Dietrich, Silvia Anthoine; Riediker, Linda; Gertsch, Jürg; Altmann, Karl-Heinz (2010). Synthesis and biological activity of new functionalized epothilones for prodrug design and tumor targeting. CHIMIA, 64(3), pp. 136-9. Bern: Schweizerische Chemische Gesellschaft 10.2533/chimia.2010.136
Full text not available from this repository.Epothilones are potent antiproliferative agents, which have served as successful lead structures for anticancer drug discovery. However, their therapeutic efficacy would benefit greatly from an increase in their selectivity for tumor cells, which may be achieved through conjugation with a tumor-targeting moiety. Three novel epothilone analogs bearing variously functionalized benzimidazole side chains were synthesized using a strategy based on palladium-mediated coupling and macrolactonization. The synthesis of these compounds is described and their in vitro biological activity is discussed with respect to their interactions with the tubulin/microtubule system and the inhibition of human cancer cell proliferation. The additional functional groups may be used to synthesize conjugates of epothilone derivatives with a variety of tumor-targeting moieties.
Item Type: |
Journal Article (Original Article) |
|---|---|
Division/Institute: |
04 Faculty of Medicine > Pre-clinic Human Medicine > Institute of Biochemistry and Molecular Medicine |
UniBE Contributor: |
Gertsch, Jürg |
ISSN: |
0009-4293 |
Publisher: |
Schweizerische Chemische Gesellschaft |
Language: |
English |
Submitter: |
Factscience Import |
Date Deposited: |
04 Oct 2013 14:12 |
Last Modified: |
05 Dec 2022 14:01 |
Publisher DOI: |
10.2533/chimia.2010.136 |
PubMed ID: |
21140905 |
Web of Science ID: |
000276613600006 |
URI: |
https://boris.unibe.ch/id/eprint/2432 (FactScience: 204931) |
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