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

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

Journal Name: Medicinal Chemistry

Volume 9 , Issue 7 , 2013

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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.

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

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Article Details

Year: 2013
Published on: 31 July, 2013
Page: [911 - 919]
Pages: 9
DOI: 10.2174/1573406411309070004
Price: $65

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