Regioselective monoalkylation of 17β-estradiol for the synthesis of cytotoxic estrogens.
作者信息
Gansbeke Koen Van, Solum Eirik Johansson, Liekens Sandra, Vik Anders, Hansen Trond Vidar
机构信息
School of Pharmacy, Department of Pharmaceutical Chemistry, University of Oslo, PO Box 1068 Blindern, N-0316 Oslo, Norway; On Leave from the Department of Pharmaceutical Sciences of the Vrije Universiteit Brussel, Brussel, Belgium.
Faculty of Health Sciences, Nord University, 7801 Namsos, Norway.
出版信息
Steroids. 2017 Aug;124:54-59. doi: 10.1016/j.steroids.2017.06.001. Epub 2017 Jun 15.
The regioselective synthesis of estrogens and their derivatives continues to be of interest. Most reported syntheses require multistep protocols associated with poor overall yield and lack of regioselectivity. New preparative protocols are still desired. Herein, 11 2-alkylated 17β-estradiol analogs were synthesized in a highly regioselective manner. The products were obtained using a convenient, one pot and high-yielding protocol. The anti-proliferative activity of the compounds was tested in human T-cell leukemia (CEM), human cervix carcinoma (HeLa) and human dermal microvascular endothelial (HMEC-1) cells.
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