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Indoleamine 2,3-dioxygenase inhibitory activity of derivatives of marine alkaloid tsitsikammamine A
Dolusic, E.; Larrieu, P.; Meinguet, C.; Colette, D.; Rives, A.; Blanc, S.; Ferain, T.; Pilotte, L.; Stroobant, V.; Wouters, J.; van den Eynde, B.; Masereel, B.; Delfourne, E.; Frederick, R. (2013). Indoleamine 2,3-dioxygenase inhibitory activity of derivatives of marine alkaloid tsitsikammamine A. Bioorg. Med. Chem. Lett. 23(1): 47-54.
In: Bioorganic & Medicinal Chemistry Letters. Elsevier: Amsterdam. ISSN 0960-894X; e-ISSN 1464-3405, more
Peer reviewed article  

Available in  Authors 
    VLIZ: Open Repository 292079 [ OMA ]

Author keywords
    Pyrroloiminoquinones; Tsitsikammamines; Indoleamine 2,3-dioxygenase;Cancer immunology; Molecular modeling

Authors  Top 
  • Dolusic, E.
  • Larrieu, P.
  • Meinguet, C.
  • Colette, D.
  • Rives, A.
  • Blanc, S.
  • Ferain, T.
  • Pilotte, L.
  • Stroobant, V.
  • Wouters, J.
  • van den Eynde, B.
  • Masereel, B.
  • Delfourne, E.
  • Frederick, R.

    Tsitsikammamines are marine alkaloids whose structure is based on the pyrroloiminoquinone scaffold. These and related compounds have attracted attention due to various interesting biological properties, including cytotoxicity, topoisomerase inhibition, antimicrobial, antifungal and antimalarial activity. Indoleamine 2,3-dioxygenase (IDO1) is a well-established therapeutic target as an important factor in the tumor immune evasion mechanism. In this preliminary communication, we report the inhibitory activity of tsitsikammamine derivatives against IDO1. Tsitsikammamine A analogue 11b displays submicromolar potency in an enzymatic assay. A number of derivatives are also active in a cellular assay while showing little or no activity towards tryptophan 2,3-dioxygenase (TDO), a functionally related enzyme. This IDO1 inhibitory activity is rationalized by molecular modeling studies. An interest is thus established in this class of compounds as a potential source of lead compounds for the development of new pharmaceutically useful IDO1 inhibitors.

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