title: Synthesis and evaluation of a novel series of indoloisoquinolines as small molecule anti-malarial leads.
abstract: A group of novel synthetic indoloisoquinolines was prepared and its potential as a novel series of small-molecule anti-malarial leads was assessed. The structure-activity relationship on variation of three distinct regions of chemical space was investigated. A lead compound was generated with an activity close to that observed for a known anti-malarial natural product, dihydrousambarensine, that shares the indoloisoquinoline template structure.
authors.affiliation: School of Medicine, Keele University, UK.
authors.forename: Paul
authors.initials: P
authors.lastname: Horrocks
authors.forename: Samantha
authors.initials: S
authors.lastname: Fallon
authors.forename: Laura
authors.initials: L
authors.lastname: Denman
authors.forename: Oliver
authors.initials: O
authors.lastname: Devine
authors.forename: Liam J
authors.initials: LJ
authors.lastname: Duffy
authors.forename: Anthony
authors.initials: A
authors.lastname: Harper
authors.forename: Emma-Louise
authors.initials: EL
authors.lastname: Meredith
authors.forename: Sandra
authors.initials: S
authors.lastname: Hasenkamp
authors.forename: Adam
authors.initials: A
authors.lastname: Sidaway
authors.forename: Daniel
authors.initials: D
authors.lastname: Monnery
authors.forename: Theresa R
authors.initials: TR
authors.lastname: Phillips
authors.forename: Steven M
authors.initials: SM
authors.lastname: Allin
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D010963:Plasmodium falciparum / Q000187:drug effects*; D054852:Small Molecule Libraries; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D007211:Indoles; D007546:Isoquinolines; D054852:Small Molecule Libraries; C572310:dihydrousambarensine