Cytotoxic, Antibacterial, and in Silico Pks13 Inhibitory Properties of Indole‐Coupled Dihydrobenzo[c]phenanthridines

The indoles and benzo[c]phenanthridines have attracted much interest as potential anticancer and antibacterial agents. Herein, the synthesis and bioactivity of new and known indole‐coupled dihydrobenzo[c]phenanthridines are reported. Among the investigated compounds, 2j displays potent and selective activity against drug‐resistant Staphylococcus aureus , S. epidermidis , and Enterococcus faecium strains. In addition, 1a‐c and 2a specifically target the multidrug‐resistant Mycobacterium tuberculosis G122, possibly by inhibiting the Pks13 enzyme, as deduced from the in silico analyses. Additionally, compound 1g is more potent than cisplatin against MCF‐7 (breast) and PC‐3 (prostate) human cancer cell lines, whereas 2b is found to be almost as active as cisplatin against PC‐3 and SW‐480 (colorectal) cell lines. Compounds 1a and 1g display remarkable selectivity index values, thus being promising antibacterial and anticancer hits.