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Carboranyl Derivatives of Rofecoxib with Cytostatic Activity Against Human Melanoma and Colon Cancer Cells

Buzharevski, A.; Paskas, S.; Sárosi, M.-B.; Laube, M.; Lönnecke, P.; Neumann, W.; Murganić, B.; Mijatović, S.; Maksimović-Ivanić, D.; Pietzsch, J.; Hey-Hawkins, E.
Due to the involvement of cyclooxygenase-2 (COX-2) in carcinogenesis, COX-2-selective inhibitors are increasingly studied for their potential cytotoxic properties. Moreover, the incorporation of carboranes in structures of established anti-inflammatory drugs can improve the potency and metabolic stability of the inhibitors. Herein, we report the synthesis of carborane-containing derivatives of rofecoxib that display remarkable cytostatic activity in the micromolar range with excellent selectivity for melanoma and colon cancer cell lines over normal cells. Furthermore, it was shown that the carborane-modified derivatives of rofecoxib displayed different modes of action that was dependent on the cell type.
Keywords: cancer, rofecoxib, carborane, cytostatic drugs, NO-releasing drug

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Permalink: https://www.hzdr.de/publications/Publ-30682
Publ.-Id: 30682