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Synthesis and anti-tumor activity evaluation of salinomycin C20-O-alkyl/benzyl oxime derivatives

dc.rights.licenseopenen_US
hal.structure.identifierChimie et Biologie des Membranes et des Nanoobjets [CBMN]
dc.contributor.authorLI, Bo
dc.contributor.authorWU, Jun
dc.contributor.authorTANG, Lei
dc.contributor.authorLIAN, Xu
dc.contributor.authorLI, Zhongwen
dc.contributor.authorDUAN, Wenfang
dc.contributor.authorQIN, Tong
dc.contributor.authorZHAO, Xintong
dc.contributor.authorHU, Yuhua
dc.contributor.authorZHANG, Chi
dc.contributor.authorLI, Tianlei
dc.contributor.authorHAO, Jie
dc.contributor.authorZHANG, Wenxuan
dc.contributor.authorZHANG, Jihong
dc.contributor.authorWU, Song
dc.date.accessioned2025-02-11T15:02:14Z
dc.date.available2025-02-11T15:02:14Z
dc.date.issued2021-12-30
dc.identifier.issn1477-0539en_US
dc.identifier.urihttps://oskar-bordeaux.fr/handle/20.500.12278/204797
dc.description.abstractEnSeventeen C20-O-alkyl/benzyl oxime derivatives were synthesized by a concise and effective method. Most of these derivatives showed tens to several hundred nanomolar IC50 values against HT-29 colorectal, HGC-27 gastric and MDA-MB-231 breast cancer cells, whose antiproliferative activity is 15–240 fold better than that of salinomycin. The C20-oxime etherified derivatives can coordinate potassium ions, and further adjust the cytosolic Ca2+ concentrations in HT-29 cells. The significant improvement of the potency should be attributed to the better ion binding and transport ability of the modified derivatives. In addition, the C20-O-alkyl/benzyl oxime derivatives showed much better selectivity indexes (SI) than salinomycin, indicating that they present lower neurotoxic risk.
dc.language.isoENen_US
dc.title.enSynthesis and anti-tumor activity evaluation of salinomycin C20-O-alkyl/benzyl oxime derivatives
dc.title.alternativeOrg. Biomol. Chem.en_US
dc.typeArticle de revueen_US
dc.identifier.doi10.1039/D1OB02292Jen_US
dc.subject.halChimie/Matériauxen_US
dc.identifier.pubmed35006233en_US
bordeaux.journalOrganic & Biomolecular Chemistryen_US
bordeaux.page870-876en_US
bordeaux.volume20en_US
bordeaux.hal.laboratoriesCBMN : Chimie & de Biologie des Membranes & des Nano-objets - UMR 5248en_US
bordeaux.issue4en_US
bordeaux.institutionUniversité de Bordeauxen_US
bordeaux.institutionBordeaux INPen_US
bordeaux.institutionCNRSen_US
bordeaux.peerReviewedouien_US
bordeaux.inpressnonen_US
hal.identifierhal-04941005
hal.version1
hal.date.transferred2025-02-11T15:02:17Z
hal.popularnonen_US
hal.audienceInternationaleen_US
hal.exporttrue
dc.rights.ccPas de Licence CCen_US
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