Aromatic Sulfonamides Containing a Condensed Piperidine Moiety as Potential Oxidative Stress-Inducing Anticancer Agents

Title:Aromatic Sulfonamides Containing a Condensed Piperidine Moiety as Potential Oxidative Stress-Inducing Anticancer Agents

Volume: 9 Issue: 7

Author(s): Ramóna Madácsi, Iván Kanizsai, Liliána Z. Fehér, Márió Gyuris, Béla Ózsvári, András Erdélyi, János Wölfling and László G. Puskás

Affiliation:

Keywords: Sulfonamide, tetrahydroquinoline, tetrahydroisoquinoline, tetrahydropyridoindle, anticancer agent, oxidative stress.

Abstract: 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.

Cite this article as:

Madácsi Ramóna, Kanizsai Iván, Fehér Z. Liliána, Gyuris Márió, Ózsvári Béla, Erdélyi András, Wölfling János and Puskás G. László, Aromatic Sulfonamides Containing a Condensed Piperidine Moiety as Potential Oxidative Stress-Inducing Anticancer Agents, Medicinal Chemistry 2013; 9 (7) . https://dx.doi.org/10.2174/1573406411309070004