title: Antitrypanosomal activities of tryptanthrins.
abstract: New drugs and molecular targets are needed against Trypanosoma brucei, the protozoan that causes African sleeping sickness. Tryptanthrin (indolo[2,1-b]quinazoline-6,12-dione), a traditional antifungal agent, and 11 analogs were tested against T. brucei in vitro. The greatest activity was conferred by electron-withdrawing groups in the 8 position of the tryptanthrin ring system; the most potent compound had a 50% effective concentration of 0.40 microM.
authors.affiliation: Department of Chemistry, Bucknell University, Lewisburg, Pennsylvania 17837, USA.
authors.forename: John
authors.initials: J
authors.lastname: Scovill
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Blank
authors.forename: Michael
authors.initials: M
authors.lastname: Konnick
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Nenortas
authors.forename: Theresa
authors.initials: T
authors.lastname: Shapiro
mesh_terms: D000818:Animals; D002478:Cells, Cultured; D006801:Humans; D011799:Quinazolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D014346:Trypanosoma brucei brucei / Q000187:drug effects
chemical_list: D011799:Quinazolines; D014344:Trypanocidal Agents; C046243:tryptanthrine