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Evaluation of in vitro Biological Activity of O-Alkylated Hydroxamic Derivatives of Some Nonsteroidal Anti-inflammatory Drugs (CROSBI ID 165438)

Prilog u časopisu | izvorni znanstveni rad | međunarodna recenzija

Kraljević Pavelić, Sandra ; Sedić, Mirela, Poznić, Miroslav ; Rajić, Zrinka ; Zorc, Branka ; Pavelić, Krešimir ; Balzarini, Jan ; Mintas, Mladen Evaluation of in vitro Biological Activity of O-Alkylated Hydroxamic Derivatives of Some Nonsteroidal Anti-inflammatory Drugs // Anticancer Research, 30 (2010), 10; 3987-3994

Podaci o odgovornosti

Kraljević Pavelić, Sandra ; Sedić, Mirela, Poznić, Miroslav ; Rajić, Zrinka ; Zorc, Branka ; Pavelić, Krešimir ; Balzarini, Jan ; Mintas, Mladen

engleski

Evaluation of in vitro Biological Activity of O-Alkylated Hydroxamic Derivatives of Some Nonsteroidal Anti-inflammatory Drugs

Several published studies suggest that nonsteroidal anti-inflammatory drugs (NSAIDs) are promising anticancer agents. This study examined the in vitro effect of O-alkylated NSAID hydroxamic acid derivatives 3a-i on cell survival for a panel of human tumour cell lines, their cytotoxicity on normal human fibroblasts and their antiviral activity. Established methods of cell viability testings, cell cycle analyses and Western blot assays were used. O-alkylated NSAID hydroxamic acid derivatives exerted poor antiviral activity butreduced the viability of the studied tumour cell lines in a concentration-dependent manner showing low cytotoxic effect on normal fibroblasts. The compounds 3a and 3i were shown to be potent inhibitors of the growth of MIA PaCa-2 cell line. They induced p53-independent S-phase arrest and triggered caspase 3-dependent apoptosis. Two novel O-alkylated NSAID hydroxamic acid derivatives may be useful in the treatment of pancreatic cancer and should be further evaluated in vivo.

nonsteroidal anti-inflammatory drugs (NSAID); hydroxamic acids; cytostatic activity; cytotoxicity; human pancreatic cancer; Akt signalling; cell cycle; apoptosis

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Podaci o izdanju

30 (10)

2010.

3987-3994

objavljeno

0250-7005

Povezanost rada

Kemija, Temeljne medicinske znanosti, Biologija

Indeksiranost