1208459-96-4Relevant academic research and scientific papers
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.
INDOLO-SUBSTITUTED-PIPERIDINE COMPOUNDS AS ESTROGEN RECEPTOR DEGRADING AGENT
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Paragraph 0128, (2019/02/09)
Disclosed is a new indole compound, in particular, the compound as shown in formula (I), and a preparation method, pharmaceutical composition and use thereof as an estrogen receptor down-regulator in preparing drugs for treating estrogen receptor-positive breast cancer.
NOVEL 3-INDOL SUBSTITUTED DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USE
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Page/Page column 74; 75, (2016/10/04)
A compound of Formula I is provided: or pharmaceutically acceptable enantiomers, salts or solvates thereof. The 5 invention further relates to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also 10 relates to a process for manufacturing compounds of Formula I.
Bismuth Acetate as a Catalyst for the Sequential Protodeboronation of Di- and Triborylated Indoles
Shen, Fangyi,Tyagarajan, Sriram,Perera, Damith,Krska, Shane W.,Maligres, Peter E.,Smith, Milton R.,Maleczka, Robert E.
supporting information, p. 1554 - 1557 (2016/05/02)
Bismuth(III) acetate is a safe, inexpensive, and selective facilitator of sequential protodeboronations, which when used in conjunction with Ir-catalyzed borylations allows access to a diversity of borylated indoles. The versatility of combining Ir-catalyzed borylations with Bi(III)-catalyzed protodeboronation is demonstrated by selectively converting 6-fluoroindole into products with Bpin groups at the 4-, 5-, 7-, 2,7-, 4,7-, 3,5-, and 2,4,7-positions and the late-stage functionalization of sumatriptan.
