Kozlova, Arina; Thabault, Leopold; Liberelle, Maxime; Klaessens, Simon; Prevost, Julien R. C.; Mathieu, Caroline; Pilotte, Luc; Stroobant, Vincent; Van den Eynde, Benoit; Frederick, Raphael published the artcile< Rational Design of Original Fused-Cycle Selective Inhibitors of Tryptophan 2,3-Dioxygenase>, Recommanded Product: 6-Bromo-3H-[1,2,3]triazolo[4,5-b]pyridine, the main research area is tumor rejection TDO2 inhibitor rational design scaffold structural modulations.
Tryptophan 2,3-dioxygenase (TDO2) is a heme-containing enzyme constitutively expressed at high concentrations in the liver and responsible for L-tryptophan (L-Trp) homeostasis. Expression of TDO2 in cancer cells results in the inhibition of immune-mediated tumor rejection due to an enhancement of L-Trp catabolism via the kynurenine pathway. In the study herein, we disclose a new 6-(1H-indol-3-yl)-benzotriazole scaffold of TDO2 inhibitors developed through rational design, starting from existing inhibitors. Rigidification of the initial scaffold led to the synthesis of stable compounds displaying a nanomolar cellular potency and a better understanding of the structural modulations that can be accommodated inside the active site of hTDO2.
Journal of Medicinal Chemistry published new progress about Catabolism (L-Trp). 92276-38-5 belongs to class triazoles, and the molecular formula is C5H3BrN4, Recommanded Product: 6-Bromo-3H-[1,2,3]triazolo[4,5-b]pyridine.
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics