title: Antitumor activity and COMPARE analysis of bis-indole derivatives.
abstract: This paper reports the synthesis of new derivatives (formed by two indole systems separated by a central moiety) analogous of potent antitumor agents previously described. The activity of the bis-indoles bearing a pyridine core confirms the good result described in the previous paper and compound 4c was chosen for the first in vivo experiment (Hollow Fiber Assay). COMPARE analysis and structure-activity relationships were also considered. Contrary to data reported by other Authors, no correlations were found between antitumor activity and NQO1 induction.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Bologna, Via Belmeloro 6, 40126 Bologna, Italy. aldo.andreani@unibo.it
authors.forename: Aldo
authors.initials: A
authors.lastname: Andreani
authors.forename: Silvia
authors.initials: S
authors.lastname: Burnelli
authors.forename: Massimiliano
authors.initials: M
authors.lastname: Granaiola
authors.forename: Alberto
authors.initials: A
authors.lastname: Leoni
authors.forename: Alessandra
authors.initials: A
authors.lastname: Locatelli
authors.forename: Rita
authors.initials: R
authors.lastname: Morigi
authors.forename: Mirella
authors.initials: M
authors.lastname: Rambaldi
authors.forename: Lucilla
authors.initials: L
authors.lastname: Varoli
authors.forename: Laura
authors.initials: L
authors.lastname: Landi
authors.forename: Cecilia
authors.initials: C
authors.lastname: Prata
authors.forename: Francesco Vieceli
authors.initials: FV
authors.lastname: Dalla Sega
authors.forename: Cristiana
authors.initials: C
authors.lastname: Caliceti
authors.forename: Robert H
authors.initials: RH
authors.lastname: Shoemaker
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D007211:Indoles