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
| Language | English |
|---|---|
| Pages | 40-49 |
| Number of pages | 10 |
| Journal | Australian Journal of Chemistry |
| Volume | 66 |
| Issue number | 1 |
| DOIs | |
| Publication status | Published - 2013 |
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Natural product-inspired pyranonaphthoquinone inhibitors of indoleamine 2,3-dioxygenase-1 (IDO-1)*. / Bridewell, David J A; Sperry, Jonathan; Smith, Jason R.; Kosim-Satyaputra, Priambudi; Ching, Lai Ming; Jamie, Joanne F.; Brimble, Margaret A.
In: Australian Journal of Chemistry, Vol. 66, No. 1, 2013, p. 40-49.Research output: Contribution to journal › Article › Research › peer-review
TY - JOUR
T1 - Natural product-inspired pyranonaphthoquinone inhibitors of indoleamine 2,3-dioxygenase-1 (IDO-1)*
AU - Bridewell, David J A
AU - Sperry, Jonathan
AU - Smith, Jason R.
AU - Kosim-Satyaputra, Priambudi
AU - Ching, Lai Ming
AU - Jamie, Joanne F.
AU - Brimble, Margaret A.
PY - 2013
Y1 - 2013
N2 - 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
AB - 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
UR - http://www.scopus.com/inward/record.url?scp=84872876505&partnerID=8YFLogxK
U2 - 10.1071/CH12393
DO - 10.1071/CH12393
M3 - Article
VL - 66
SP - 40
EP - 49
JO - Australian Journal of Chemistry
T2 - Australian Journal of Chemistry
JF - Australian Journal of Chemistry
SN - 0004-9425
IS - 1
ER -