Naslov
Synthesis and biological activity of bis-6-amidino- benzazoles linked through aliphatic unit

Autori
Ptiček, Lucija ; Grbčić, Petra ; Kraljević Pavelić, Sandra ; Taylor, Martin C. ; Kelly, John M. ; Raić- Malić, Silvana ; Racané, Livio

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

Izvornik
27th Croatian Meeting of Chemists and Chemical Engineers, Book of Abstracts / Marković, Dean ; Meštrović, Ernest ; Namjesnik, Danijel ; Tomašić, Vesna - Zagreb : Hrvatsko kemijsko društvo, 2021, 158-158

Skup
27. hrvatski skup kemičara i kemijskih inženjera (27HSKIKI)

Mjesto i datum
Veli Lošinj, Hrvatska, 05.10.2021. - 08.10.2021

Vrsta sudjelovanja
Poster

Vrsta recenzije
Domaća recenzija

Ključne riječi
synthesis, amidine, benzazoles, antiproliferative activity, antitrypanosomal activity

Sažetak
Cationic amidine drivatives have been well established as potent antiparasitic and antitumor compounds. Our recent results of biological evaluation of amidino-substituted 2-arylbenzazole derivatives revealed strong and selective antiproliferative [1a, b] as well as antitrypanosomal activities [1c]. Newly designed and synthesized series of dicationic bis-6- amidinobenzazole derivatives linked with the aliphatic moiety were prepared by our previously developed method [1b] and have been evaluated in vitro against four human tumor cell lines and protozoan parasite Trypanosoma brucei. Compounds with imidazolinyl amidine showed activity on colorectal adenocarcinoma (SW620) with IC50 = 0.2- 9.7 µM, while unsubstituted amidines exhibited pronounced antitrypanosomal potency with IC50 = 0.51-890 nM.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Biologija

POVEZANOST RADA