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dc.contributor.authorMoosa, Basem
dc.contributor.authorSagar, Sunil
dc.contributor.authorLi, Song
dc.contributor.authorEsau, Luke
dc.contributor.authorKaur, Mandeep
dc.contributor.authorKhashab, Niveen M.
dc.date.accessioned2016-02-07T14:46:06Z
dc.date.available2016-02-07T14:46:06Z
dc.date.issued2016-02-04
dc.identifier.citationSynthesis and anticancer evaluation of spermatinamine analogues 2016 Bioorganic & Medicinal Chemistry Letters
dc.identifier.issn0960894X
dc.identifier.pmid26874403
dc.identifier.doi10.1016/j.bmcl.2016.01.083
dc.identifier.urihttp://hdl.handle.net/10754/595859
dc.description.abstractSpermatinamine was isolated from an Australian marine sponge, Pseudoceratina sp. as an inhibitor of isoprenylcystiene carboxyl methyltransferase (Icmt), an attractive and novel anticancer target. Herein, we report the synthesis of spermatinamine analogues and their cytotoxic evaluation against three human cancer cell lines i.e. cervix adenocarcinoma (HeLa), breast adenocarcinoma (MCF-7), and prostate carcinoma (DU145). Analogues 12, 14 and 15 were found to be the most potent against one or more cell lines with the IC50 values in the range of 5 - 10 μM. The obtained results suggested that longer polyamine linker along with aromatic oxime substitution provided the most potent analogue compounds against cancer cell lines.
dc.language.isoen
dc.publisherElsevier BV
dc.relation.urlhttp://linkinghub.elsevier.com/retrieve/pii/S0960894X16300919
dc.rightsNOTICE: this is the author’s version of a work that was accepted for publication in Bioorganic & Medicinal Chemistry Letters. Changes resulting from the publishing process, such as peer review, editing, corrections, structural formatting, and other quality control mechanisms may not be reflected in this document. Changes may have been made to this work since it was submitted for publication. A definitive version was subsequently published in Bioorganic & Medicinal Chemistry Letters, 4 February 2016. DOI: 10.1016/j.bmcl.2016.01.083
dc.subjectNatural products
dc.subjectBromotyrosine
dc.subjectSpermatinamine
dc.subjectCancer
dc.subjectCytotoxicity
dc.titleSynthesis and anticancer evaluation of spermatinamine analogues
dc.typeArticle
dc.contributor.departmentAdvanced Membranes and Porous Materials Research Center
dc.contributor.departmentBiological and Environmental Sciences and Engineering (BESE) Division
dc.contributor.departmentBiomolecular Lab
dc.contributor.departmentChemical Science Program
dc.contributor.departmentComputational Bioscience Research Center (CBRC)
dc.contributor.departmentComputer, Electrical and Mathematical Sciences and Engineering (CEMSE) Division
dc.contributor.departmentNGS, qPCR and Single Cell Genomics
dc.contributor.departmentOffice of the VP
dc.contributor.departmentPhysical Science and Engineering (PSE) Division
dc.contributor.departmentSanger and Third Generation Sequencing
dc.contributor.departmentSmart Hybrid Materials (SHMs) lab
dc.contributor.departmentTechnology Transfer
dc.identifier.journalBioorganic & Medicinal Chemistry Letters
dc.eprint.versionPost-print
dc.contributor.institutionSchool of Molecular and Cell Biology, University of the Witwatersrand, Private Bag 3, Wits, 2050, Johannesburg, Republic of South Africa
dc.contributor.affiliationKing Abdullah University of Science and Technology (KAUST)
kaust.personMoosa, Basem
kaust.personSagar, Sunil
kaust.personLi, Song
kaust.personEsau, Luke
kaust.personKaur, Mandeep
kaust.personKhashab, Niveen M.
refterms.dateFOA2018-02-04T00:00:00Z
dc.date.published-online2016-02-04
dc.date.published-print2016-03


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