Naslov
Synthesis, crystal structure and antiproliferative evaluation of some new substituted benzothiazoles and styrlbenzothiazoles

Autori
Ćaleta, Irena ; Grdiša, Mira ; Mrvoš-Sermek, Draginja ; Cetina, Mario ; Tralić-Kulenović, Vesna ; Pavelić, Krešimir ; Karminski-Zamola, Grace

Izvornik
Il Farmaco (Pavia) (0014-827X) 59 (2004), 4; 297-305

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
aminodibenzothiazoles ; aminostyrylbenzothiazoles ; X-ray crystal structure analysis ; antitumor activity ; cell lines

Sažetak
The multistep synthesis of a series of new substituted-benzothiazoles as hydrochloride or quaternary salts is described. 6-Amidino substituted 2-aminobenzothiazoles (5, 6), N-methyl-2-(4-cyanostyryl)benzothiazolium iodide (8), cyano-substituted-2-styrylbenzothiazoles (9-11) and amidino and bis-amidino-substituted 2-styrylbenzothiazoles (12-17) were prepared. The crystal structure of amidino derivative (6) was determined by single crystal X-ray analysis. All new prepared compounds were tested on the cytostatic activities against malignant cell lines: (SW620, colon carcinoma ; Hep2, laryngeal carcinoma ; HBL, melanoma ; HeLa, cervical carcinoma and WI38, human normal fibroblasts). The compounds exerted a different inhibitory effect, depended on concentration and type of the cells. The best inhibitory effect was achieved with compounds (12-15), with slight differences among them. All of them inhibited the growth of examined tumor cell lines and also normal fibroblasts. Other examined compounds exhibited a moderate inhibitory effect, depending on type of the cells. Majority of them inhibited the growth of HeLa cells and WI38.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Temeljne medicinske znanosti

POVEZANOST RADA