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The quinoline-5,8 dicarboxylic acid scaffold has been identified by fragment-based approach as new potential lead compound for the development of JMJD3 inhibitors. Among them, compound 3 shows low micromolar inhibitory activity against JMJD3. The experimental evaluation of inhibition activity vs. related seven isoforms of JMJD3 highlighted an unprecedented selectivity towards the biological target of interest.

Original publication

DOI

10.1002/cmdc.201800198

Type

Journal article

Journal

ChemMedChem

Publication Date

06/04/2018

Addresses

ITALY.