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Issue 4, 2012
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Novel candesartan derivatives as indoleamine 2,3-dioxygenase inhibitors

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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

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Publication details

The article was received on 04 Nov 2011, accepted on 08 Jan 2012 and first published on 10 Jan 2012


Article type: Concise Article
DOI: 10.1039/C2MD00278G
Citation: Med. Chem. Commun., 2012,3, 475-479

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    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

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