title: Synthesis and biological evaluation of quinones derived from natural product komaroviquinone as anti-Trypanosoma cruzi agents.
abstract: Current chemotherapy drugs for Chagas' disease are insufficient due to their limited efficacy; however, anti-trypanosomal agents have recently shown promise. As such, synthetic intermediates of komaroviquinone were evaluated for anti-trypanosomal activity. Based on the results, a series of novel quinone derivatives were screened for anti-trypanosomal activity and mammalian cytotoxicity. Several quinone derivatives displayed higher antiprotozoal activity against Trypanosoma cruzi trypomastigotes than the reference drug benznidazole, without concomitant toxicity toward the host cell.
authors.affiliation: Faculty of Pharmacy, Takasaki University of Health and Welfare, Takasaki 370-0033, Japan. Electronic address: ysuto@takasaki-u.ac.jp.
authors.forename: Yutaka
authors.initials: Y
authors.lastname: Suto
authors.affiliation: Department of Molecular and Cellular Parasitology, Graduate School of Health Sciences, Gunma University, Maebashi 371-8514, Japan.
authors.forename: Junko
authors.initials: J
authors.lastname: Nakajima-Shimada
authors.affiliation: Faculty of Pharmacy, Takasaki University of Health and Welfare, Takasaki 370-0033, Japan.
authors.forename: Noriyuki
authors.initials: N
authors.lastname: Yamagiwa
authors.affiliation: Department of Molecular and Cellular Parasitology, Graduate School of Health Sciences, Gunma University, Maebashi 371-8514, Japan.
authors.forename: Yoko
authors.initials: Y
authors.lastname: Onizuka
authors.affiliation: Faculty of Pharmacy, Takasaki University of Health and Welfare, Takasaki 370-0033, Japan.
authors.forename: Genji
authors.initials: G
authors.lastname: Iwasaki
mesh_terms: D016475:3T3 Cells; D000818:Animals; D014355:Chagas Disease / Q000188:drug therapy* / Q000469:parasitology; D004224:Diterpenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D051379:Mice; D011809:Quinones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D014344:Trypanocidal Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects*
chemical_list: D004224:Diterpenes; D011809:Quinones; D014344:Trypanocidal Agents; C508550:komaroviquinone
keywords: Chagas’ disease; Quinone; Trypanosoma cruzi