title: Synthesis and biological activity of some new 5'-O-acyl tiazofurin derivatives.
abstract: Three new 5'-O-acyl tiazofurin derivatives 2-4 were synthesized and evaluated for their antiproliferative activity against different tumour cell lines as well as for their ability to induce apoptosis in C6 cells in vitro. Apart of the antitumour assays, the cell membrane permeation of 2-4 and their intracellular metabolism in C6 cells in vitro was also studied in order to evaluate their potential as possible tiazofurin bioisosteres or prodrugs.
authors.affiliation: Department of Chemistry, Faculty of Sciences, University of Novi Sad, Serbia & Montenegro. vpejanovic@hemofarm.co.yu
authors.forename: Vjera
authors.initials: V
authors.lastname: Pejanović
authors.forename: Vesna
authors.initials: V
authors.lastname: Piperski
authors.forename: Dragana
authors.initials: D
authors.lastname: Ugljesić-Kilibarda
authors.forename: Jelena
authors.initials: J
authors.lastname: Tasić
authors.forename: Mirjana
authors.initials: M
authors.lastname: Dacević
authors.forename: Ljubica
authors.initials: L
authors.lastname: Medić-Mijacević
authors.forename: Esmir
authors.initials: E
authors.lastname: Gunić
authors.forename: Mirjana
authors.initials: M
authors.lastname: Popsavin
authors.forename: Velimir
authors.initials: V
authors.lastname: Popsavin
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002455:Cell Division / Q000187:drug effects; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004273:DNA, Neoplasm / Q000096:biosynthesis / Q000235:genetics; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020287:In Situ Nick-End Labeling; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D012254:Ribavirin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D004273:DNA, Neoplasm; D007202:Indicators and Reagents; D012254:Ribavirin; C033706:tiazofurin