Abstract
We describe the synthesis of an 11beta isomer 3 of the steroidal antiestrogen fulvestrant 2. Partial fluorination of the 11beta side chain in 3 leads to 4, which still shows strong antiproliferative activity on MCF-7 cells. However, unlike 2 and 3, compound 4 fails to down-regulate estrogen receptor alpha (ERalpha). This result suggests that ERalpha down-regulation is not a sine qua non condition for the antitumor activity of steroidal antiestrogens.
Publication types
-
Comparative Study
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Antineoplastic Agents / chemical synthesis
-
Antineoplastic Agents / pharmacology*
-
Breast Neoplasms
-
Cell Line, Tumor
-
Down-Regulation
-
Estradiol / analogs & derivatives*
-
Estradiol / chemical synthesis
-
Estradiol / chemistry
-
Estradiol / pharmacology
-
Estrogen Receptor Modulators / chemical synthesis
-
Estrogen Receptor Modulators / pharmacology*
-
Estrogen Receptor alpha / drug effects
-
Fulvestrant
-
Humans
Substances
-
Antineoplastic Agents
-
Estrogen Receptor Modulators
-
Estrogen Receptor alpha
-
Fulvestrant
-
Estradiol