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Indoleamine 2,3-dioxygenase (IDO1) and tryptophane 2,3-dioxygenase (TDO) are two heme-containing enzymes which catalyze the conversion of tryptophan to N-formylkynurenine. Both enzymes are well establish therapeutic targets as important factors in the tumor immune evasion mechanism. A number of analogues of the marine pyrroloquinoline alkaloids tsitsikammamines or wakayin have been synthesized, two of them were synthesized using an original method to build the bispyrroloquinone framework. All the derivatives were evaluated in a cellular assay for their capacity to inhibit the enzymes. Six compounds have shown a significant potency on HEK 293-EBNA cell lines expressing hIDO1 or hTDO.

Original publication

DOI

10.1016/j.bmcl.2021.127910

Type

Journal article

Journal

Bioorganic & medicinal chemistry letters

Publication Date

10/03/2021

Volume

40

Addresses

Université Paul Sabatier, UMR CNRS 5068, Laboratoire de Synthèse et Physicochimie de Molécules d'Intérêt Biologique, 118 Route de Narbonne, 31062 Toulouse Cédex 9, France.