Dong, Junmin published the artcileDesign, synthesis and biological evaluation of exiguamine A analogues as IDO1 inhibitors, Computed Properties of 86-51-1, the main research area is exiguamine A preparation SAR mol docking antitumor indoleamine dioxygenase; Cancer immunotherapy; Exiguamine A; Indoleamine 2,3-dioxygenase 1.
A series of exiguamine A analogs were designed and synthesized via 15 steps. Their inhibitory activities against IDO1 were tested and the structure-activity relationships were studied. Most compounds exhibited potent IDO1 inhibitory activities with IC50 values at the level of 10-7-10-8 M. Compound I was the most potent IDO1 inhibitor with an IC50 value of 65.3 nM, which was comparable with the pos. control drug epacadostat (IC50 = 46 nM). Moreover, compound I showed higher selectivity for IDO1 over tryptophan 2,3-dioxygenase (TDO) and no cytotoxicity at its effective concentration, rending it justifiable for further optimization and evaluation.
European Journal of Medicinal Chemistry published new progress about Antitumor agents. 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, Computed Properties of 86-51-1.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem