Lead identification of a potent benzopyranone selective estrogen receptor modulator

Autor:	Adam Kois, Normand Richard, Khammungkhune Sak, Graziella I. Shevlin, Shripad S. Bhagwat, John Sapienza, Helen Brady, Mathew Hickman, Jalluri Ravi Kumar, Deborah Mortensen, Gayo Leah M, Jeffrey A. Mckie, Mary Doubleday, May S Kung Sutherland, Bernd Stein
Rok vydání:	2002
Předmět:	Clinical Biochemistry Cell Pharmaceutical Science Pharmacology Biochemistry chemistry.chemical_compound Estrogen Receptor Modulators Piperidines Coumarins Drug Discovery medicine Tumor Cells Cultured Animals Raloxifene Molecular Biology Binding Sites Estradiol Molecular Structure Chemistry Interleukin-6 Organic Chemistry Estrogen Antagonists Estrogen Receptor alpha Ligand (biochemistry) In vitro Tamoxifen medicine.anatomical_structure Selective estrogen receptor modulator Raloxifene Hydrochloride Molecular Medicine Female Estrogen receptor alpha Lead compound hormones hormone substitutes and hormone antagonists medicine.drug
Zdroj:	Bioorganicmedicinal chemistry letters. 14(13)
ISSN:	0960-894X
Popis:	Starting from a phenol screening hit (6), three series of benzopyranone selective estrogen receptor modulators (SERMs) have been designed, synthesized, and analyzed for both estrogen receptor alpha binding affinity and in vitro activity in two cell assays. The lead compound identified, SP500263 (13), was more potent than raloxifene and tamoxifen in a cell-based assay measuring inhibition of interleukin-6 release.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5671bfae4e2deb683ad3fb739f4caaed https://pubmed.ncbi.nlm.nih.gov/15177442 Zobrazit plný text záznamu Full Text from ScienceDirect