title: Design, synthesis, and biological evaluation of combretabenzodiazepines: a novel class of anti-tubulin agents.
abstract: In the present manuscript, starting from the 1,4-benzodiazepin-2-one nucleus, a privileged structure in medicinal chemistry, we have synthesized a novel class of cis-locked combretastatins named combreatabenzodiazepines. They show similar cytotoxic and antitubulin activity compared to combretastatin A-4 in neuroblastoma cells, showing a better pharmacokinetic profile. This class of compounds has therefore the potential for further development as antitubulin agents.
authors.affiliation: Dipartimento di Scienze del Farmaco, Università degli Studi del Piemonte Orientale "A. Avogadro" , Largo Donegani 2, 28100 Novara, Italy.
authors.forename: Ubaldina
authors.initials: U
authors.lastname: Galli
authors.forename: Cristina
authors.initials: C
authors.lastname: Travelli
authors.forename: Silvio
authors.initials: S
authors.lastname: Aprile
authors.forename: Elena
authors.initials: E
authors.lastname: Arrigoni
authors.forename: Simone
authors.initials: S
authors.lastname: Torretta
authors.forename: Giorgio
authors.initials: G
authors.lastname: Grosa
authors.forename: Alberto
authors.initials: A
authors.lastname: Massarotti
authors.forename: Giovanni
authors.initials: G
authors.lastname: Sorba
authors.forename: Pier Luigi
authors.initials: PL
authors.lastname: Canonico
authors.forename: Armando A
authors.initials: AA
authors.lastname: Genazzani
authors.forename: Gian Cesare
authors.initials: GC
authors.lastname: Tron
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001570:Benzodiazepinones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D018360:Crystallography, X-Ray; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014404:Tubulin / Q000378:metabolism*; D050257:Tubulin Modulators / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D001570:Benzodiazepinones; D014404:Tubulin; D050257:Tubulin Modulators