Naslov
Synthesis and anti-proliferative activity of novel amidino-substituted aryl-bisbenzothiazoles
(Sinteza i antiproliferativna aktivnost novih amidino-supstituiranih arilnih bisbenzotiazola)

Autori
Ptiček, Lucija ; Mudrešić, Marija ; Grbčić, Petra ; Kraljević Pavelić, Sandra ; Racane, Livio

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

Izvornik
26th Croatian Meeting of Chemists and Chemical Engineers, Book of Abstracts, N. Galić i M. Rogošić (ur.), Zagreb HKD/HDKI 2019. / - , 2019, 113-113

Skup
26. hrvatski skup kemičara i kemijskih inženjera (26HSKIKI) ; 4. simpozij Vladimir Prelog

Mjesto i datum
Šibenik, Hrvatska, 09.04.2019. - 12.04.2019

Vrsta sudjelovanja
Poster

Vrsta recenzije
Domaća recenzija

Ključne riječi
synthesis, amidino-substituted benzothiazoles, anti-proliferative activity

Sažetak
2-Arylbenzothiazole derivatives are of considerable interest due to their diverse pharmaceutical properties and have emerged as a privileged scaffold in drug discovery bearing remarkable activity profiles in non-invasive diagnosis of Alzheimer's disease and antitumour effects. Strong anti-proliferative effects on some tumour cell lines were previously shown for isomeric imidazolinyl-substituted phenylene-bisbenzothiazole, and imidazolinyl- substituted phenyl- and naphtyl-benzothiazoles. These findings have led us to further investigate this class of compounds by introducing different types of amidinic substituents with the aim of improving activity and selectivity on different human tumour cell lines. Additionally, we explored reaction conditions for sustainable approach to synthesis of amidino-substituted phenylene- bisbenzothyazoles by condensation reaction from the corresponding bis(2-aminophenyl) disulfide and aldehyde using glycerol as a green solvent. We found new efficient and sustainable synthetic method for preparation of isomeric amidino-substituted derivatives of bisbenzothiazolyl-phenylenes and naphtalenes. Generally, the in vitro anti-proliferative screening of novel diamidino-bisbenzothiazolyl derivatives revealed strong activity on tested tumour cell lines (SW620, HepG2, CFPAC-1 and HeLa) depending on the type of amidinic substituent as well as positions of benzothiazolyl moieties.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Biotehnologija u biomedicini (prirodno područje, biomedicina i zdravstvo, biotehničko područje)

POVEZANOST RADA