Austin Christopher J D, Kahlert Jan, Issa Fatiah, Reed John H, Smith Jason R, Ioppolo Joseph A, Ong Jennifer A, Jamie Joanne F, Hibbs David, Rendina Louis M
School of Chemistry, The University of Sydney, Sydney, NSW 2006, Australia.
Dalton Trans. 2014 Jul 28;43(28):10719-24. doi: 10.1039/c4dt00444b.
Indoleamine-2,3-dioxygenase-1 (IDO1) is a critical immunoregulatory enzyme responsible for the metabolism of tryptophan during inflammation and disease. Based upon a pyranonaphthoquinone framework, the first examples of indoleamine-2,3-dioxygenase-1 (IDO1) inhibitors containing a carborane cage are reported. The novel closo-1,2-carboranyl-N-pyranonaphthoquinone derivatives display low μM binding affinity for the human recombinant enzyme, with IC50 values ranging from 0.78 to 1.77 μM.
吲哚胺-2,3-双加氧酶-1（IDO1）是一种关键的免疫调节酶，在炎症和疾病过程中负责色氨酸的代谢。基于吡喃萘醌骨架，报道了首例含碳硼烷笼的吲哚胺-2,3-双加氧酶-1（IDO1）抑制剂。新型闭式-1,2-碳硼烷基-N-吡喃萘醌衍生物对重组人酶表现出低 microM结合亲和力，IC50值范围为0.78至1.77 μM。
