title: Synthesis and biological evaluation of epothilone A dimeric compounds.
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.
authors.affiliation: Dipartimento di Chimica Organica e Industriale, Università degli Studi di Milano, Via Venezian 21, Italy. Daniele.Passarella@unimi.it
authors.forename: Daniele
authors.initials: D
authors.lastname: Passarella
authors.forename: Daniela
authors.initials: D
authors.lastname: Comi
authors.forename: Graziella
authors.initials: G
authors.lastname: Cappelletti
authors.forename: Daniele
authors.initials: D
authors.lastname: Cartelli
authors.forename: Juerg
authors.initials: J
authors.lastname: Gertsch
authors.forename: Ana R
authors.initials: AR
authors.lastname: Quesada
authors.forename: Jurgen
authors.initials: J
authors.lastname: Borlak
authors.forename: Karl-Heinz
authors.initials: KH
authors.lastname: Altmann
mesh_terms: D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D002454:Cell Differentiation; D045744:Cell Line, Tumor; D002465:Cell Movement; D019281:Dimerization; D004354:Drug Screening Assays, Antitumor; D042783:Endothelial Cells / Q000166:cytology; D034261:Epothilones / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D006801:Humans; D014404:Tubulin / Q000378:metabolism; D050257:Tubulin Modulators / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity
chemical_list: D020533:Angiogenesis Inhibitors; D034261:Epothilones; D014404:Tubulin; D050257:Tubulin Modulators; C093787:epothilone A