title: Synthesis, in vitro and in vivo cytotoxicity of 6,7-diaryl-2,3,8,8a-tetrahydroindolizin-5(1H)-ones.
abstract: A 6,7-diaryl-2,3,8,8a-tetrahydroindolizin-5(1H)-one library was constructed and tested against the colon cancer cell line HCT-116 as an initial screen for cytotoxic properties. Of this library, the parent compound, in which the southern aromatic ring remains unsubstituted, and the northern aromatic ring carries a 4-methoxy group, exhibited the most potent cytotoxicity with an IC50 value of 0.39 microM and displayed promising activity in vivo in the NCI's mouse hollow fiber assay.
authors.affiliation: Department of Medicinal Chemistry, University of Kansas, 1251 Wescoe Hall Drive, Lawrence, KS 66045, USA.
authors.forename: F Scott
authors.initials: FS
authors.lastname: Kimball
authors.forename: Ashok Rao
authors.initials: AR
authors.lastname: Tunoori
authors.forename: Samuel F
authors.initials: SF
authors.lastname: Victory
authors.forename: Dinah
authors.initials: D
authors.lastname: Dutta
authors.forename: Jonathan M
authors.initials: JM
authors.lastname: White
authors.forename: Richard H
authors.initials: RH
authors.lastname: Himes
authors.forename: Gunda I
authors.initials: GI
authors.lastname: Georg
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D006801:Humans; D007211:Indoles / Q000737:chemistry* / Q000494:pharmacology*; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D007211:Indoles