35 KB153 KB21 KB199220252004Badowska-Rosłonek, KatarzynaGodlewska, JoannaKaczmarek, ŁukaszOpolski, AdamPeczyńska-Czoch, WandaRamza, Janštevilka:2letnik:388 stranistr. 137-144ISSN:1318-2099COBISSID:18167513URN:URN:NBN:SI:doc-10OFGHTOenAssociation of Radiology and OncologyRadiology and oncology (Ljubljana)Antagonists And Inhibitorsbiokemijacelične kultureDna Topoisomerase (Atp-Hydrolysing)DNA topoizomeraza (ATP-hidrolizirajoča)Drug EffectsindoliKinoniMicroscopy, FluorescenceMikroskopija fluorescenčnaQuinonessintezaTumor Cells, CulturedTumorske celične kultureNew saccharide derivatives of indolo2,3-bquinoline as cytotoxic compounds and topoisomerase II inhibitors|Some of alkyl- and alkylamino- derivatives of 6H-indološ2,3-bđquinolines are known to be active antiproliferative and cell cycle modulating compounds. Their cytotoxic properties are, at least in part, due to DNA intercalation ability and topoisomerase 11 inhibition activity. To improve physicochemical and biological properties of 6H-indološ2,3-bđquinolines the series of new, saccharide (C-2, C-9 or N-6) derivatives were designed and synthesized. The influence of different carbohydrate units (D glucose, D-lactose, L-rhamnose, Lacosamine, L-daunosamine), position of attachment and linker size on cytotoxic properties and topoisomerase 11 inhibition activity were tested. Among compounds tested there were 2-deoxy-a-D glucopyranoside (1-6), 2-deoxy-alpha-L-rhamnopyranoside (7-12) and 2-deoxy-alpha-D-lactopyranoside (13-18) derivatives in the group of saccharide moiety containing compounds anda-L-daunosaminide (19-24) and a-L-acosaminide (2527) in the aminosaccharidederivatives series as wellNekateri alkilni in alkilaminski derivati 6H-indološ2,3-bđkinolinov imajo antiproliferativen učinek in modulirajo celični cikel. Njihove citotoksične lastnosti deloma izvirajo iz sposobnosti interkaliranja DNK in sposobnosti inhibiranja topoizomeraze II. Ker smo želeli doseči boljše fizikalno-kemične in biološke lastnosti 6H-indološ2,3-bđkinolinov, smo sintetizirali serijo novih saharidnih derivatov ((C2, C-9 ali N-6). Testirali smo vpliv različnih karbohiratnih enot (D-glukoza, D-laktoza, L-ramnoza, Lakozamin, L-daunozamin),mesto vezave in velikosti linkerja na citotoksične lastnosti in inhibicijo topoizomeraze II. Testirali smo spojine iz skupine saharidov, ki vsebujejo derivate 2-deoksi-?-Dglukopiranozida (1-6), 2-deoksi-?-L-ramnopiranozida (7-12) in 2-deoksi-?-D-laktopiranozida (13-18) ter tudi serijo aminosaharidnih derivatov ?-L-daunozaminid (19-24) in ?-L-akozaminid (25-27)TEXTznanstveno časopisjejournalsSlovenian National E-content AggregatorNational and University Library of SloveniaDruštvo radiologije in onkologije