Issue 4, 2012

Novel candesartan derivatives as indoleamine 2,3-dioxygenase inhibitors

Abstract

IDO is considered a promising therapeutic target for immunological cancer treatment. We found that the antihypertensive agent candesartan cilexetil inhibits IDO. The structural modifications provided a >10-fold more potent inhibitor. Structure–activity relationship and docking studies suggested that candesartan analogues uniquely bind to the entrance of the active site in IDO, and not to the haem region. Analogue synthesis, kinetic analysis and cellular activity are also described herein.

Graphical abstract: Novel candesartan derivatives as indoleamine 2,3-dioxygenase inhibitors

Supplementary files

Article information

Article type
Concise Article
Submitted
04 Nov 2011
Accepted
08 Jan 2012
First published
10 Jan 2012

Med. Chem. Commun., 2012,3, 475-479

Novel candesartan derivatives as indoleamine 2,3-dioxygenase inhibitors

K. Matsuno, H. Yamazaki, Y. Isaka, K. Takai, Y. Unno, N. Ogo, Y. Ishikawa, S. Fujii, O. Takikawa and A. Asai, Med. Chem. Commun., 2012, 3, 475 DOI: 10.1039/C2MD00278G

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Spotlight

Advertisements