Design, Synthesis, and Biological Evaluation of Some Novel Retinoid Derivatives

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dc.authoridFOTO, Egemen/0000-0002-0305-5467
dc.contributor.authorKonyar, Dilan
dc.contributor.authorFoto, Egemen
dc.contributor.authorFoto, Fatma Zilifdar
dc.contributor.authorBuyukbingol, Mehmet Erdem
dc.date.accessioned2025-02-22T14:08:44Z
dc.date.available2025-02-22T14:08:44Z
dc.date.issued2024
dc.departmentDicle Üniversitesien_US
dc.description.abstractBackground As cancer stands as a significant global health concern, many heterocyclic compounds that are more effective in cancer cells than healthy cells are being investigated for their selective anticancer potentials. One such compound is fenretinide, a synthetic derivative of retinoic acid that has a broad spectrum of cytotoxic activity against primary tumor cells, cell lines, and/or xenografts of various cancers. In this context, bexarotene and its derivatives, synthesized from hybridization of the fenretinide, are expected to possess a potential anticancer activity.Objective The objective of the present study was to investigate the synthesis of novel amid-derived and bexarotene-based compounds, as well as to assess their cytotoxic effects in different cancer cell lines.Methods This study involved the synthesis of twelve novel retinoid derivatives (6-17) in a six-step process. The cytotoxic activities of these compounds were assessed against various cancer cell lines, such as A549 (human lung carcinoma), HeLa (human cervical cancer), MCF7 (human breast adenocarcinoma), and WiDr (human colon adenocarcinoma). The chemical structures of these compounds were elucidated through their elemental analysis, mass spectrometry (ESI+, ESI-), as well as 1H-NMR and 13C-NMR spectroscopic data.Results The obtained cell toxicity results indicated that compounds 6, 8, 11, 12, 13, 14, and 17 were found to exhibit the strongest cytotoxic activity in above mentioned cancer cell lines. The IC50 values for active compounds, 11 and 12, were determined as 2.38 mu M and 2.29 mu M, respectively. Remarkably, these compounds displayed higher cytotoxic activity in the WiDr cell line related to positive control, camptothecin (CPT). Moreover, compounds 14 and 17 demonstrated very similar level of cytotoxic activity to CPT, indicating their potential for antitumoral applications upon further studies.Conclusion While compounds 11, 12, 14, and 17 indicated a very comparable anticancer activity to CPT, compounds 6, 8, 11 and 12 showed more selective anticancer effect against cancer cells than non-cancerous cells. In accordance with the findings of the present study, they can be evaluated as primary candidates for further studies, specifically as RXR alpha-targeted anticancer agents.en_US
dc.description.sponsorshipAnkara University [13B3336001]en_US
dc.description.sponsorshipThis study is funded by the research fund of Ankara University (Grant No. 13B3336001).en_US
dc.identifier.doi10.2174/0115701808243556231017055256
dc.identifier.endpage2938en_US
dc.identifier.issn1570-1808
dc.identifier.issn1875-628X
dc.identifier.issue14en_US
dc.identifier.scopus2-s2.0-85202517444en_US
dc.identifier.scopusqualityQ3en_US
dc.identifier.startpage2926en_US
dc.identifier.urihttps://doi.org/10.2174/0115701808243556231017055256
dc.identifier.urihttps://hdl.handle.net/11468/29611
dc.identifier.volume21en_US
dc.identifier.wosWOS:001344437400007
dc.identifier.wosqualityQ4
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.language.isoenen_US
dc.publisherBentham Science Publ Ltden_US
dc.relation.ispartofLetters in Drug Design & Discoveryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.snmzKA_WOS_20250222
dc.subjectBexaroteneen_US
dc.subjectcytotoxicityen_US
dc.subjectanticanceren_US
dc.subjecthybrid moleculesen_US
dc.subjectretinoiden_US
dc.subjectRXRaen_US
dc.titleDesign, Synthesis, and Biological Evaluation of Some Novel Retinoid Derivativesen_US
dc.typeArticleen_US

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