Nalazite se na CroRIS probnoj okolini. Ovdje evidentirani podaci neće biti pohranjeni u Informacijskom sustavu znanosti RH. Ako je ovo greška, CroRIS produkcijskoj okolini moguće je pristupi putem poveznice www.croris.hr
izvor podataka: crosbi

Novel 2-Thienyl- and 2-Benzothienyl-Substituted 6-(2-Imidazolinyl)Benzothiazoles: Synthesis ; in vitro Evaluation of Antitumor Effects and Assessment of Mitochondrial Toxicity (CROSBI ID 229128)

Prilog u časopisu | izvorni znanstveni rad | međunarodna recenzija

Racané, Livio ; Sedić, Mirela ; Ilić, Nataša ; Aleksić, Maja ; Kraljević Pavelić, Sandra ; Karminski-Zamola, Grace Novel 2-Thienyl- and 2-Benzothienyl-Substituted 6-(2-Imidazolinyl)Benzothiazoles: Synthesis ; in vitro Evaluation of Antitumor Effects and Assessment of Mitochondrial Toxicity // Anti-Cancer Agents in Medicinal Chemistry, 17 (2017), 1; 57-66. doi: 10.2174/1871520615666160504094753

Podaci o odgovornosti

Racané, Livio ; Sedić, Mirela ; Ilić, Nataša ; Aleksić, Maja ; Kraljević Pavelić, Sandra ; Karminski-Zamola, Grace

engleski

Novel 2-Thienyl- and 2-Benzothienyl-Substituted 6-(2-Imidazolinyl)Benzothiazoles: Synthesis ; in vitro Evaluation of Antitumor Effects and Assessment of Mitochondrial Toxicity

A series of novel cationic 2-thiophene and 2-benzothiophene substituted 6-(2-imidazolinyl)benzothiazole derivatives were prepared and tested for their antiproliferative activity against several human cancer cell lines. An efficient synthesis approach used for the preparation of water soluble mesylate salts 3a-3j of title compounds was achieved by the condensation reaction of 2-amino-5-(2-imidazolinium)benzenethiolate with aldehydes or carbonyl chloride derivatives followed by two simple acid-base reaction steps for their conversion into targeted mesylates. In general, all compounds showed pronounced anticancer activities in vitro. Compound 3f showed strong and selective cytostatic activity in cervical carcinoma cells (HeLa) with moderate toxicity on normal fibroblasts. Similar to all other tested compounds, 3f cannot be considered mitochondrial toxicant. One of the major mechanisms accounting for observed cytostatic effects of 3f was induction of apoptosis, probably due to specific inhibition of acid ceramidase activity. Compound 3h negatively regulated activity of sphingosine kinase 1 in HeLa cells. Thus, design of novel inhibitors targeting enzymes that regulate sphingolipid biosynthesis and turnover could change the landscape for the development of new anticancer drugs.

thieny- ; benzothienyl- ; imidazolinyl- substituted benzothiazoles ; acid ceramidase inhibitor ; sphingosine kinase 1 inhibitor

Rad je finaciran od HRZZ-IP-11-2013-5596. Prvi autor je Livio Racane, koji radi na navedenom projektu.

nije evidentirano

nije evidentirano

nije evidentirano

nije evidentirano

nije evidentirano

Podaci o izdanju

17 (1)

2017.

57-66

objavljeno

1871-5206

10.2174/1871520615666160504094753

Povezanost rada

Kemija, Temeljne medicinske znanosti, Biologija

Poveznice
Indeksiranost