申请人:University of Maryland, Baltimore
公开号:US10329246B2
公开(公告)日:2019-06-25
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.
本文提供的化合物具有以下一般化学结构:
取代基 R1 和 R2 独立地为 H、Cl、F、Br、CH3、CF3、SH、-N(C1-3 烷基)2、-NHC(O)C1-3 烷基或-NHC(O)C5-7 环烷基,取代基 R3 为 H 或 C1-3 烷基,R4 为桥式环烯,如桥式环己烯或桥式取代环己烯。这些化合物是治疗癌症(如乳腺癌)或转移性癌症的药物,可抑制癌细胞中 RUNX2 的活性(如蛋白表达),提高乳腺癌患者的存活率。