title: Synthesis and antitumor properties of 2,5-bis(3'-indolyl)thiophenes: analogues of marine alkaloid nortopsentin.
abstract: A series of 11 bis-indolylthiophenes of type 8-10 were obtained by cyclization of diketones 4 and 7 using Lawesson's reagent. Derivatives 8c, 9c, 9d, and 10c were selected to be evaluated in the full panel of about 60 human tumor cell lines derived from nine human cancer cell types and showed antiproliferative activity generally in the micromolar range. The most sensitive cell lines were: CCRF-CEM, MOLT-4, HL60 (TB), and RPMI-8226 of the leukemia subpanel, HT29 and HCC-2998 cell lines of the colon sub-panel, NCI-H522 of the non-small cell lung cancer sub-panel, LOX IMVI of the melanoma sub-panel, and UO-31 of the renal cancer sub-panel.
authors.affiliation: Dipartimento Farmacochimico Tossicologico e Biologico, Università degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy. diana@unipa.it
authors.forename: Patrizia
authors.initials: P
authors.lastname: Diana
authors.forename: Anna
authors.initials: A
authors.lastname: Carbone
authors.forename: Paola
authors.initials: P
authors.lastname: Barraja
authors.forename: Alessandra
authors.initials: A
authors.lastname: Montalbano
authors.forename: Annamaria
authors.initials: A
authors.lastname: Martorana
authors.forename: Gaetano
authors.initials: G
authors.lastname: Dattolo
authors.forename: Ornella
authors.initials: O
authors.lastname: Gia
authors.forename: Lisa
authors.initials: L
authors.lastname: Dalla Via
authors.forename: Girolamo
authors.initials: G
authors.lastname: Cirrincione
mesh_terms: D000470:Alkaloids; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004247:DNA; D004250:DNA Topoisomerases, Type II; D006801:Humans; D007093:Imidazoles / Q000737:chemistry; D007211:Indoles / Q000737:chemistry; D020128:Inhibitory Concentration 50; D013876:Thiophenes / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000470:Alkaloids; D000970:Antineoplastic Agents; D007093:Imidazoles; D007211:Indoles; D013876:Thiophenes; C413129:topsentin A; D004247:DNA; D004250:DNA Topoisomerases, Type II