title: Primary anti-proliferative activity evaluation of 1-(quinolizidin-1'-yl)methyl- and 1-(ω-tert-amino)alkyl-substituted 2-phenyl-, 2-benzyl- and 2-[(benzotriazol-1/2-yl)methyl]benzimidazoles on human cancer cell lines.
abstract: Twenty benzimidazole derivatives bearing in position 1 a ([Formula: see text]-tert-amino)alkyl chain (mainly quinolizidin-1-ylmethyl) and in position 2 an aromatic moiety (phenyl, benzyl or benzotriazol-1/2-ylmethyl) were evaluated at the National Cancer Institute (NCI) for anti-proliferative activity against a panel of 60 human cancer cell lines. Four compounds (6, 7, 9 and 10) displayed a large spectrum of activity with [Formula: see text] 10 [Formula: see text] on 24-57 cell lines, while thirteen compounds exhibited sub-micromolar or even nanomolar activity against single cell lines, such as leukemia CCRF-CEM, HL-60 and MOLT-4, CNS cancer SF-268 and, particularly, renal cancer UO-31, sometimes with outstanding selectivity (compounds 5-7, 11, 13 and 18).
authors.affiliation: Dipartimento di Farmacia, Università di Genova, Viale Benedetto XV 3, 16132 , Genoa, Italy. michele.tonelli@unige.it
authors.forename: Michele
authors.initials: M
authors.lastname: Tonelli
authors.forename: Bruno
authors.initials: B
authors.lastname: Tasso
authors.forename: Lorenzo
authors.initials: L
authors.lastname: Mina
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Paglietti
authors.forename: Vito
authors.initials: V
authors.lastname: Boido
authors.forename: Fabio
authors.initials: F
authors.lastname: Sparatore
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D001562:Benzimidazoles / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy; D054837:Quinolizidines / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D001562:Benzimidazoles; D054837:Quinolizidines