Abstract
The structure-activity relationships of the anthracycline-related antibiotics of the tetracenomycin C/elloramycin-type were investigated by derivatization of elloramycin (1) and elloramycinone (2). During hydrolysis experiments a unique transglycosylation reaction was discovered, converting elloramycin (1) into isoelloramycin (10) by treatment with anhydrous trifluoroacetic acid. Following the proposed structure-activity relationship concept, 8-O-methylelloramycinone (14) was synthesized from elloramycinone (2), and was shown to be the most active derivative according to the proliferation inhibition assay against murine L1210 leukemia cells.
| Original language | English |
|---|---|
| Pages (from-to) | 1169-1178 |
| Number of pages | 10 |
| Journal | Journal of Antibiotics |
| Volume | 43 |
| Issue number | 9 |
| DOIs | |
| State | Published - 1990 |
ASJC Scopus subject areas
- Pharmacology
- Drug Discovery
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