N-Cyano Sulfoximines: COX Inhibition, Anticancer Activity, Cellular Toxicity, and Mutagenicity

• Published in: ChemMedChem Vol. 8; no. 2; pp. 217 - 220
• Main Authors: Park, Seong Jun, Baars, Hannah, Mersmann, Stefanie, Buschmann, Helmut, Baron, Jens Malte, Amann, Philipp M., Czaja, Katharina, Hollert, Henner, Bluhm, Kerstin, Redelstein, Regine, Bolm, Carsten
• Format: Journal Article
• Language: English
• Published: Weinheim WILEY-VCH Verlag 01-02-2013; WILEY‐VCH Verlag; Wiley Subscription Services, Inc
• Subjects: Animals; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Antineoplastic Agents - toxicity; Antitumor activity; cancer; Cell Line; Cell Line, Tumor; Cell Proliferation - drug effects; Cyclooxygenase Inhibitors - chemistry; Cyclooxygenase Inhibitors - pharmacology; Cyclooxygenase Inhibitors - toxicity; cyclooxygenases; cytotoxicity; Humans; inhibitors; Insecta; N-cyano sulfoximines; Neoplasms - drug therapy; Neoplasms - enzymology; Nitriles - chemistry; Nitriles - pharmacology; Prostaglandin-Endoperoxide Synthases - metabolism; Sulfur Compounds - chemistry; Sulfur Compounds - pharmacology
• ISSN: 1860-7179; 1860-7187
• DOI: 10.1002/cmdc.201200403

From insects to cancer: N‐Cyano sulfoximines were evaluated for COX inhibition and antiproliferative activity against a panel of cancer cell lines. The most active compound exhibited potent COX‐2 inhibition, some selectivity for COX‐2 over COX‐1, only slight cytotoxicity towards healthy cells (HaCaT skin cells), and no mutagenic potential (as determined by an Ames assay).