RUNX2 transcription factor inhibitors and uses thereof
AssigneesUniversity of Maryland, Baltimore, The United States of America as represented by the Department of Veterans Affairs
InventorsAntonino Passaniti, MacKerell D. Alexander, Jr.
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Abstract
Provide herein are compounds with a general chemical structure of: Substituents R1 and R2 independently are H, Cl, F, Br, CH3, CF3, SH, —N(C1-3alkyl)2, —NHC(O)C1-3alkyl, or —NHC(O)C5-7cycloalkyl, substituent R3 is H or C1-3 alkyl and R4 is a bridged cycloalkene such as a bridged cyclohexene or a bridge-substituted cyclohexene. The compounds are therapeutics to treat a cancer, such as breast cancer, or metastatic cancers, to inhibit RUNX2 activity, such as protein expression, in a cancer cell and to increase survival of a subject with breast cancer.
Claims22
A method for treating breast cancer in a subject, comprising:
- administering to the subject a dose of one or more compounds having the chemical structure
- wherein
- R1 and R2 independently are H, Cl, F, Br, CH3, CF3, SH, —N(C1-3alkyl)2, —NHC(O)C1-3alkyl, or —NHC(O)C5-7cycloalkyl;
- R3 is H or C1-3 alkyl;
- and
- R4 is
- or
- a pharmaceutically acceptable salt thereof effective to inhibit a RUNX2 activity, thereby treating the breast cancer.
A method for treating a metastatic cancer originating from a breast cancer in a subject, comprising:
- administering to the subject a dose of one or more compounds having the chemical structure
- wherein
- R1 and R2 independently are H, Cl, F, Br, CH3, CF3, SH, —N(C1-3alkyl)2, —NHC(O)C1-3alkyl, or —NHC(O)C5-7cycloalkyl;
- R3 is H or C1-3 alkyl;
- and
- R4 is
- or
- a pharmaceutically acceptable salt thereof effective to inhibit a RUNX2 activity, thereby treating the metastatic cancer.
A method for treating breast cancer in a subject, comprising
- administering to the subject a dose of a compound having the chemical structure:
- or a pharmaceutically acceptable salt thereof effective to inhibit RUNX2, thereby treating the breast cancer.
Dependencies are inferred from the claim text.