Naslov
Synthesis and biological evaluation of novel 2- (hetero)aryl-6-(2-imidazolinyl)benzothiazoles as anticancer agents

Autori
Racané, Livio ; Ptiček, Lucija ; Sedić, Mirela ; Grbčić, Petra ; Kraljević Pavelić, Sandra ; Sović, Irena ; Karminski-Zamola, Grace

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

Izvornik
The 10th Joint Meeting on Medicinal Chemistry 2017 - Book of abstracts / Basarić, N. ; Namjesnik, D. ; Perković, I. ; Stepanić, V. - Zagreb : Hrvatsko knjižničarsko društvo, 2017, 204-204

ISBN
978-953-55232-8-4

Skup
The 10th Joint Meeting on Medicinal Chemistry 2017

Mjesto i datum
Srebreno, Hrvatska; Dubrovnik, Hrvatska, 25.06.2017. - 28.06.2017

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
benzothiazoles ; synthesis ; anticancer agents

Sažetak
Benzothiazole as an important pharmacophore, has recently emerged as a privileged scaffold in drug discovery due to a variety of pharmacological properties, and its derivatives offer a high degree of structural diversity that has proven useful for the search of new therapeutic agents.Through last decade, our scientific focus has been placed on this particular series of heterocyclic compounds, with an emphasis on their synthesis, study of anticancer activities and DNA binding properties. Recently, we efficiently synthesized a series of 2-thienyl- and 2- benzothienyl-substituted 6-(2- imidazolinyl)benzothiazole derivatives, investigated their antitumor effects and explored the possible involvement of key enzymes regulating sphingolipid metabolism. We have found in this group of sulphur-containing heterocycles the 2-benzothienyl derivative to have remarkable and selective cytostatic activity. One of the major mechanisms accounting for observed cytostatic effects was induction of apoptosis, probably due to specific inhibition of acid ceramidase activity. Based on these results a novel series of title compounds are synthesized and evaluated for their potential as anticancer agents. An efficient synthesis is achieved by the condensation reaction of 2-amino-5-(2- imidazolinium)benzenethiolate with the corresponding aldehydes or carboxylic acid and compounds were isolated as monocationic highly water soluble mesylates. The in vitro antiproliferative activity against several human cancer cell lines is tested.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Biologija

POVEZANOST RADA