Synthesis and biological evaluation of epothilone A dimeric compounds

Passarella, Daniele; Comi, Daniela; Cappelletti, Graziella; Cartelli, Daniele; Gertsch, Juerg; Quesada, Ana R; Borlak, Jurgen; Altmann, Karl-Heinz (2009). Synthesis and biological evaluation of epothilone A dimeric compounds. Bioorganic & medicinal chemistry, 17(21), pp. 7435-40. Amsterdam: Elsevier 10.1016/j.bmc.2009.09.032

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The preparation and biological evaluation of a novel series of dimeric epothilone A derivatives (1-6) are described. Two types of diacyl spacers were introduced to establish the various dimeric epothilone A constructs. The effect of these compounds on tubulin polymerization and their cytotoxicity against four different cancer cell lines are reported. Several of the newly synthesized compounds inhibit endothelial cell differentiation and endothelial cell migration that are key steps of the angiogenic process.

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:

0968-0896

Publisher:

Elsevier

Language:

English

Submitter:

Factscience Import

Date Deposited:

04 Oct 2013 15:12

Last Modified:

04 May 2014 23:23

Publisher DOI:

10.1016/j.bmc.2009.09.032

PubMed ID:

19804980

Web of Science ID:

000270903100004

URI:

https://boris.unibe.ch/id/eprint/31617 (FactScience: 196248)

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