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2-phenylindole sulfamates: inhibitors of steroid sulfatase with antiproliferative activity in MCF-7 breast cancer cells

Walter, Georg and Liebl, Renate and Angerer, Erwin von (2004) 2-phenylindole sulfamates: inhibitors of steroid sulfatase with antiproliferative activity in MCF-7 breast cancer cells. The Journal of Steroid Biochemistry and Molecular Biology 88 (4-5), pp. 409-420.

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Abstract

A number of 2-phenylindole sulfamates with lipophilic side chains in 1- or 5-position of the indole were synthesized and evaluated as steroid sulfatase (estrone sulfatase) inhibitors. Most of the new sulfamates inhibited the enzymatic hydrolysis of estrone sulfate in MDA-MB 231 breast cancer cells with IC(50) values between 2 nM and 1 microM. A favorable position for a long side chain is the ...

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Item Type:Article
Date:2004
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Projects:DFG Projekt An 139/6
Identification Number:
ValueType
15145451PubMed ID
10.1016/j.jsbmb.2003.12.012DOI
Classification:
NotationType
Antineoplastic Agents/chemistryMESH
Breast Neoplasms/drug therapyMESH
Cell Division/drug effectsMESH
Enzyme Inhibitors/chemistryMESH
Estrone/analogs & derivativesMESH
FemaleMESH
Gene Expression Regulation, Neoplastic/drug effectsMESH
HumansMESH
Hydrolysis/drug effectsMESH
HydrophobicityMESH
Inhibitory Concentration 50MESH
Receptors, Estrogen/metabolismMESH
Steryl-Sulfatase/antagonists & inhibitorsMESH
Structure-Activity RelationshipMESH
Sulfonic Acids/chemistryMESH
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 15:14
Last Modified:05 Aug 2009 13:48
Item ID:4781
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