title: Remarkable influence of the aromatic substructure in 9-methoxystrobilurin derivatives on their antifungal activity.
abstract: 9-Methoxystrobilurin-type beta-methoxyacrylate antibiotics (MOSBs) having various aromatic substructures were synthesized. The antifungal activity of the synthesized MOSBs against pathogenic and non-pathogenic fungi was examined, and the obtained results revealed that the antifungal activity of MOSBs was highly dependent on the aromatic substructures. However, no significant correlation was observed between cytotoxicity against human fibroblasts-like cell line and their structural properties. In addition, our results suggested that the strong growth-inhibitory activity of 9-methoxystrobilurin K against human-derived cell lines should be related to its hindered ether-type substructure.
authors.affiliation: Faculty of Pharmaceutical Sciences, Tokyo University of Science, 12 Ichigayafunagawara-machi, Shinjuku-ku, Tokyo, Japan.
authors.forename: Hiromi
authors.initials: H
authors.lastname: Uchiro
authors.forename: Koh
authors.initials: K
authors.lastname: Nagasawa
authors.forename: Tomohiro
authors.initials: T
authors.lastname: Sawa
authors.forename: Daiju
authors.initials: D
authors.lastname: Hasegawa
authors.forename: Tomoya
authors.initials: T
authors.lastname: Kotake
authors.forename: Yoshitsugu
authors.initials: Y
authors.lastname: Sugiura
authors.forename: Susumu
authors.initials: S
authors.lastname: Kobayashi
authors.forename: Kazuhiko
authors.initials: K
authors.lastname: Otoguro
authors.forename: Satoshi
authors.initials: S
authors.lastname: Omura
mesh_terms: D000179:Acrylates / Q000737:chemistry* / Q000494:pharmacology*; D000935:Antifungal Agents / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D004148:Dioxolanes / Q000737:chemistry* / Q000494:pharmacology*; D015195:Drug Design; D005658:Fungi / Q000187:drug effects; D006801:Humans; D007202:Indicators and Reagents; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship
chemical_list: C101803:9-methoxystrobilurin E; D000179:Acrylates; D000935:Antifungal Agents; D004148:Dioxolanes; D007202:Indicators and Reagents