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.
Synthesis and biological evaluation of epothilone A dimeric compounds / D. Passarella, D. Comi, G. Cappelletti, D. Cartelli, J. Gertsch, A. R. Quesada, J. Borlak, K.-H. Altmann. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - 17:21(2009 Nov), pp. 7435-7440.
Synthesis and biological evaluation of epothilone A dimeric compounds
D. Passarella;D. Comi;G. Cappelletti;D. Cartelli;
2009
Abstract
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.
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