☆ 4.7 Article

Novel 3,5-Bis(bromohydroxybenzylidene)piperidin-4-ones as Coactivator-Associated Arginine Methyltransferase 1 Inhibitors: Enzyme Selectivity and Cellular Activity

JOURNAL OF MEDICINAL CHEMISTRY (2011)

期刊

JOURNAL OF MEDICINAL CHEMISTRY

卷 54, 期 13, 页码 4928-4932

出版社

AMER CHEMICAL SOC

DOI: 10.1021/jm200453n

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Chemistry, Medicinal

资金

Fondazione Roma
COST Action Epigenetics [TD09/05]
NIEHS [ES007784, ES015188]

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Coactivator-associated arginine methyltransferase 1 (CARM1) represents a valuable target for hormone-dependent tumors such as prostate and breast cancers. Here we report the enzyme and cellular characterization of the 1-benzyl-3,5-bis(3-bromo-4-hydroxybenzylidene)piperidin-4-one (7g) and its analogues 8a-1. Among them, 7g, 8e, and 8a-1 displayed high and selective CARM1 inhibition, with lower or no activity against a panel of different PRMTs or HKMTs. In human LNCaP cells, 7g showed a significant dose-dependent reduction of the PSA promoter activity.

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