| Summary: | A series of novel quinoline-based tetracyclic ring-systems were synthesized and evaluated in vitro for their antiplasmodial, antiproliferative and antimicrobial activities. The novel hydroiodide salts <b>10</b> and <b>21</b> showed the most promising antiplasmodial inhibition, with compound <b>10</b> displaying higher selectivity than the employed standards. The antiproliferative assay revealed novel pyridophenanthridine <b>4b</b> to be significantly more active against human prostate cancer (IC<sub>50</sub> = 24 nM) than Puromycin (IC<sub>50</sub> = 270 nM) and Doxorubicin (IC<sub>50</sub> = 830 nM), which are used for clinical treatment. Pyridocarbazoles <b>9</b> was also moderately effective against all the employed cancer cell lines and moreover showed excellent biofilm inhibition (<b>9a</b>: MBIC = 100 µM; <b>9b</b>: MBIC = 100 µM).
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