Naslov
Novel NSAID semicarbazide derivatives as potential anticancer and anti-inflammatory drugs

Autori
Perković, Ivana ; Butula, Ivan ; Zorc, Branka

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
Pharmaceutical Sciences for the Future of Medicines / - , 2011, 70-70

Skup
3rd PharmSciFair

Mjesto i datum
Prag, Češka Republika, 13.06.2011. - 17.06.2011

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
NSAID; semicarbazide

Sažetak
Non-steroidal anti-inflammatory drugs (NSAIDs) are widley used because of their pronounced analgesic, antipiretic and antiinflammatory properties. However, the presence of carboxylic acid moiety and their non-selective action on COX1/COX2 often induce gastrointestinal side-effects, specially after prolonged use. Numerous derivatives were prepared ; some of them showed not only increased analgesic activity, but also dual COX and LOX inhibition, and therefore increased antiinflammatory efficacy and supressed toxicity. NSAIDs are potential anticancer drugs also. On the other hand, various semicarbazides have exerted antitumour activity in vitro. Thus, we set to prepare a series of NSAID (ibuprofen, fenoprofen and reduced ketoprofen) derivatives bearing semicarbazide moiety and to test their antitumour and LOX inhibition activities. NSAID benzotriazolides, were used for the synthesis of NSAID hydrazides. In the second step, NSAID hydrazides reacted with active ureas (1-carbamoylbenzotriazoles, BtcNHR) bearing various alkyls/aryls (R = cyclopentyl, cyclohexyl, cyclohexylmethyl, benzyl, phenylethyl, benzhydryl) in the presence of triethylamine and gave the corresponding semicarbazide derivatives. Structures of the new semicarbazides were deduced from analysis of their IR, 1H and 13C NMR spectra. The evaluation of their pharmacological activity is in progress.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Farmacija

POVEZANOST RADA