Natural product-inspired pyranonaphthoquinone inhibitors of indoleamine 2,3-dioxygenase-1 (IDO-1)*

David J A Bridewell, Jonathan Sperry, Jason R. Smith, Priambudi Kosim-Satyaputra, Lai Ming Ching, Joanne F. Jamie, Margaret A. Brimble*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

20 Citations (Scopus)

Abstract

A series of pyranonaphthoquinone derivatives possessing structural features present in both natural products annulin B and exiguamine A have been shown to exhibit low micromolar inhibition of indoleamine 2,3-dioxygenase-1 (IDO-1). These inhibitors retain activity against the enzyme in a cellular context with an approximate one-log loss of dose potency against IDO-1 in cells. One particular analogue, triazole 8 shows good inhibition of IDO-1 along with little loss of cell viability at low drug concentrations. These results have extended the naphthoquinone series of novel IDO-1 inhibitors based on lead compounds from nature. Journal compilation

Original languageEnglish
Pages (from-to)40-49
Number of pages10
JournalAustralian Journal of Chemistry
Volume66
Issue number1
DOIs
Publication statusPublished - 2013

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