Modular synthesis of polyene side chain analogues of the potent macrolide antibiotic etnangien by a flexible coupling strategy based on hetero-bis-metallated alkenes
An efficient procedure for the concise synthesis of hetero-bis-metallated alkenes as useful building blocks for the modular access to highly elaborate polyenes and stabilized analogues is reported. By applying these bifunctional olefins in convergent Stille/Suzuki-Miyaura couplings, novel, carefully...
Gespeichert in:
| 1. Verfasser: | |
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| Dokumenttyp: | Article (Journal) |
| Sprache: | Englisch |
| Veröffentlicht: |
2013
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| In: |
Organic & biomolecular chemistry
Year: 2012, Jahrgang: 11, Heft: 13, Pages: 2116-2139 |
| ISSN: | 1477-0539 |
| DOI: | 10.1039/c2ob26906f |
| Online-Zugang: | Verlag, Volltext: http://dx.doi.org/10.1039/c2ob26906f
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| Verfasserangaben: | Mario Altendorfer, Aruna Raja, Florenz Sasse, Herbert Irschik and Dirk Menche |
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| 520 | |a An efficient procedure for the concise synthesis of hetero-bis-metallated alkenes as useful building blocks for the modular access to highly elaborate polyenes and stabilized analogues is reported. By applying these bifunctional olefins in convergent Stille/Suzuki-Miyaura couplings, novel, carefully selected side chain analogues of the potent RNA polymerase inhibitor etnangien were synthesized by a modular late stage coupling strategy and evaluated for antibacterial and antiproliferative activities. | ||
| 534 | |c 2012 | ||
| 650 | 4 | |a Alkenes | |
| 650 | 4 | |a Animals | |
| 650 | 4 | |a Anti-Bacterial Agents | |
| 650 | 4 | |a Bacillus subtilis | |
| 650 | 4 | |a Cell Proliferation | |
| 650 | 4 | |a Cells, Cultured | |
| 650 | 4 | |a Corynebacterium | |
| 650 | 4 | |a DNA-Directed RNA Polymerases | |
| 650 | 4 | |a Dose-Response Relationship, Drug | |
| 650 | 4 | |a Enzyme Inhibitors | |
| 650 | 4 | |a Fibroblasts | |
| 650 | 4 | |a Macrolides | |
| 650 | 4 | |a Mice | |
| 650 | 4 | |a Microbial Sensitivity Tests | |
| 650 | 4 | |a Molecular Structure | |
| 650 | 4 | |a Organometallic Compounds | |
| 650 | 4 | |a Polyenes | |
| 650 | 4 | |a Structure-Activity Relationship | |
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