Walter, Georg and Liebl, Renate and von Angerer, Erwin (2004) Synthesis and biological evaluation of stilbene-based pure estrogen antagonists. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 14 (18). pp. 4659-4663. ISSN 0960-894X, 1464-3405
Full text not available from this repository. (Request a copy)Abstract
Replacement of one of the ethyl substituents in diethylstilbestrol by side chains with functional groups converted this potent estrogen into pure antiestrogens with the potential for the treatment of breast cancer. These agents completely suppressed estrogen receptor-mediated gene activation and inhibited the growth of estrogen-sensitive MCF-7 breast cancer cells in submicromolar concentrations. The most potent derivative displayed similar activity as fulvestrant (ICI 182,780) in vitro and in the mouse uterine weight test. Obviously, the stilbene structure can act as a substitute for estradiol in the development of pure estrogen antagonists. (C) 2004 Elsevier Ltd. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | BREAST-CANCER; RECEPTOR; 2-PHENYLINDOLES; ANTIESTROGENS; FULVESTRANT; TAMOXIFEN; |
| Subjects: | 600 Technology > 610 Medical sciences Medicine |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 28 Jun 2021 11:44 |
| Last Modified: | 28 Jun 2021 11:44 |
| URI: | https://pred.uni-regensburg.de/id/eprint/37185 |
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