A 30-membered piperidine ring-fused aromatic sulfonamide library was synthetized, including N-arylsulfonyl
1,2,3,4-tetrahydroquinolines, 1,2,3,4-tetrahydroisoquinolines and 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indoles. The compounds
induced oxidative stress and glutathione depletion in HT168 melanoma and K562 leukemia cells and in micromolar
concentrations exerted cytotoxic effects. Among the tested sulfonamides, compounds 21, 22, 23, 35 and 41 exhibited
100% cytotoxic effects with low (< 10 µM) EC50 values on K562 cells. The cytotoxicity of lead compound 22 was investigated
in 24 different cancer cell lines, and it was found to be active against leukemia, melanoma, glioblastoma, and liver,
breast and lung cancer cells, as confirmed by classical biochemical and holographic microscopic analyses.