Kumar, Sunil and Mueller, Klaus (1999) Depsides as non-redox inhibitors of leukotriene B-4 biosynthesis and HaCaT cell growth. 1. Novel analogues of barbatic and diffractaic acid. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 34 (12). pp. 1035-1042. ISSN 0223-5234, 1768-3254
Full text not available from this repository.Abstract
A series of barbatic and diffractaic acid analogues has been synthesized and evaluated as inhibitors of leukotriene B-4 (LTB4) biosynthesis and as antiproliferative agents. The 4-O-demethyl barbatic and diffractaic acid derivatives were among the most active compounds in both assays. In particular, ethyl 4-O-demethylbarbatate was the most potent LTB4 biosynthesis inhibitor of this series, with an IC50 value in the submicromolar range. Because the compounds did not show appreciable reactivity against a stable free radical, 2,2-diphenyl-1-picrylhydrazyl, and did not produce appreciable amounts of deoxyribose degradation as a measure of their potency to generate hydroxyl radicals, a simple redox effect could not explain their biological activity. Also, there was no nonspecific cytotoxicity as documented by the activity of lactate dehydrogenase released from the cytoplasm of keratinocytes, which was in the control range. (C) 1999 Editions scientifiques et medicales Elsevier SAS.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | ANTIPSORIATIC ANTHRONES; 5-LIPOXYGENASE; 1,8-DIHYDROXY-9(10H)-ANTHRACENONES; ACTIVATION; RADICALS; LICHENS; barbatic acid; diffractaic acid; antiproliferative activity; keratinocytes; lactate dehydrogenase release; leukotriene 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: | 06 Dec 2022 11:11 |
| Last Modified: | 06 Dec 2022 11:11 |
| URI: | https://pred.uni-regensburg.de/id/eprint/48781 |
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