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dc.contributor.authorHanson, Robert N.
dc.contributor.authorHua, Edward
dc.contributor.authorLabaree, David
dc.contributor.authorHochberg, Richard B.
dc.contributor.authorProffitt, Kyle
dc.contributor.authorEssigmann, John M.
dc.contributor.authorCroy, Robert G.
dc.date.accessioned2014-08-19T17:55:17Z
dc.date.available2014-08-19T17:55:17Z
dc.date.issued2012-09
dc.date.submitted2012-05
dc.identifier.issn1477-0520
dc.identifier.issn1477-0539
dc.identifier.urihttp://hdl.handle.net/1721.1/88910
dc.description.abstractA convergent synthesis of a novel estrogen receptor-targeted drug hybrid was developed based on structures of the potent anti-proliferative mitomycin C and the steroidal anti-estrogen RU 39411. The steroidal antiestrogen was prepared with an azido-triethylene glycoloxy linker while the mitomycin C derivative (porfirimycin) incorporated a complementary 7-N-terminal alkyne. The two components were ligated using the Huisgen [3 + 2] cycloaddition (“click”) reaction. Preliminary biological assays demonstrated that the final hybrid compound retained both potent anti-estrogenic and anti-proliferative activities.en_US
dc.description.sponsorshipNational Institutes of Health (U.S.) (Grant PHS 5R01 CA 086061-09)en_US
dc.language.isoen_US
dc.publisherRoyal Society of Chemistryen_US
dc.relation.isversionofhttp://dx.doi.org/10.1039/c2ob25902hen_US
dc.rightsCreative Commons Attribution-Noncommercial-Share Alikeen_US
dc.rights.urihttp://creativecommons.org/licenses/by-nc-sa/4.0/en_US
dc.sourcePMCen_US
dc.titleConvergent synthesis of a steroidal antiestrogen-mitomycin C hybrid using “click” chemistryen_US
dc.typeArticleen_US
dc.identifier.citationHanson, Robert N., Edward Hua, David Labaree, Richard B. Hochberg, Kyle Proffitt, John M. Essigmann, and Robert G. Croy. “Convergent Synthesis of a Steroidal Antiestrogen-Mitomycin C Hybrid Using ‘click’ Chemistry.” Organic & Biomolecular Chemistry 10, no. 42 (2012): 8501.en_US
dc.contributor.departmentdeleteen_US
dc.contributor.departmentMassachusetts Institute of Technology. Department of Biological Engineeringen_US
dc.contributor.departmentMassachusetts Institute of Technology. Department of Chemistryen_US
dc.contributor.mitauthorProffitt, Kyleen_US
dc.contributor.mitauthorEssigmann, John M.en_US
dc.contributor.mitauthorCroy, Robert G.en_US
dc.relation.journalOrganic & Biomolecular Chemistryen_US
dc.eprint.versionAuthor's final manuscripten_US
dc.type.urihttp://purl.org/eprint/type/JournalArticleen_US
eprint.statushttp://purl.org/eprint/status/PeerRevieweden_US
dspace.orderedauthorsHanson, Robert N.; Hua, Edward; Labaree, David; Hochberg, Richard B.; Proffitt, Kyle; Essigmann, John M.; Croy, Robert G.en_US
dc.identifier.orcidhttps://orcid.org/0000-0002-2196-5691
mit.licenseOPEN_ACCESS_POLICYen_US


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