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Owing 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 cytotoxic or 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 showed different modes of action that were dependent on the cell type.


Antonio Buzharevski, Svetlana Paskaš, Menyhárt-Botond Sárosi, Markus Laube, Peter Lönnecke, Wilma Neumann, Blagoje Murganić, Sanja Mijatović, Danijelа Maksimović-Ivanić, Jens Pietzsch, Evamarie Hey-Hawkins. Carboranyl Derivatives of Rofecoxib with Cytostatic Activity against Human Melanoma and Colon Cancer Cells. Scientific reports. 2020 Mar 16;10(1):4827

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PMID: 32179835

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