Carboranyl Derivatives of Rofecoxib with Cytostatic Activity against Human Melanoma and Colon Cancer Cells.
2020
Authors:
Buzharevski, AntonioPaskaš, Svetlana
Sárosi, Menyhárt-Botond
Laube, Markus
Lönnecke, Peter
Neumann, Wilma
Murganić, Blagoje
Mijatović, Sanja
Maksimović-Ivanić, Danijela
Pietzsch, Jens
Hey-Hawkins, Evamarie
Document Type:
Article (Published version)
Metadata
Show full item recordAbstract:
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.
Source:
Scientific Reports, 2020, 10, 1, 4827-Funding / projects:
- Molecular mechanisms of physiological and pharmacological control of inflammation and cancer (RS-MESTD-Basic Research (BR or ON)-173013)
- Deutscher Akademischer Austauschdienst
- DFG (HE 1376/38-1; SA 2902/2-1)
- Graduate School BuildMoNa
DOI: 10.1038/s41598-020-59059-3
ISSN: 2045-2322
PubMed: 32179835
WoS: 000562126100001
Scopus: 2-s2.0-85081989889
URI
http://www.ncbi.nlm.nih.gov/pubmed/32179835http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=PMC7076013
https://radar.ibiss.bg.ac.rs/handle/123456789/3640