Synthesis and biological activity of some new 5'-O-acyl tiazofurin derivatives.
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.
Pejanović
Vjera
V
Department of Chemistry, Faculty of Sciences, University of Novi Sad, Serbia & Montenegro. vpejanovic@hemofarm.co.yu
Piperski
Vesna
V
Ugljesić-Kilibarda
Dragana
D
Tasić
Jelena
J
Dacević
Mirjana
M
Medić-Mijacević
Ljubica
L
Gunić
Esmir
E
Popsavin
Mirjana
M
Popsavin
Velimir
V
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
D000970:Antineoplastic Agents; D004273:DNA, Neoplasm; D007202:Indicators and Reagents; D012254:Ribavirin; C033706:tiazofurin