title: A general approach to the synthesis of polyamine linked-monoindolylmaleimides, a new series of trypanothione reductase inhibitors.
abstract: A simplified approach to the synthesis of 2-polyamine linked-monoindolylmaleimides has been achieved, leading to a new series of trypanothione reductase inhibitors. The conditions of access to N,2-bis(polyamine)-3-monoindolylmaleimides and N,N'-bis(monoindolylmaleimide) polyamines are described. Measured inhibitory activities towards trypanothione reductase from Tryanosoma cruzi show the importance of both aromatic moieties and polyamine chains for trypanothione reductase recognition.
authors.affiliation: Institut de Biologie de Lille-Institut Pasteur de Lille-URA CNRS 1309, France.
authors.forename: L
authors.initials: L
authors.lastname: Salmon
authors.forename: V
authors.initials: V
authors.lastname: Landry
authors.forename: O
authors.initials: O
authors.lastname: Melnyk
authors.forename: L
authors.initials: L
authors.lastname: Maes
authors.forename: C
authors.initials: C
authors.lastname: Sergheraert
authors.forename: E
authors.initials: E
authors.lastname: Davioud-Charvet
mesh_terms: D000818:Animals; D004791:Enzyme Inhibitors / Q000138:chemical synthesis; D007211:Indoles / Q000138:chemical synthesis; D008301:Maleimides / Q000138:chemical synthesis; D009247:NADH, NADPH Oxidoreductases / Q000037:antagonists & inhibitors*; D011073:Polyamines / Q000138:chemical synthesis*; D014345:Trypanosoma / Q000201:enzymology
chemical_list: D004791:Enzyme Inhibitors; D007211:Indoles; D008301:Maleimides; D011073:Polyamines; C043592:maleimide; D009247:NADH, NADPH Oxidoreductases; C049608:trypanothione reductase