IDO1 and TDO inhibitory evaluation of analogues of the marine pyrroloiminoquinone alkaloids: Wakayin and Tsitsikammamines

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