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Sulfamoyloxy-substituted 2-phenylindoles: antiestrogen-based inhibitors of the steroid sulfatase in human breast cancer cells

Golob, Thomas and Liebl, Renate and Angerer, Erwin von (2002) Sulfamoyloxy-substituted 2-phenylindoles: antiestrogen-based inhibitors of the steroid sulfatase in human breast cancer cells. Bioorganic & Medicinal Chemistry 10 (12), pp. 3941-3953.

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Abstract

Estrone sulfate (E1S) is an endogenous prodrug that delivers estrone and, subsequently, estradiol to the target cells following the hydrolysis by the enzyme estrone sulfatase which is active in various tissues including hormone dependent breast cancer cells. Blockade of this enzyme should reduce the estrogen level in breast cancer cells and prevent hormonal growth stimulation. Sulfamates of a ...

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Item Type:Article
Date:2002
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Projects:DFG Projekt An 139/6
Identification Number:
ValueType
12413846PubMed ID
Classification:
NotationType
Arylsulfatases/antagonists & inhibitorsMESH
Breast Neoplasms/pathologyMESH
Estrogen Receptor Modulators/chemical synthesisMESH
FemaleMESH
HumansMESH
Indoles/chemical synthesisMESH
Inhibitory Concentration 50MESH
Neoplasm Proteins/antagonists & inhibitorsMESH
Radioligand AssayMESH
Steryl-SulfataseMESH
Structure-Activity RelationshipMESH
Sulfatases/antagonists & inhibitorsMESH
Sulfonic AcidsMESH
Tumor Cells, CulturedMESH
Subjects:500 Science > 570 Life sciences
500 Science > 540 Chemistry & allied sciences
600 Technology > 610 Medical sciences Medicine
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Owner: Prof. Armin Buschauer
Deposited On:11 Dec 2008 16:57
Last Modified:05 Aug 2009 13:48
Item ID:4778
Owner Only: item control page
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