Walter, Georg and Liebl, Renate and von Angerer, Erwin (2004) 2-Phenylindole sulfamates: inhibitors of steroid sulfatase with antiproliferative activity in MCF-7 breast cancer cells. JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, 88 (4-5). pp. 409-420. ISSN 0960-0760
Full text not available from this repository. (Request a copy)Abstract
A number of 2-phenylindole sulfamates with lipophilic side chains in I - 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 IC50 values between 2 nM and I muM. A favorable position for a long side chain is the nitrogen of a carbamoyl group at C-5 of the indole when the phenyl ring carries the sulfamate function. These derivatives inhibit gene activation in estrogen receptor (ER)-positive MCF-7 breast cancer cells in submicromolar concentrations and reduce cell proliferation with IC50 values of ca. I muM. All of the potent inhibitors were devoid of estrogenic activity and have the potential for in vivo application as steroid sulfatase inhibitors. (C) 2004 Elsevier Ltd. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | ESTROGEN-RECEPTOR AFFINITY; POTENT INHIBITORS; (P-O-SULFAMOYL)-N-ALKANOYL TYRAMINES; AROMATASE ACTIVITIES; PROLIFERATION; EXPRESSION; ESTRADIOL; DERIVATIVES; ENZYME; 17-BETA-HYDROXYSTEROID-DEHYDROGENASE; steroid sulfatase; breast cancer; phenylindole sulfamate; enzyme inhibition |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 26 Jul 2021 05:54 |
| Last Modified: | 26 Jul 2021 05:54 |
| URI: | https://pred.uni-regensburg.de/id/eprint/37817 |
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