Solid-Phase synthesis and investigation of benzofurans as selective estrogen receptor modulators
| Autor: | William G. Stirtan, Diana Marrero, Ulrike Moehler, Ingo Muegge, Jinshan Chen, Mary M. Mader, Suresh Katti, Daniel R. Weaver, Hong Xiao, Roger A. Smith, William Carley |
|---|---|
| Rok vydání: | 2002 |
| Předmět: |
Models
Molecular Selective Estrogen Receptor Modulators Agonist medicine.drug_class Clinical Biochemistry Pharmaceutical Science Estrogen receptor Breast Neoplasms Biochemistry Chemical synthesis Cell Line Solid-phase synthesis Drug Discovery medicine Estrogen Receptor beta Humans Raloxifene Molecular Biology Benzofurans Chemistry Cell growth Organic Chemistry Estrogen Receptor alpha Receptors Estrogen Selective estrogen receptor modulator Estrogen Drug Design Raloxifene Hydrochloride Molecular Medicine Female medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 12:2875-2878 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(02)00613-3 |
| Popis: | A library of benzofurans was prepared by solid-phase synthesis methods, and several analogues were identified as potent ligands for the estrogen receptors ER-alpha and ER-beta, with some compounds having selectivity for ER-alpha. Analogues designed to more closely mimic Raloxifene were less effective. Certain benzofurans were effective in a bone pit assay, but were characterized as agonists in a MCF-7 breast tumor cell proliferation assay. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect