Bazı benzoksazin türevlerinin ökaryotik DNA topoizomeraz I enzimi üzerindeki inhibisyon etkilerinin incelenmesi
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Abstract
Bu çalısmada, kemoterapötik etkili olabilecegi düsünülen yeni sentezlenmis 18 tanebenzoksazin türevi bilesigin ökaryotik DNA topoizomeraz I enzimi üzerindekiinhibisyon etkileri arastırıldı.Test edilen bilesiklerden 14 tanesinin ökaryotik DNA topoizomeraz I enzimi üzerindekatalitik inhibitör etki gösterdigi (S18 (IC50=1,61 ?g/?l) > S1 > S16 > S17 > S5 > S14 >S15 > S13 > S2 > S3 > S12 > S9 > S8 > S4 (IC50=24,84 ?g/?l)), 1 tanesinin (S10)topoizomeraz zehiri olarak inhibisyon etki gösterdigi, 3 tanesinin ise enzim üzerindeinhibisyon etki göstermedigi bulundu.Denenen bilesikler arasında en güçlü inhibisyon etki gösteren S10 (IC50=0,00017?g/?l) bilesiginin klinikte ilaç olarak kullanılan camptothecinden (IC50=0,013 ?g/?l)daha güçlü inhibisyon etki gösterdigi saptandı.Anahtar Kelimeler: Benzoksazin, ökaryotik DNA topoizomeraz I (insan),topoizomeraz inhibitörleri, camptothecin. In this study, derivates of newly synthesized 18 benzoxazine compounds, which arethought to have a chemotherapeuticly effective, have been investigated about theirinhibitory effects on eucaryotic DNA topoisomerase I.It has been showed that 14 of the tested compounds (S18 (IC50=1,61 ?g/?l) > S1 >S16 > S17 > S5 > S14 > S15 > S13 > S2 > S3 > S12 > S9 > S8 > S4 (IC50=24,84?g/?l)) have inhibitory effect on DNA topoisomerase I enzyme as catalytic inhibitor, 1of them has poison effect on the enzyme,tough and 3 of them don?t have anyinhibitory effect on the enzyme.It has been determined that S10 (IC50=0,00017?g/?l)has the strongest inhibitoryeffect among tested compounds on topoisomerase I enzyme than camptothecin usedas a drug in clinic (IC50=0,013 ?g/?l).Keywords: Benzoxazine, eukaryotic DNA topoisomerase I (human), topoisomeraseinhibitors, camptothecin
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