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Synthesis and Preliminary Evaluation Steroidal AntiestrogenGeldanamycin Conjugates
dc.contributor.author | Hendricks, J. Adam | |
dc.contributor.author | Hanson, Robert N. | |
dc.contributor.author | Amolins, Michael Wayne | |
dc.contributor.author | Mihelcic, John M. | |
dc.contributor.author | Blagg, Brian S. J. | |
dc.date.accessioned | 2017-05-04T18:48:09Z | |
dc.date.available | 2017-05-04T18:48:09Z | |
dc.date.issued | 2013-06-15 | |
dc.identifier.citation | Hendricks, J. A., Hanson, R. N., Amolins, M., Mihelcic, J. M., & Blagg, B. S. (2013). Synthesis and Preliminary Evaluation Steroidal Antiestrogen-Geldanamycin Conjugates. Bioorganic & Medicinal Chemistry Letters, 23(12), 3635–3639. http://doi.org/10.1016/j.bmcl.2013.03.116 | en_US |
dc.identifier.uri | http://hdl.handle.net/1808/23894 | |
dc.description.abstract | Three novel steroidal antiestrogen-geldanamycin conjugates were prepared using a convergent strategy. The antiestrogenic component utilized the 11β-(4-functionalized-oxyphenyl) estradiol scaffold, while the geldanamycin component was derived by replacement of the 17-methoxy group with an appropriately functionalized amine. Ligation was achieved in high yield using azide alkyne cyclization reactions. Evaluation of the products against two breast cancer cell lines indicated that the conjugates retained significant antiproliferative activity. | en_US |
dc.publisher | Elsevier | en_US |
dc.rights | This article is made available under an Attribution-NonCommercial-NoDerivs 3.0 United States (CC BY-NC-ND 3.0 US) License. | en_US |
dc.rights.uri | https://creativecommons.org/licenses/by-nc-nd/3.0/us/ | en_US |
dc.subject | Anti-estrogen geldanamycin conjugates | en_US |
dc.subject | Targeted drug delivery | en_US |
dc.subject | Breast cancer | en_US |
dc.subject | Click chemistry | en_US |
dc.title | Synthesis and Preliminary Evaluation Steroidal AntiestrogenGeldanamycin Conjugates | en_US |
dc.type | Article | en_US |
kusw.kuauthor | Hendricks, J. Adam | |
kusw.kuauthor | Hanson, Robert N. | |
kusw.kuauthor | Amolins, Michael | |
kusw.kuauthor | Mihelcic, John M. | |
kusw.kuauthor | Blagg, Brian S. J. | |
kusw.kudepartment | Chemistry and Chemical Biology | en_US |
kusw.kudepartment | Medicinal Chemistry | en_US |
dc.identifier.doi | 10.1016/j.bmcl.2013.03.116 | en_US |
kusw.oaversion | Scholarly/refereed, author accepted manuscript | en_US |
kusw.oapolicy | This item meets KU Open Access policy criteria. | en_US |
dc.identifier.pmid | PMC4123820 | en_US |
dc.rights.accessrights | openAccess |