title: Synthesis and biological evaluation of paclitaxel-thiocolchicine hybrids.
abstract: The bifunctional taxoid-colchicinoid hybrids 6-8 were synthesized and evaluated in assays of cytotoxicity and tubulin assembly/disassembly. All compounds showed a high degree of cytotoxicity, but, while 6 and 7 behaved as bifunctional tubulin binders not unlike an equimolecular mixture of taxol and thiocolchicine, 8 was surprisingly devoid of tubulin activity, acting on a distinct and yet to identify molecular target.
authors.affiliation: Dipartimento di Chimica Organica e Industriale, Università degli Studi di Milano, Via Venezian 21, I-20133 Milano. bruno.danieli@unimi.it
authors.forename: Bruno
authors.initials: B
authors.lastname: Danieli
authors.forename: Alessandra
authors.initials: A
authors.lastname: Giardini
authors.forename: Giordano
authors.initials: G
authors.lastname: Lesma
authors.forename: Daniele
authors.initials: D
authors.lastname: Passarella
authors.forename: Alessandra
authors.initials: A
authors.lastname: Silvani
authors.forename: Giovanni
authors.initials: G
authors.lastname: Appendino
authors.forename: Alain
authors.initials: A
authors.lastname: Noncovich
authors.forename: Gabriele
authors.initials: G
authors.lastname: Fontana
authors.forename: Ezio
authors.initials: E
authors.lastname: Bombardelli
authors.forename: Olov
authors.initials: O
authors.lastname: Sterner
mesh_terms: D000818:Animals; D000971:Antineoplastic Combined Chemotherapy Protocols / Q000138:chemical synthesis / Q000494:pharmacology; D002417:Cattle; D045744:Cell Line, Tumor; D003078:Colchicine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D006801:Humans; D008870:Microtubules / Q000187:drug effects / Q000502:physiology; D017239:Paclitaxel / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: C014856:thiocholchicine; D017239:Paclitaxel; D003078:Colchicine