Indol-2-yl ethanones as novel indoleamine 2,3-dioxygenase (IDO) inhibitors

Indol-2-yl ethanones as novel indoleamine 2,3-dioxygenase (IDO) inhibitors.

Indoleamine 2,3-dioxygenase (IDO) is a heme dioxygenase which has been shown to be involved in the pathological immune escape of diseases such as cancer. The synthesis and structure-activity relationships (SAR) of a novel series of IDO inhibitors based on the indol-2-yl ethanone scaffold is described. In vitro and in vivo biological activities have been evaluated, leading to compounds with IC(5...

IDO 2 ( indoleamine 2 , 3 - dioxygenase 2 )

Discovery and preliminary SARs of keto-indoles as novel indoleamine 2,3-dioxygenase (IDO) inhibitors.

Indoleamine 2,3-dioxygenase (IDO) is an important new therapeutic target for the treatment of cancer. With the aim of discovering novel IDO inhibitors, a virtual screen was undertaken and led to the discovery of the keto-indole derivative 1a endowed with an inhibitory potency in the micromolar range. Detailed kinetics were performed and revealed an uncompetitive inhibition profile. Preliminary ...

Cyclooxygenase-2 (COX-2) Inhibitors Reduce Immune Tole- rance through Indoleamine 2,3-dioxygenase (IDO)

Purpose: Cyclooxygenase-2 (COX-2) and its metabolite, PGE2 affect multiple tumorigenesis, including angiogenesis, invasion, and tumor-induced immune suppression. Their overexpression is association with impaired immune cell function in many tumors. Indoleamine 2,3-dioxygenase (IDO) is an emerging immuno-regulatory enzyme that can catalyze the initial rate-limiting step in tryptophan catabolism,...

Indoleamine 2,3-dioxygenase (ido) and Immune Tolerance

The IDO facilitates immune tolerance and is one of the main actors involved in the inhibition of cell proliferation, including activated T cells. IDO induces production of reactive oxygen species (ROS) and nitric oxide (NO) radicals. Several pathways involved in the regulation of immune response are regulated by redox mechanisms. Reactive oxygen and nitrogen species (ROSRNS) and other redox act...