期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 13, 期 3, 页码 557-560出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(02)00987-3
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A rapid and efficient synthesis of a series Of C-2-symmetric 17beta-estradiol dimers is described. The new molecules are linked at position 17alpha of the steroid nucleus with either an alkyl chain or a polyethylene glycol chain. They are made from estrone in five chemical steps with an overall yield exceeding 30%. The biological activity of these compounds was evaluated in vitro on estrogen dependent and independent (ER+ and ER-) human breast tumor cell lines: MCF-7 and MDA-MB-231. Some of the dimers present selective cytotoxic activity against the ER+ cell line. (C) 2002 Elsevier Science Ltd. All rights reserved.
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