Synthesis and Cytotoxic Activity Study of Novel 2-(Aryldiazenyl)-3-methyl-1H-benzo[g]indole Derivatives

A novel series of 2-(aryldiazenyl)-3-methyl-1H-benzo[g]indole derivatives (3a-f) were prepared through the cyclization of the corresponding arylamidrazones, employing polyphosphoric acid (PPA) as a cyclizing agent. All of the compounds (3a-f) were characterized using H-1 NMR, C-13 NMR, MS, elemental analysis, and melting point techniques. The synthesized compounds were evaluated for cytotoxic activity against diverse human cancer cell lines by the National Cancer Institute. While all of the screened compounds were found to be cytotoxic at a 10 mu M concentration, two of them (2c) and (3c) were subjected to five dose screens and showed a significant cytotoxicity and selectivity.

Automated summary

A novel series of 2-(aryldiazenyl)-3-methyl-1H-benzo[g]indole derivatives were synthesized using polyphosphoric acid as a cyclizing agent. The compounds were characterized and evaluated for cytotoxic activity, with two of them showing significant cytotoxicity and selectivity after dose screening.