Carboranyl Analogues of Celecoxib with Potent Cytostatic Activity against Human Melanoma and Colon Cancer Cell Lines.
2019
Аутори:
Buzharevski, AntonioPaskas, Svetlana
Sárosi, Menyhárt‐Botond
Laube, Markus
Lönnecke, Peter
Neumann, Wilma
Mijatović, Sanja
Maksimović-Ivanić, Danijela
Pietzsch, Jens
Hey-Hawkins, Evamarie
Тип документа:
Чланак у часопису (Објављена верзија)
,
© 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim
Метаподаци
Приказ свих података о документуАпстракт:
Nonsteroidal anti-inflammatory drugs (NSAIDs) are the most common way of treating inflammatory disorders. Their widespread use helped reveal their other modes of action as pharmaceuticals, such as a profound effect on various cancers. Celecoxib has proven to be a very prominent member of this group with cytostatic activities. On the other hand, the highly dynamic field of drug design is constantly searching for new ways of modifying known structures to obtain more powerful and less harmful drugs. A very interesting development is the implementation of carboranes in pharmacologically active structures, mostly as phenyl mimetics. Herein we report the synthesis of three carborane-containing derivatives of the COX-2-selective NSAID celecoxib. The new compounds proved to have promising cytostatic potential against various melanoma and colorectal adenocarcinoma cell lines. Inhibited proliferation accompanied by caspase-independent apoptotic cell death was found to be the main cause of decreased cell viability upon treatment with the most efficient celecoxib analogue, 3 b (4-[5-(1,7-dicarba-closo-dodecaboranyl)-3-trifluoromethyl-1H-pyrazol-1-yl]-1-methylsulfonylbenzene).
Кључне речи:
Cancer; Carboranes; Celecoxib; Cytotoxicity; Drug discoveryИзвор:
ChemMedChem, 2019, 14, 3, 315-321Финансирање / пројекти:
- Молекуларни механизми физиолошке и фармаколошке контроле инфламације и канцера (RS-MESTD-Basic Research (BR or ON)-173013)
- Deutscher Akademischer Austauschdienst
- Deutsche Forschungsgemeinschaft. Grant Numbers: He 1376/38-1, SA 2902/2-1
DOI: 10.1002/cmdc.201800685
PubMed: 30602073
WoS: 000458432600004
Scopus: 2-s2.0-85060592983
URI
https://onlinelibrary.wiley.com/doi/abs/10.1002/cmdc.201800685https://radar.ibiss.bg.ac.rs/handle/123456789/3254