a C5-20aryl group;
• or a pharmaceutically acceptable salt, ester, or protected form thereof.

A method of diagnosis of a patient for the presence of tumour cells expressing the CYP1B1 enzyme, comprising:

• (a) administering to the patient a compound having the formula:
• wherein:
• X is —H;
• 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 C3-20heterocyclyl group, or a C5-20aryl group;
• or a pharmaceutically acceptable salt, ester, or protected form thereof;
• (b) determining the amount of the corresponding hydroxylated metabolite, wherein X is —OH, which is subsequently produced;
• and,
• (c) correlating the amount with the presence or absence of the tumour cells in the patient.

A compound of the formula:

• 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 C3-20heterocyclyl group, or a C5-20aryl group;
• or a pharmaceutically acceptable salt, ester, or protected form thereof;
• with the proviso that X, Y, Z, R1, and R2 are not all —H and at least two of X, Y and Z are not hydrogen when R1 and R2 are hydrogen.