Virtual fragment screening identification of a novel Quinoline-5,8-dicarboxylic acid derivative as selective JMJD3 inhibitor.
Giordano A., Del Gaudio F., Johansson C., Riccio R., Oppermann U., Di Micco S.
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.