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American Chemical Society, Journal of Medicinal Chemistry, 13(54), p. 4928-4932, 2011

DOI: 10.1021/jm200453n

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

Journal article published in 2011 by Donghang Cheng, Sergio Valente, Sabrina Castellano, Gianluca Sbardella, Roberto Di Santo ORCID, Roberta Costi ORCID, Mark T. Bedford, Antonello Mai
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This paper is available in a repository.

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Abstract

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-l. Among them, 7g, 8e, and 8l 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. © 2011 American Chemical Society.