title: Symmetrical alpha-bromoacryloylamido diaryldienone derivatives as a novel series of antiproliferative agents. Design, synthesis and biological evaluation.
abstract: In a continuing study of hybrid compounds containing the alpha-bromoacryloyl moiety as potential anticancer drugs, we synthesized a novel series of hybrids 4a-h, in which this moiety was linked to a 1,5-diaryl-1,4-pentadien-3-one system. Many of the conjugates prepared (4b, 4c, 4e and 4g) demonstrated pronounced, submicromolar antiproliferative activity against four cancer cell lines. Moreover, compound 4b induced apoptosis through the mitochondrial pathway and activated caspase-3 in a concentration-dependent manner.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Ferrara, 44100 Ferrara, Italy. rmr@unife.it
authors.forename: Romeo
authors.initials: R
authors.lastname: Romagnoli
authors.forename: Pier Giovanni
authors.initials: PG
authors.lastname: Baraldi
authors.forename: Olga
authors.initials: O
authors.lastname: Cruz-Lopez
authors.forename: Carlota
authors.initials: C
authors.lastname: Lopez Cara
authors.forename: Maria Dora
authors.initials: MD
authors.lastname: Carrion
authors.forename: Jan
authors.initials: J
authors.lastname: Balzarini
authors.forename: Ernest
authors.initials: E
authors.lastname: Hamel
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Basso
authors.forename: Roberta
authors.initials: R
authors.lastname: Bortolozzi
authors.forename: Giampietro
authors.initials: G
authors.lastname: Viola
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D053148:Caspase 3 / Q000378:metabolism; D045744:Cell Line, Tumor; D047188:Chalcones / Q000737:chemistry*; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D051379:Mice
chemical_list: D000970:Antineoplastic Agents; D047188:Chalcones; D053148:Caspase 3