title: Mutasynthesis of fluorinated pactamycin analogues and their antimalarial activity.
abstract: A mutasynthetic strategy has been used to generate fluorinated TM-025 and TM-026, two biosynthetically engineered pactamycin analogues produced by Streptomyces pactum ATCC 27456. The fluorinated compounds maintain excellent activity and selectivity toward chloroquine-sensitive and multidrug-resistant strains of malarial parasites as the parent compounds. The results also provide insights into the biosynthesis of 3-aminobenzoic acid in S. pactum.
authors.affiliation: Department of Pharmaceutical Sciences, Oregon State University, Corvallis, Oregon 97331-3507, United States.
authors.forename: Khaled H
authors.initials: KH
authors.lastname: Almabruk
authors.forename: Wanli
authors.initials: W
authors.lastname: Lu
authors.forename: Yuexin
authors.initials: Y
authors.lastname: Li
authors.forename: Mostafa
authors.initials: M
authors.lastname: Abugreen
authors.forename: Jane X
authors.initials: JX
authors.lastname: Kelly
authors.forename: Taifo
authors.initials: T
authors.lastname: Mahmud
mesh_terms: D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002738:Chloroquine / Q000494:pharmacology; D004351:Drug Resistance / Q000187:drug effects; D018432:Drug Resistance, Multiple / Q000187:drug effects; D006845:Hydrocarbons, Fluorinated / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D010142:Pactamycin / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D010963:Plasmodium falciparum / Q000187:drug effects; D013302:Streptomyces / Q000737:chemistry / Q000235:genetics / Q000378:metabolism; D062368:meta-Aminobenzoates
chemical_list: D000962:Antimalarials; D006845:Hydrocarbons, Fluorinated; C583546:TM-025; C583545:TM-026; D062368:meta-Aminobenzoates; D010142:Pactamycin; D002738:Chloroquine; C044855:3-aminobenzoic acid