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, Alexander D. MacKerell, 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.
Claims5
A pharmaceutical composition, comprising:
- a compound pharmacologically effective to inhibit Runt-related transcription factor 2 (RUNX2) activity in a cancer cell having a 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
- with a proviso that R1 and R2 are not both Cl or not both H or are not NHC(O)C1-3alkyl and Cl, or are not H and Br, Cl or CF3 when R4 is
- or are not H and Cl when R4 is
- or
- a pharmaceutically acceptable salt thereof;
- and
- a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.