Naslov
Anti-proliferative effects of novel hybrids of 1, 2, 3-triazole-pyrimidines, 1, 2, 3–triazole–benzimidazoles and 1, 2, 3-triazole-coumarins

Autori
Tomljenović Paravić, Andrea ; Kraljević Pavelić, Sandra ; Raić Malić, Silvana ; Sedić, Mirela

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

Izvornik
11th Central European Oncology Congress, Croatian Society of Oncology’s Best of ASCO® Conference : abstracts / - , 2015

Skup
Central European Oncology Congress, Croatian Society of Oncology’s Best of ASCO® Conference (11 ; 2015)

Mjesto i datum
Opatija, Hrvatska, 17.06.2015. - 20.06.2015

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
1; 2; 3-triazole-pyrimidines; 1; 2; 3-triazole-coumarins and 1; 2; 3-triazole benzimidazoles; human cancer cell lines

Sažetak
The series of novel hybrids including: 1, 2, 3-triazole-pyrimidines, 1, 2, 3-triazole-coumarins and 1, 2, 3-triazole benzimidazoles were evaluated for their anti-proliferative activity against five human cancer cell lines and normal embryo mouse fibroblasts. Among these, TG-16 (C16H12ClN5 ; IC50=4, 83µM), TG-14 (C22H15BrF2N8O2 ; IC50=4, 53µM) and TG-15 (C22H15BrCl2N8O2 ; IC50=1µM) exerted the most potent cytostatic activity in lung, pancreatic and hepatocellular carcinoma cell lines, respectively. Interestingly, the most selective anticancer effects were observed with compounds MM-11(C17H14FN5) and MM-19 (C17H14FN5) in lung carcinoma cells with IC50=4, 78 µM and IC50=7, 79 µM, respectively. Additional in vitro toxicity studies revealed mitochondrial impairment as a primary mechanism accounting for observed cytotoxic effects of TG-16, MM-11 and MM-19. The latter also showed strong in vitro renal toxicity.

Izvorni jezik
Engleski

Znanstvena područja
Temeljne medicinske znanosti

POVEZANOST RADA