Novel 3,5-bis(bromohydroxybenzylidene)piperidin-4-ones as coactivator-associated arginine methyltransferase 1 inhibitors: enzyme selectivity and cellular activity.

Donghang Cheng 1 Sergio Valente 2 Sabrina Castellano 3 Gianluca Sbardella 3 Roberto Di Santo 2 Roberta Costi 2 Mark T Bedford 1 Antonello Mai 2, *
* Corresponding author
1 Anderson Cancer Center
2 Department of Medicinal Chemistry and Technologies
3 Dipartimento di Scienze Farmaceutiche e Biomediche
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.
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Donghang Cheng, Sergio Valente, Sabrina Castellano, Gianluca Sbardella, Roberto Di Santo, et al.. Novel 3,5-bis(bromohydroxybenzylidene)piperidin-4-ones as coactivator-associated arginine methyltransferase 1 inhibitors: enzyme selectivity and cellular activity.. Journal of Medicinal Chemistry, American Chemical Society, 2011, 54 (13), pp.4928-32. ⟨10.1021/jm200453n⟩. ⟨pasteur-00968654⟩

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