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dc.contributor.authorNaman, C. Benjamin
dc.contributor.authorAlmaliti, Jehad
dc.contributor.authorArmstrong, Lorene
dc.contributor.authorCaro-Díaz, Eduardo J.
dc.contributor.authorPierce, Marsha L.
dc.contributor.authorGlukhov, Evgenia
dc.contributor.authorFenner, Amanda
dc.contributor.authorSpadafora, Carmenza
dc.contributor.authorDebonsi, Hosana M.
dc.contributor.authorDorrestein, Pieter C.
dc.contributor.authorMurray, Thomas F.
dc.contributor.authorGerwick, William H.
dc.date.accessioned2020-06-26T03:57:41Z
dc.date.available2020-06-26T03:57:41Z
dc.date.issued2017-08-07
dc.identifier.otherDOI: 10.1021/acs.jnatprod.7b00367
dc.identifier.urihttp://repositorio-indicasat.org.pa/handle/123456789/116
dc.descriptionA recent untargeted metabolomics investigation into the chemical profile of 10 organic extracts from cf. Symploca spp. revealed several interesting chemical leads for further natural product drug discovery. Subsequent targetdirected isolation efforts with one of these, a Panamanian marine cyanobacterium cf. Symploca sp., yielded a phenethylamide metabolite that terminates in a relatively rare gemdichlorovinylidene moiety, caracolamide A (1), along with a known isotactic polymethoxy-1-alkene (2). Detailed NMR and HRESIMS analyses were used to determine the structures of these molecules, and compound 1 was confirmed by a threestep synthesis. Pure compound 1 was shown to have in vitro calcium influx and calcium channel oscillation modulatory activity when tested as low as 10 pM using cultured murine cortical neurons, but was not cytotoxic to NCI-H460 human non-small-cell lung cancer cells in vitro (IC50 > 10 μM).en_US
dc.description.abstractA recent untargeted metabolomics investigation into the chemical profile of 10 organic extracts from cf. Symploca spp. revealed several interesting chemical leads for further natural product drug discovery. Subsequent targetdirected isolation efforts with one of these, a Panamanian marine cyanobacterium cf. Symploca sp., yielded a phenethylamide metabolite that terminates in a relatively rare gemdichlorovinylidene moiety, caracolamide A (1), along with a known isotactic polymethoxy-1-alkene (2). Detailed NMR and HRESIMS analyses were used to determine the structures of these molecules, and compound 1 was confirmed by a threestep synthesis. Pure compound 1 was shown to have in vitro calcium influx and calcium channel oscillation modulatory activity when tested as low as 10 pM using cultured murine cortical neurons, but was not cytotoxic to NCI-H460 human non-small-cell lung cancer cells in vitro (IC50 > 10 μM).en_US
dc.formatapplication/pdf
dc.language.isoengen_US
dc.rightsInfo:eu-repo/semantics/openAccess
dc.rightshttps://creativecommons.org/licenses/by/4.0/
dc.subjectDiscovery and Synthesisen_US
dc.subjectModulating Dichlorovinylideneen_US
dc.subjectPanamanian Marineen_US
dc.titleDiscovery and Synthesis of Caracolamide A, an Ion Channel Modulating Dichlorovinylidene Containing Phenethylamide from a Panamanian Marine Cyanobacterium cf. Symploca Speciesen_US
dc.typeinfo:eu-repo/semantics/articleen_US
dc.typeInfo:eu-repo/semantics/publishedversion


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