A General Approach to the Synthesis of Polyamine Linked-Monoindolylmaleimides, a New Series of Trypanothione Reductase Inhibitors

Laurence SALMON; Valerie LANDRY; Oleg MELNYK; Louis MAES; Christian SERGHERAERT; Elisabeth DAVIOUD-CHARVET

doi:10.1248/cpb.46.707

Laurence SALMON, Valerie LANDRY, Oleg MELNYK, Louis MAES, Christian SERGHERAERT, Elisabeth DAVIOUD-CHARVET

著者情報

キーワード: trypanosomatid, trypanothione reductase, polyamine, N-alkylmaleimide, 2-alkylamino-3-(indol-3-yl)maleimide, protein kinase C

ジャーナルフリー

1998 年 46 巻 4 号 p. 707-710

DOI https://doi.org/10.1248/cpb.46.707

詳細

抄録

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.

責任著者(Corresponding author)

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