886049-61-2Relevant articles and documents
Rational Design of Original Fused-Cycle Selective Inhibitors of Tryptophan 2,3-Dioxygenase
Kozlova, Arina,Thabault, Léopold,Liberelle, Maxime,Klaessens, Simon,Prévost, Julien R. C.,Mathieu, Caroline,Pilotte, Luc,Stroobant, Vincent,Van Den Eynde, Beno?t,Frédérick, Rapha?l
supporting information, p. 10967 - 10980 (2021/08/24)
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.
Optimisation of a novel series of selective CNS penetrant CB2 agonists
Watson, Christine,Owen, Dafydd R.,Harding, Denise,Kon-I, Kana,Lewis, Mark L.,Mason, Helen J.,Matsumizu, Miyako,Mukaiyama, Takasuke,Rodriguez-Lens, Margarita,Shima, Akiko,Takeuchi, Mifune,Tran, Isabelle,Young, Tim
scheme or table, p. 4284 - 4287 (2011/08/06)
A series of benzimidazole CB2 receptor agonists were prepared and their properties investigated. Optimisation of the three benzimidazole substituents led to the identification of compound 23, a potent CB2 full agonist (EC50/sub
N-SUBSTITUTED SATURATED HETEROCYCLIC SULFONE COMPOUNDS WITH CB2 RECEPTOR AGONISTIC ACTIVITY
-
Page/Page column 53, (2010/08/08)
This invention relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X, R1, R2,R3, R4, R5, R6, R7, k, m, n, p, q, r and s are each as described herein, and compositions containing such compounds, and the use of such compounds in the treatment of a condition mediated by CB2 receptor activity.