title: Synthesis of 5,6-dimethyl-9-methoxy-1-phenyl-6H-pyrido[4,3-b]carbazole derivatives and their cytotoxic activity.
abstract: Starting from 2-(6-methoxy-1-methyl-9H-carbazol-2-yl)ethylamine 7 and mixed anhydrides of 4-nitrobenzoic acid or 4-methoxybenzoic acid, the corresponding 5,6-dimethyl-9-methoxy-1-(4-substituted phenyl)-6H-pyrido[4,3-b]carbazoles 11a-b, 5,6-dimethyl-9-hydroxy-1-(4-substituted phenyl)-6H-pyrido[4,3-b]carbazoles 12a, 12c, and their quaternary salts 13a-d were obtained. The four new pyridocarbazole derivatives 12a-c and 13d satisfy the international activity criterion for synthetic compounds, namely an ID(50) value lower then 4 microg/mL in preliminary in vitro cytotoxic activity screening against the A549 cell line (non-small cell lung cancer).
authors.affiliation: Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, Wroclaw, Poland. howorko@bf.uni.wroc.pl
authors.forename: Ryszard
authors.initials: R
authors.lastname: Jasztold-Howorko
authors.forename: Marzena
authors.initials: M
authors.lastname: Pelczynska
authors.forename: Anna
authors.initials: A
authors.lastname: Nasulewicz
authors.forename: Joanna
authors.initials: J
authors.lastname: Wietrzyk
authors.forename: Adam
authors.initials: A
authors.lastname: Opolski
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002227:Carbazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D002227:Carbazoles