| Literature DB >> 23648180 |
J Adam Hendricks1, Robert N Hanson, Michael Amolins, John M Mihelcic, Brian S Blagg.
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.Entities:
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Year: 2013 PMID： 23648180 PMCID： PMC4123820 DOI： 10.1016/j.bmcl.2013.03.116
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823