1236152-84-3Relevant academic research and scientific papers
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)
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.
