Chemical synthesis and biological evaluation of palmerolide A analogues
| Autor: | Chek Shik Lim, Ramakrishna Guduru, Ya-Ping Sun, David Y.-K. Chen, Dattatraya H. Dethe, Kyriacos C. Nicolaou, Gulice Y. C. Leung |
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| Rok vydání: | 2008 |
| Předmět: |
Antitumor activity
Adenosine Triphosphatases Natural product Chemistry Stereochemistry Substituent General Chemistry Polyenes Biochemistry Combinatorial chemistry Chemical synthesis Amides Catalysis chemistry.chemical_compound Structure-Activity Relationship Colloid and Surface Chemistry Cell Line Tumor Side chain Structure–activity relationship Humans Macrolides Drug Screening Assays Antitumor Enzyme Inhibitors Biological evaluation |
| Zdroj: | Journal of the American Chemical Society. 130(30) |
| ISSN: | 1520-5126 |
| Popis: | Molecular design and chemical synthesis of several palmerolide A analogues allowed the first structure activity relationships (SARs) of this newly discovered marine antitumor agent. From several analogues synthesized and tested (ent- 1, 5- 14, 21- 26, 50, 51), compounds 25 (with a phenyl substituent on the side chain) and 51 (lacking the C-7 hydroxyl group) were the most interesting, exhibiting approximately a 10-fold increase in potency and equipotency, respectively, to the natural product. These findings point the way to more focused structure activity relationship studies. |
| Databáze: | OpenAIRE |
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