Carborane-containing hydroxyamidine scaffolds as novel inhibitors of indoleamine 2,3-Dioxygenase 1 (IDO1)

Journal article

Austin, Christopher J. D., Moir, Michael, Kahlert, Jan, Smith, Jason R., Jamie, Joanne F., Kassiou, Michael and Rendina, Louis M.. (2015). Carborane-containing hydroxyamidine scaffolds as novel inhibitors of indoleamine 2,3-Dioxygenase 1 (IDO1). Australian Journal of Chemistry. 68(12), pp. 1866 - 1870. https://doi.org/10.1071/CH15489
AuthorsAustin, Christopher J. D., Moir, Michael, Kahlert, Jan, Smith, Jason R., Jamie, Joanne F., Kassiou, Michael and Rendina, Louis M.
Abstract

Two new carborane-containing hydroxyamidines were prepared as potential inhibitors of the indoleamine 2,3-dioxygenase 1 (IDO1) enzyme. One compound (3) displayed low micromolar (1.90 μM) inhibition of IDO1, with the related compound (4) displaying >5-fold lower inhibitory activity, i.e. subtle differences in structure between the two carborane compounds led to dramatic changes in inhibitor binding. In silico docking experiments unravel a possible molecular mechanism that is consistent with the observed difference in IDO1 binding for 3 and 4 and also for the phenyl bioisosteres 1 and 2.

Year2015
JournalAustralian Journal of Chemistry
Journal citation68 (12), pp. 1866 - 1870
PublisherCSIRO Publishing
ISSN0004-9425
Digital Object Identifier (DOI)https://doi.org/10.1071/CH15489
Scopus EID2-s2.0-84950256708
Page range1866 - 1870
Research GroupSchool of Behavioural and Health Sciences
Publisher's version
File Access Level
Controlled
Place of publicationAustralia
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https://acuresearchbank.acu.edu.au/item/85zww/carborane-containing-hydroxyamidine-scaffolds-as-novel-inhibitors-of-indoleamine-2-3-dioxygenase-1-ido1

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