Mueller, Klaus and Breu, Klaus and Reindl, Hans (2001) 10-phenylbutyryl-substituted anthracenones as inhibitors of keratinocyte growth and LTB4 biosynthesis. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 36 (2). pp. 179-184. ISSN 0223-5234, 1768-3254
Full text not available from this repository. (Request a copy)Abstract
A recent observation that phenylbutyryl anthracenone 2, an analogue of the antipsoriatic anthralin, is a potent inhibitor of leukotriene B-4 (LTB4) biosynthesis has prompted a search of other anthracenones with improved antiproliferative activity. In that direction, a limited number of analogues related to 2 have been prepared and evaluated in the HaCaT keratinocytes proliferation and in the polymorphonuclear leukocyte LTB4 assay. The 4-methoxy analogue 2a and the side chain methylated 21 retain the full inhibitory activity of 1 against LTB4 biosynthesis while their antiproliferative activity is markedly enhanced and comparable to that of the antipsoriatic anthralin. In contrast to anthralin, cytotoxic effects against cell membranes are strongly reduced as documented by the LDH activity released from cytoplasm of keratinocytes. (C) 2001 Editions scientifiques et medicales Elsevier SAS.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | MODULATED REDOX PROPERTIES; ANTIPSORIATIC ANTHRONES; LEUKOTRIENE BIOSYNTHESIS; 5-LIPOXYGENASE; DERIVATIVES; 1,8-DIHYDROXY-9(10H)-ANTHRACENONES; 12(S)-HETE; ANTHRALIN; RADICALS; POTENT; anthracenone; antiproliferative activity; HaCaT; hydroxyl radicals; lactate dehydrogenase release; LTB4 biosynthesis |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 15 Feb 2022 07:57 |
| Last Modified: | 15 Feb 2022 07:57 |
| URI: | https://pred.uni-regensburg.de/id/eprint/41766 |
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