Abstract
| Original language | French |
|---|---|
| Title of host publication | Oral Communication, 25èmes Journées Franco-belges de Pharmacochimie, 19-20/05/11, Liège |
| Subtitle of host publication | De la conception à la réalisation en pharmacochimie |
| Pages | 22-22 |
| Number of pages | 1 |
| Volume | OC10 |
| Publication status | Published - 2011 |
| Event | JFB 2011. - Liege, Belgium Duration: 19 May 2011 → … |
Conference
| Conference | JFB 2011. |
|---|---|
| Country | Belgium |
| City | Liege |
| Period | 19/05/11 → … |
Cite this
}
Indoleamine 2,3-Dioxygenase Inhibitory Activity of Derivatives of Marine Alkaloid Tsitsikammamine A. / Dolusic, Eduard; Larrieu, Pierre; Colette, Delphine; Blanc, Sébastien; Rives, Arnaud; Fraser, Graeme; Wouters, Johan; Kiss, Robert; Van den Eynde, Benoît; Masereel, Bernard; Delfourne, Evelyne; Frédérick, Raphaël.
Oral Communication, 25èmes Journées Franco-belges de Pharmacochimie, 19-20/05/11, Liège: De la conception à la réalisation en pharmacochimie. Vol. OC10 2011. p. 22-22.Research output: Contribution in Book/Catalog/Report/Conference proceeding › Conference contribution
TY - GEN
T1 - Indoleamine 2,3-Dioxygenase Inhibitory Activity of Derivatives of Marine Alkaloid Tsitsikammamine A
AU - Dolusic, Eduard
AU - Larrieu, Pierre
AU - Colette, Delphine
AU - Blanc, Sébastien
AU - Rives, Arnaud
AU - Fraser, Graeme
AU - Wouters, Johan
AU - Kiss, Robert
AU - Van den Eynde, Benoît
AU - Masereel, Bernard
AU - Delfourne, Evelyne
AU - Frédérick, Raphaël
PY - 2011
Y1 - 2011
N2 - Tsitsikammamines belonging to the pyrroloiminoquinone class of marine alkaloids were first isolated and characterized in 1996 from a Latrunculiidae sponge collected in the Tsitsikamma Marine Reserve of South Africa.[1] These and related compounds have attracted attention due to various interesting biological properties, including cytotoxicity, topoisomerase inhibition, antimicrobial and antifungal activity.[2] Recently, two novel regioisomeric series of tsitsikammamine A analogues were described.[3] The products were evaluated in an in vitro antiproliferative test against several cancer and normal (fibroblast) cell lines. This work allowed identifying a cytotoxic synthetic intermediate 1 with an unknown mechanism of action. Indoleamine 2,3-dioxygenase (IDO) was identified as an important factor in the tumor immune evasion mechanism. It was demonstrated that many human tumors express IDO in a constitutive manner.[4] Our groups recently published several articles on the development of new series of IDO inhibitors.[5] Here, we would like to report for the first time on an inhibitory activity of tsitsikammamine derivatives against IDO. Tsitsikammamine A analogue 2 displays submicromolar potency in an enzymatic test. A number of derivatives are also moderately active in a cellular test, establishing interest in this class of compounds as a potential source of leads for the development of new pharmaceutically useful IDO inhibitors.
AB - Tsitsikammamines belonging to the pyrroloiminoquinone class of marine alkaloids were first isolated and characterized in 1996 from a Latrunculiidae sponge collected in the Tsitsikamma Marine Reserve of South Africa.[1] These and related compounds have attracted attention due to various interesting biological properties, including cytotoxicity, topoisomerase inhibition, antimicrobial and antifungal activity.[2] Recently, two novel regioisomeric series of tsitsikammamine A analogues were described.[3] The products were evaluated in an in vitro antiproliferative test against several cancer and normal (fibroblast) cell lines. This work allowed identifying a cytotoxic synthetic intermediate 1 with an unknown mechanism of action. Indoleamine 2,3-dioxygenase (IDO) was identified as an important factor in the tumor immune evasion mechanism. It was demonstrated that many human tumors express IDO in a constitutive manner.[4] Our groups recently published several articles on the development of new series of IDO inhibitors.[5] Here, we would like to report for the first time on an inhibitory activity of tsitsikammamine derivatives against IDO. Tsitsikammamine A analogue 2 displays submicromolar potency in an enzymatic test. A number of derivatives are also moderately active in a cellular test, establishing interest in this class of compounds as a potential source of leads for the development of new pharmaceutically useful IDO inhibitors.
M3 - Article dans les actes d'une conférence/un colloque
VL - OC10
SP - 22
EP - 22
BT - Oral Communication, 25èmes Journées Franco-belges de Pharmacochimie, 19-20/05/11, Liège
ER -