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Compounds and methods for inhibiting histone demethylases: a patent evaluation of US20160102096A1

2016; Taylor & Francis; Volume: 26; Issue: 12 Linguagem: Inglês

10.1080/13543776.2016.1246539

1744-7674

Florian Thaler, Ciro Mercurio,

RNA modifications and cancer

The Jumonji C (JmjC) domain containing histone lysine demethylases have a clear role both in the development and in some diseases including inflammation and cancer. The histone lysine demethylases represent an attractive target for the identification of therapeutic agents and the pyridine derivatives are a scaffolds largely investigated for the identification and development of inhibitors of enzymes of the Jumonji family. This commentary is a scientific evaluation of a patent application US20160102096A1 that describes novel pyridine derivatives in which the introduction of specific substituents is used to modulate the selectivity profile of the inhibitors.