Abstract
Structure-activity relationship of 13-deoxytedanolide showed that the southern and northern hemispheres play independent roles to exhibit potent biological activity. To obtain information of structure-activity relationships (SARs) of 13-deoxytedanolide, its chemical transformation has been carried out, targeting on such functional groups as an epoxide, hydroxyls, ketones, and olefins. A total of 10 derivatives have been prepared and their cytotoxicity against P388 murine leukemia cells and inhibitory activity of polypeptide elongation in yeast cell lysate provided some important SARs; the southern hemisphere comprises the pharmacophore, while the epoxide-bearing side chain is essential for the activity.
Original language | English |
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Pages (from-to) | 455-462 |
Number of pages | 8 |
Journal | Bioorganic and Medicinal Chemistry |
Volume | 13 |
Issue number | 2 |
DOIs | |
Publication status | Published - 2005 Jan 17 |
Externally published | Yes |
Keywords
- 13-Deoxytedanolide
- Antitumor
- Cytotoxicity
- Marine sponge-derived macrolide
- Protein synthesis inhibition
- SAR
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry