title: Synthesis and antitumour activity of new derivatives of flavone-8-acetic acid (FAA). Part 2: Ring-substituted derivatives.
abstract: A range of 18 derivatives of flavone-8-acetic acid (FAA) with substituents on the 2-phenyl group have been prepared and their anti-tumour activity evaluated in vitro against a panel of human and murine tumour cell lines and in vivo against MAC 15A. There was no clear-cut relationship between in vitro and in vivo activity but the activity in each situation was found to be very sensitive to the precise substitution pattern with closely related isomers giving widely different activities. Some of the compounds, notably 10b,c,j, and r, were active in vivo and these require further studies in order to evaluate their potential for development.
authors.affiliation: School of Chemistry, University of St. Andrews, North Haugh, Fife, UK.
authors.forename: R A
authors.initials: RA
authors.lastname: Aitken
authors.forename: M C
authors.initials: MC
authors.lastname: Bibby
authors.forename: J A
authors.initials: JA
authors.lastname: Double
authors.forename: A L
authors.initials: AL
authors.lastname: Laws
authors.forename: R B
authors.initials: RB
authors.lastname: Ritchie
authors.forename: D W
authors.initials: DW
authors.lastname: Wilson
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D003110:Colonic Neoplasms / Q000188:drug therapy; D004354:Drug Screening Assays, Antitumor; D005419:Flavonoids / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D051379:Mice; D014407:Tumor Cells, Cultured / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D005419:Flavonoids; C049328:flavone acetic acid