title: Novel carbazole and acyl-indole antimitotics.
abstract: In the course of our Heat Shock 90 program, certain carbazole compounds were identified which had an off-target antiproliferative activity. To understand the off-target activity, we studied one analog with strong activity. We discovered that it had an effect on tubulin polymerization kinetics and was competitive with colchicine. Additional analogs were made, and a number of potent compounds were identified.
authors.affiliation: thomas_e_barta@yahoo.com
authors.forename: Thomas E
authors.initials: TE
authors.lastname: Barta
authors.forename: Amy F
authors.initials: AF
authors.lastname: Barabasz
authors.forename: Briana E
authors.initials: BE
authors.lastname: Foley
authors.forename: Lifeng
authors.initials: L
authors.lastname: Geng
authors.forename: Steven E
authors.initials: SE
authors.lastname: Hall
authors.forename: Gunnar J
authors.initials: GJ
authors.lastname: Hanson
authors.forename: Matthew
authors.initials: M
authors.lastname: Jenks
authors.forename: Wei
authors.initials: W
authors.lastname: Ma
authors.forename: John W
authors.initials: JW
authors.lastname: Rice
authors.forename: James
authors.initials: J
authors.lastname: Veal
mesh_terms: D050256:Antimitotic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002227:Carbazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D003078:Colchicine / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D018841:HSP90 Heat-Shock Proteins / Q000378:metabolism; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D014404:Tubulin / Q000378:metabolism
chemical_list: D050256:Antimitotic Agents; D002227:Carbazoles; D018841:HSP90 Heat-Shock Proteins; D007211:Indoles; D014404:Tubulin; D003078:Colchicine