Naslov
Novi 5-amidinobenzimazoli kao selektivni agensi protiv karcinoma pluća
(Novel 5-amidino benzimazoles as selective cytostatic agents against lung cancer cells)

Autori
Bistrović, Andrea ; Krstulović, Luka ; Grbčić, Petra ; Harej, Anja ; Sedić, Mirela ; Kraljević Pavelić, Sandra ; Bajić, Miroslav ; Raić-Malić, Silvana

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

Izvornik
25th Meeting of Croatian Chemists and Chemical Engineers : Book of abstracts / Ana Šantić, Marijana Đaković - Zagreb : Hrvatsko kemijsko društvo, 2017, 190-190

Skup
25th Meeting of Croatian Chemists and Chemical Engineers

Mjesto i datum
Poreč, Hrvatska, 19.04.2017. - 22.04.2017

Vrsta sudjelovanja
Poster

Vrsta recenzije
Nije recenziran

Ključne riječi
amidinobenzimidazoli ; 1, 2, 3-triazoli ; karcinom pluća ; p38MAPK
(amidino benzimidazoles ; 1, 2, 3-triazoles ; lung carcinoma ; p38MAPK)

Sažetak
Lung cancer is one of the most common malignant tumors in the world. Dysregulation of p38 mitogenactivated protein kinase (MAPK) levels in patients are associated with advanced stages and short survival in cancer patients (e.g., prostate, breast, bladder, liver, and lung cancer) [1]. The benzimidazole derivatives have shown various biological activities such as anticancer, antimicrobial, antivirus, anti- inflammatory and antioxidant [2]. Moreover, the amidino moiety is among the strongest neutral bases with high proton affinity and has therefore found wide application in biologically active compounds [3]. We designed and synthesized novel 1, 2, 3-triazolyl linked 5- amidino benzimidazoles (Figure 1) in order to evaluate their cytostatic activities. Environmentally benign synthetic protocols using microwave- and ultrasound irradiation were used to prepare 1, 4- disubstituted-1, 2, 3-triazoles, as key precursors in the synthesis of novel 5-amidino benzimidazoles. Some representatives have shown selective inhibitory effects against non-small lung carcinoma (A-549) and cervical carcinoma (HeLa). Further biological evaluations of the most selective compounds indicated their mechanism of action via the p38 MAP kinase pathway.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Biologija

POVEZANOST RADA