Carboranyl Derivatives of Rofecoxib with Cytostatic Activity Against Human Melanoma and Colon Cancer Cells
| Autor: | 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 |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2020 |
| Předmět: |
Boron Compounds
Carcinogenesis lcsh:Medicine Antineoplastic Agents Drug development rofecoxib Article Lactones carborane Cell Line Tumor Humans cancer Sulfones lcsh:Science Melanoma Cyclooxygenase 2 Inhibitors lcsh:R cytostatic drugs NO-releasing drug Cyclooxygenase 2 Drug Design Colonic Neoplasms lcsh:Q Structure-based drug design Hydrophobic and Hydrophilic Interactions Diversity-oriented synthesis |
| Zdroj: | Scientific Reports 10(2020), 4827 Scientific Reports Scientific Reports, Vol 10, Iss 1, Pp 1-13 (2020) |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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