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Substituted 1-methyl-4-phenylpyrrolidin-2-ones - Fragment-based design of N-methylpyrrolidone-derived bromodomain inhibitors.

European journal of medicinal chemistry (2020-03-03)
J P Hilton-Proctor, O Ilyichova, Z Zheng, I G Jennings, R W Johnstone, J Shortt, S J Mountford, M J Scanlon, P E Thompson
RESUMEN

N-Methylpyrrolidone is one of several chemotypes that have been described as a mimetic of acetyl-lysine in the development of bromodomain inhibitors. In this paper, we describe the synthesis of a 4-phenyl substituted analogue - 1-methyl-4-phenylpyrrolidin-2-one - and the use of aryl substitution reactions as a divergent route for derivatives. Ultimately, this has led to structurally complex, chiral compounds with progressively improved affinity as inhibitors of bromodomain-containing protein 4.

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SAFC
Carbonato de calcio, precipitated (≤ 0.0001% Al), EMPROVE® ESSENTIAL, Ph. Eur., BP, JP, USP, FCC, E 170