Hydantoin derivatives of L- and D-amino acids: synthesis, antiviral and antitumoral activity evaluations (CROSBI ID 127377)
Prilog u časopisu | izvorni znanstveni rad | međunarodna recenzija
Podaci o odgovornosti
Rajić, Zrinka ; Zorc, Branka ; Raić-Malić, Silvana ; Ester, Katja ; Kralj, Marijeta ; Pavelić, Krešimir ; Balzarini, Jan ; De Clercq, Erik ; Mintas, Mladen
engleski
Hydantoin derivatives of L- and D-amino acids: synthesis, antiviral and antitumoral activity evaluations
3, 5-Disubstituted hydantoin (1, 3-imidazolidinedione) derivatives 5a-h were prepared by base induced cyclization of the corresponding N-(1-benzotriazolecarbonyl)-L- and D-amino acid amides 4a-h. Compounds 5a-h were evaluated for their cytostatic and antiviral activities. Among all the compounds evaluated, 3-benzhydryl-5-isopropyl hydantoin (5a) showed a weak but selective inhibitory effect against vaccinia virus (EC50 = 16 g/mL ; selectivity index: 25). 3-Cyclohexyl-5-phenyl hydantoin (5g) showed inhibitory activity against cervical carcinoma (HeLa, IC50 = 5.4 M) and breast carcinoma (MCF-7, IC50 = 2 M), but also cytotoxic effects towards human normal fibroblasts (WI 38). On the contrary, the 3-benzhydryl-5-phenyl substituted hydantoin derivative 5h showed moderate inhibitory activity towards HeLa, MCF-7, pancreatic carcinoma (MiaPaCa-2), lung carcinoma (H 460) and colon carcinoma (SW 620) (IC50 = 20 23 M), but no effect on WI 38.
Hydantoin ; L- and D-amino acids ; antiviral activity ; antitumoral activity
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Podaci o izdanju
Povezanost rada
Kemija, Temeljne medicinske znanosti, Farmacija