Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
A General Approach to the Synthesis of Polyamine Linked-Monoindolylmaleimides, a New Series of Trypanothione Reductase Inhibitors
Laurence SALMONValerie LANDRYOleg MELNYKLouis MAESChristian SERGHERAERTElisabeth DAVIOUD-CHARVET
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1998 年 46 巻 4 号 p. 707-710

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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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© The Pharmaceutical Society of Japan
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