Synthesis and biological activity of new functionalized epothilones for prodrug design and tumor targeting

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

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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:

17 Mar 2015 19:14

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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