1381868-77-4Relevant articles and documents
Convergent synthesis of a steroidal antiestrogen-mitomycin C hybrid using "click" chemistry
Hanson, Robert N.,Hua, Edward,Labaree, David,Hochberg, Richard B.,Proffitt, Kyle,Essigmann, John M.,Croy, Robert G.
, p. 8501 - 8508 (2012/11/14)
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.
STEROIDAL ANTI-HORMONE HYBRIDS
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Page/Page column 48-49, (2010/08/08)
Disclosed are novel compounds and compositions for inhibition of androgen and estrogen receptor signaling, methods for inhibiting androgen signaling, methods for inhibiting estrogen signaling, methods for inhibiting the interaction between a co-regulatory protein and an androgen or estrogen receptor, and methods for treating cancer.