title: Antimalarial and cytotoxic activities of chiral triamines.
abstract: Chiral triamine antimalarial compounds have been identified following the screening of mixture-based positional scanning libraries made up of 31,320 compounds against P. falciparum. The library, namely N-methyl triamine (TPI 762) was generated following exhaustive reduction of resin-bound acylated dipeptides. Using the PSCL approach, individual compounds were rapidly identified which were only 10 times less active than the standard drugs chloroquine (CQ) and Artemisinin (Artes).
authors.affiliation: Faculté de Pharmacie, Laboratoire de Pharmacologie Marine, 5000 Monastir, Tunisia.
authors.forename: Afef
authors.initials: A
authors.lastname: Dellai
authors.forename: Jon
authors.initials: J
authors.lastname: Appel
authors.forename: Abderrahman
authors.initials: A
authors.lastname: Bouraoui
authors.forename: Simon
authors.initials: S
authors.lastname: Croft
authors.forename: Adel
authors.initials: A
authors.lastname: Nefzi
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity*; D037621:Artemisinins / Q000494:pharmacology; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects*; D002738:Chloroquine / Q000494:pharmacology; D003500:Cyclization; D006801:Humans; D010963:Plasmodium falciparum / Q000187:drug effects*; D011073:Polyamines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity*; D054852:Small Molecule Libraries / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity
chemical_list: D000962:Antimalarials; D037621:Artemisinins; D011073:Polyamines; D054852:Small Molecule Libraries; D002738:Chloroquine; C031327:artemisinin
keywords: Antimalrial; Chiral amines; Libraries; Malaria; Mixtures based libraries; Parallel synthesis; Solid-phase organic synthesis