期刊
ACS OMEGA
卷 4, 期 5, 页码 8824-8833出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsomega.9b00412
关键词
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资金
- Deutscher Akademischer Austauschdienst (DAAD)
- DFG [HE 1376/38-1]
- Graduate School BuildMoNa
- Ministry of Education, Science and Technological Development of the Republic of Serbia [173013]
- German Research Foundation (DFG)
- Leipzig University within the program of Open Access Publishing
Ketoprofen is a widely used nonsteroidal anti-inflammatory drug (NSAID) that also exhibits cytotoxic activity against various cancers. This makes ketoprofen an attractive structural lead for the development of new NSAIDs and cytotoxic agents. Recently, the incorporation of carboranes as phenyl mimetics in structures of established drugs has emerged as an attractive strategy in drug design. Herein, we report the synthesis and evaluation of four novel carborane-containing derivatives of ketoprofen, two of which are prodrug esters with an nitric oxide-releasing moiety. One of these prodrug esters exhibited high cytostatic activity against melanoma and colon cancer cell lines. The most pronounced activity was found in cell lines that are sensitive to oxidative stress, which was apparently induced by the ketoprofen analogue.
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