9Th Brazilian Symposium on Medicinal Chemistry

Marinoquinolines represent a new class of natural and unnatural compounds containing the uncommon 3H-pyrrolo[2,3-c]quinoline scaffold which has rarely been studied. In 2012, our research group reported the total synthesis of the natural marinoquinolines A, B, C and E, and this synthetic procedure allowed the synthesis of new unnatural derivatives. In light of these results, we have been working on the synthesis of new analogues in order to set up a small library of compounds and exploit the medicinal potencial of the marinoquinoline class, specifically for cancer. A HTS-compatible assay for HaCat and HCT-116 cell lines was performed and a hit compounds was selected, with high potency (3.1 ± 0.5 μM) and selectivity (>100 μM). A second part of the study was trying to doing some molecular modifications in order to improve potency of this compound.