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Synthesis of naphthalimide derivatives with potential anticancer activity, their comparative ds- and G-quadruplex-DNA binding studies and related biological activities

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dc.creator Yildiz, Ufuk
dc.creator Kandemir, Irfan
dc.creator Comert, Fusun
dc.creator Coban, Burak
dc.creator Akkoc, Senem
dc.date 2020-02-25T01:00:00Z
dc.date.accessioned 2020-10-06T10:47:19Z
dc.date.available 2020-10-06T10:47:19Z
dc.identifier 86add15d-0738-43b3-a8b3-624256760c79
dc.identifier 10.1007/s11033-019-05239-y
dc.identifier https://avesis.sdu.edu.tr/publication/details/86add15d-0738-43b3-a8b3-624256760c79/oai
dc.identifier.uri http://acikerisim.sdu.edu.tr/xmlui/handle/123456789/65351
dc.description Two new cytotoxic 1,8-naphthalimide derivatives have been synthesized and characterized. Their biological activities as cytotoxicity and antimicrobial activities and inhibitory activities against DNA-polymerase were evaluated. The interactions of compounds with double-stranded- and quadruple-DNA have been studied by UV-Vis, fluorescent intercalator displacement, competition dialysis, circular dichroism and the findings were compared with the parent naphthalimide and the other compounds. The results show that both compounds (1 and 2) and the parent compound NI have strong cytotoxic activities against Beas-2B, MCF-7, HepG2 and MDA-MB-231 cancer cell lines, antimicrobial activities against Staphylococcus aureus ATCC 29213, Enterococcus faecalis ATCC 29212 and inhibitory activities towards Taq-polymerase and transcriptase. These novel cationic compounds 1 and 2 can stabilize G-quadruplexes DNA according to thermal denaturation experiments, they change the 3D structure of the DNA (see details in CD experiments) and they exhibit different binding affinities for q-DNA and ds-DNA revealed by spectrophotometric titrations and competitive dialysis studies.
dc.language eng
dc.rights info:eu-repo/semantics/closedAccess
dc.title Synthesis of naphthalimide derivatives with potential anticancer activity, their comparative ds- and G-quadruplex-DNA binding studies and related biological activities
dc.type info:eu-repo/semantics/article


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