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dc.contributor.authorSherer, Chris
dc.contributor.authorPrabhu, Saurabh
dc.contributor.authorAdams, David
dc.contributor.authorHayes, Joseph
dc.contributor.authorRowther, Farzana
dc.contributor.authorTolaymat, Ibrahim
dc.contributor.authorWarr, Tracy
dc.contributor.authorSnape, Timothy J.
dc.date.accessioned2018-12-05T16:25:09Z
dc.date.available2018-12-05T16:25:09Z
dc.date.issued2018-10-02
dc.identifier.citationSherer, C. et al. (2018) Towards Identifying Potent New Hits for Glioblastoma, MedChemComm. Doi: 10.1039/C8MD00436Fen_US
dc.identifier.issn2040-2503en_US
dc.identifier.doi10.1039/C8MD00436F
dc.identifier.urihttp://hdl.handle.net/2436/621952
dc.description.abstractGlioblastoma is a devastating disease of the brain and is the most common malignant primary brain tumour in adults. The prognosis for patients is very poor with median time of survival after diagnosis measured in months, due in part to the tumours being highly aggressive and often resistant to chemotherapies. Alongside the ongoing research to identify key factors involved in tumour progression in glioblastoma, medicinal chemistry approaches must also be used in order to rapidly establish new and better treatments for brain tumour patients. Using a computational similarity search of the ZINC database, alongside traditional analogue design by medicinal chemistry intuition to improve the breadth of chemical space under consideration, six new hit compounds (14, 16, 18, 19, 20 and 22) were identified possessing low micromolar activity against both established cell lines (U87MG and U251MG) and patient-derived cell cultures (IN1472, IN1528 and IN1760). Each of these scaffolds provides a new platform for future development of a new therapy in this area, with particular promise shown against glioblastoma subtypes that are resistant to conventional chemotherapeutic agents.en_US
dc.formatapplication/PDFen_US
dc.language.isoenen_US
dc.publisherRoyal Society of Chemistryen_US
dc.relation.urlhttps://pubs.rsc.org/en/content/articlelanding/2018/md/c8md00436f#!divAbstracten_US
dc.rightsAttribution-NonCommercial-NoDerivs 3.0 United States*
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/3.0/us/*
dc.subjectscaffolden_US
dc.subjectglioblastomaen_US
dc.subjectcanceren_US
dc.subjectSARen_US
dc.subjectsimilarity screeningen_US
dc.titleTowards identifying potent new hits for glioblastomaen_US
dc.typeJournal article
dc.identifier.journalMedChemCommen_US
dc.date.accepted2018-10-01
rioxxterms.funderUniversity of Wolverhamptonen_US
rioxxterms.identifier.projectUOW051218TWen_US
rioxxterms.versionAMen_US
rioxxterms.licenseref.urihttps://creativecommons.org/licenses/by-nc-nd/4.0/en_US
rioxxterms.licenseref.startdate2019-10-02en_US
rioxxterms.typeJournal Article
dc.source.volume9
dc.source.issue11
dc.source.beginpage1850
dc.source.endpage1861
dcterms.dateAccepted2018-10-01
refterms.dateFCD2018-12-05T16:24:29Z
refterms.versionFCDAM


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