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

Donghang Cheng; Sergio Valente; Sabrina Castellano; Gianluca Sbardella; Roberto Di Santo; Roberta Costi; Mark T Bedford; Antonello Mai

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.

Document type :

Journal articles

Domain :

Life Sciences [q-bio] / Pharmaceutical sciences

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

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