{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Cadoni E"],"funding":["Fundo Social Europeu e Programa Operacional Potencial Humano","Fundação para a Ciência e a Tecnologia","European Structural & Investment Funds","COMPETE Program","European Structural & Investment Funds"],"pagination":["669"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC8308870"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["14(7)"],"pubmed_abstract":["G-quadruplex (G4)-interactive small molecules have a wide range of potential applications, not only as drugs, but also as sensors of quadruplex structures. The purpose of this work is the synthesis of analogues of the bis-methylquinolinium-pyridine-2,6-dicarboxamide G4 ligand 360A, to identify relevant structure-activity relationships to apply to the design of other G4-interactive small molecules bearing bis-quinoline or bis-isoquinoline moieties. Thermal denaturation experiments revealed that non-methylated derivatives with a relative 1,4 position between the amide linker and the nitrogen of the quinoline ring are moderate G4 stabilizers, with a preference for the hybrid h-Telo G4, a 21-nt sequence present in human telomeres. Insertion of a positive charge upon methylation of quinoline/is"],"journal":["Pharmaceuticals (Basel, Switzerland)"],"pubmed_title":["New (Iso)quinolinyl-pyridine-2,6-dicarboxamide G-Quadruplex Stabilizers. A Structure-Activity Relationship Study."],"pmcid":["PMC8308870"],"funding_grant_id":["SAICTPAC/0019/2015, UIDP/04138/2020 of iMed, UIDB/00709/2020 of CICS, PTDC/BIA-BFS/28419/2017, strategic project UIDB/04046/2020-UIDP/04046/2020 (BioISI)","IF/00959/2015","LISBOA-01-0145-FEDER-016405","SAICTPAC/0019/2015"],"pubmed_authors":["Mendes E","Paulo A","Vitor J","Cruz C","Cadoni E","Victor BL","Carvalho J","Emidio RM","Magalhaes PR"],"additional_accession":[]},"is_claimable":false,"name":"New (Iso)quinolinyl-pyridine-2,6-dicarboxamide G-Quadruplex Stabilizers. A Structure-Activity Relationship Study.","description":"G-quadruplex (G4)-interactive small molecules have a wide range of potential applications, not only as drugs, but also as sensors of quadruplex structures. The purpose of this work is the synthesis of analogues of the bis-methylquinolinium-pyridine-2,6-dicarboxamide G4 ligand 360A, to identify relevant structure-activity relationships to apply to the design of other G4-interactive small molecules bearing bis-quinoline or bis-isoquinoline moieties. Thermal denaturation experiments revealed that non-methylated derivatives with a relative 1,4 position between the amide linker and the nitrogen of the quinoline ring are moderate G4 stabilizers, with a preference for the hybrid h-Telo G4, a 21-nt sequence present in human telomeres. Insertion of a positive charge upon methylation of quinoline/is","dates":{"release":"2021-01-01T00:00:00Z","publication":"2021 Jul","modification":"2026-04-08T06:49:50.787Z","creation":"2022-02-11T05:01:29.624Z"},"accession":"S-EPMC8308870","cross_references":{"pubmed":["34358095"],"doi":["10.3390/ph14070669"]}}