Chemical and Pharmaceutical Bulletin p. 707 - 710 (1998)
Update date:2022-08-11
Topics:
Salmon, Laurence
Landry, Valerie
Melnyk, Oleg
Maes, Louis
Sergheraert, Christian
Davioud-Charvet, Elisabeth
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.
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