Pregled bibliografske jedinice broj: 984632
Synthesis of New Acyclic Pyrimidine Nucleoside Analogues and Preliminary of Their Cytotoxic and Genotoxic Effects In Vitro
Synthesis of New Acyclic Pyrimidine Nucleoside Analogues and Preliminary of Their Cytotoxic and Genotoxic Effects In Vitro // Research journal of pharmaceutical, biological and chemical sciences, 10 (2019), 1; 493-502 (međunarodna recenzija, članak, znanstveni)
CROSBI ID: 984632 Za ispravke kontaktirajte CROSBI podršku putem web obrasca
Naslov
Synthesis of New Acyclic Pyrimidine Nucleoside
Analogues and Preliminary of Their Cytotoxic
and Genotoxic Effects In Vitro
Autori
Osmanović, Amar ; Salihović, Mirsada ; Kopjar, Nevenka ; Želježić, Davor ; Roca, Sunčica ; Špirtović-Halilović, Selma ; Šapčanin, Aida ; Završnik, Davorka
Izvornik
Research journal of pharmaceutical, biological and chemical sciences (0975-8585) 10
(2019), 1;
493-502
Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni
Ključne riječi
Pyrimidine analogues ; Acyclic nucleosides ; CBMN assay ; Genotoxicity ; Cytotoxicity
Sažetak
Nucleoside analogues represent an important class of compounds of wide application range in antiviral and antitumor therapy. A regular procedure in early phases of new drugs development includes assessment of cytotoxicity and genotoxicity (mutagenicity). Here we report the synthesis of two novel C-5 hydroxypropyl pyrimidine nucleosides bearing side chains like those present in drugs already used in therapy (penciclovir and cidofovir). To confirm structures of the newly synthesized compounds FT-IR, HPLC-MS and NMR spectroscopy in solution were used. New hydroxypropyl pyrimidine nucleosides were N-3-(2, 3-dihydroxypropyl)-5- (3-hydroxypropyl)pyrimidine-2, 4-dione and N-3- (4-hydroxy-3-(hydroxymethyl)butyl)-5-(3- hydroxypropyl)pyrimidine-2, 4-dione.Along with two new, we have also tested three previously synthesized nucleosides for genotoxicity and cytotoxicity using cytokinesis-block micronucleus (CBMN) assay on human peripheral blood lymphocytes. Not many studies so far used the same cell model and CBMN assay to determine cyto-/genotoxicity of pyrimidine nucleosides. Results of CBMN assay did not indicate statistically significant cyto-/genotoxicity towards human peripheral blood lymphocytes. Since preliminary testing did not suggest significant genotoxic or cytotoxic potency of novel hydroxypropyl pyrimidine nucleosides, they are excellent candidates for further biological evaluation, primarily as antiviral agents.
Izvorni jezik
Engleski
Znanstvena područja
Kemija
POVEZANOST RADA
Ustanove:
Institut za medicinska istraživanja i medicinu rada, Zagreb,
Institut "Ruđer Bošković", Zagreb