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Synthesis and Preliminary Evaluation Steroidal AntiestrogenGeldanamycin Conjugates
Hendricks, J. Adam Hanson, Robert N. Amolins, Michael Wayne Mihelcic, John M. Blagg, Brian S. J.
Hendricks, J. Adam
Hanson, Robert N.
Amolins, Michael Wayne
Mihelcic, John M.
Blagg, Brian S. J.
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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.
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Date
2013-06-15
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Elsevier
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Keywords
Anti-estrogen geldanamycin conjugates, Targeted drug delivery, Breast cancer, Click chemistry
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