title: Anti-cancer activities of pyrazolo[1,5-a]indole derivatives.
abstract: The structure activity relationship (SAR) in the anti-cancer activities of pyrazolo[1,5-a]indole derivatives was investigated, and the following conclusions were obtained: 1) N(1)-quaternarization is essential for anti-cancer activity, 2) the size and polarity of the 2-substituent is crucial for in vitro activity which allows further investigation in an in vivo test, 3) the effect of the 4-substituent on the activity is minor compared with the other two factors.
authors.affiliation: Niigata College of Pharmacy, Japan. katayama@niigata-pharm.ac.jp
authors.forename: H
authors.initials: H
authors.lastname: Katayama
authors.forename: Y
authors.initials: Y
authors.lastname: Kiryu
authors.forename: K
authors.initials: K
authors.lastname: Kaneko
authors.forename: R
authors.initials: R
authors.lastname: Ohshima
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D007211:Indoles