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Issue 42, 2012
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Convergent synthesis of a steroidal antiestrogen-mitomycin C hybrid using “click” chemistry

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Abstract

A 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.

Graphical abstract: Convergent synthesis of a steroidal antiestrogen-mitomycin C hybrid using “click” chemistry

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Publication details

The article was received on 10 May 2012, accepted on 13 Sep 2012 and first published on 14 Sep 2012


Article type: Paper
DOI: 10.1039/C2OB25902H
Citation: Org. Biomol. Chem., 2012,10, 8501-8508
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    Convergent synthesis of a steroidal antiestrogen-mitomycin C hybrid using “click” chemistry

    R. N. Hanson, E. Hua, D. Labaree, R. B. Hochberg, K. Proffitt, J. M. Essigmann and R. G. Croy, Org. Biomol. Chem., 2012, 10, 8501
    DOI: 10.1039/C2OB25902H

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