Synthesis and docking study for compounds analogs of LSD1 inhibitor.

LSD1 is an important target for cancer treatment. In this work based on hit, we performed synthesis of Scaffold and docking (GOLDv5.2 program) to analyze 10 proposed analogues, in order to evaluate the behavior in the target / for lsd1 inhibitors.
For the synthesis procedure we obtained 2-oxo-1,2-dihydroquinoline-6-sulfonyl chloride and used amino acid L-phenylalanine by nucleophilic amine substitution in order to obtain the sulfonamide.
All synthesized compounds were duly evaluated and characterized. As a result of the synthesis reactions we obtained 85% and 71% of yield respectively in each reaction. The sulfonamide will react with heterocyclic derivatives by coupling reaction.
The 10 analogs evaluated from screening showed a higher score than the hit by docking. Thus, we suggest that the synthetic methodology was effective and the compounds will be evaluated for biological activity and the results by dockings studies suggest an inhibitory activity over LSD1.