Both substituted indoles/indazoles and substituted quinolones are found in numerous biologically active compounds. A large number of these indole/indazole/quinolone sub-unit containing compounds have been found to have anticancer and/or antibiotic and/or antimicrobial activity. With this in mind, we set out to develop a research project with the overriding goal of exploring the anticancer/antibiotic/antimicrobial activity of compounds that contained both the indole/indazole and quinolone sub-units. Each individual, early stage sub-project would focus on the synthesis of analogues that varied in the sub-unit connectivity between indole/indazole and quinolone. Within each separate early stage sub-project, there would be an initial focus on the synthesis of a handful of analogues that shared the same indole/indazole and quinolone sub-unit connectivity. Our specific early stage sub-project focused on synthesizing a handful of indole-quinolone and indazole-quinolone analogues where the sub-unit connectivity was located at the N1 of the indole/indazole sub-unit and the C6 of the quinolone sub-unit. We successfully synthesized a handful of analogues with this specific N1-C6 sub-unit connectivity and have passed each of them on to our collaboration partners (Dr. Venkatram Mereddy Research Group) for in vitro biological studies testing the anticancer/antibiotic/antimicrobial activity of each compound. Our collaboration partners have conducted and will continue to conduct these in vitro biological studies on all early stage synthetic analogues produced by our research group (Dr. Timothy M. Trygstad Research Group). Based on the data provided by the biological studies of numerous early stage synthetic sub-projects with analogue series that focus on variations in indole/indazole and quinolone sub-unit connectivity, future Trygstad Research Group members will then prioritize their efforts on synthetic and anticancer/antibiotic/antimicrobial activity optimization on any early stage analogue series that shows good potential as an anticancer/antibiotic/antimicrobial agent.

Synthesis of indolyl/indazolyl (N1 substituted) quinolones (C6 substituted) for study as possible anticancer/antibiotic/antimicrobial agents

251st National Meeting (2016)

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