Journal
AUSTRALIAN JOURNAL OF CHEMISTRY
Volume 68, Issue 12, Pages 1866-1870Publisher
CSIRO PUBLISHING
DOI: 10.1071/CH15489
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Funding
- Australian Research Council
- Prostate Cancer Foundation of Australia
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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 mu M) 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.
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