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.
Virtual fragment screening identification of a novel Quinoline-5,8- dicarboxylic acid derivative as selective JMJD3 inhibitor
Assunta Giordano;
2018
Abstract
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.File in questo prodotto:
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