30886-24-9Relevant academic research and scientific papers
Interfering with the Tumor-Immune Interface: Making Way for Triazine-Based Small Molecules as Novel PD-L1 Inhibitors
Russomanno, Pasquale,Assoni, Giulia,Amato, Jussara,D'Amore, Vincenzo Maria,Scaglia, Riccardo,Brancaccio, Diego,Pedrini, Martina,Polcaro, Giovanna,La Pietra, Valeria,Orlando, Paolo,Falzoni, Marianna,Cerofolini, Linda,Giuntini, Stefano,Fragai, Marco,Pagano, Bruno,Donati, Greta,Novellino, Ettore,Quintavalle, Cristina,Condorelli, Gerolama,Sabbatino, Francesco,Seneci, Pierfausto,Arosio, Daniela,Pepe, Stefano,Marinelli, Luciana
supporting information, p. 16020 - 16045 (2021/11/10)
The inhibition of the PD-1/PD-L1 axis by monoclonal antibodies has achieved remarkable success in treating a growing number of cancers. However, a novel class of small organic molecules, with BMS-202 (1) as the lead, is emerging as direct PD-L1 inhibitors. Herein, we report a series of 2,4,6-tri- and 2,4-disubstituted 1,3,5-triazines, which were synthesized and assayed for their PD-L1 binding by NMR and homogeneous time-resolved fluorescence. Among them, compound 10 demonstrated to strongly bind with the PD-L1 protein and challenged it in a co-culture of PD-L1 expressing cancer cells (PC9 and HCC827 cells) and peripheral blood mononuclear cells enhanced antitumor immune activity of the latter. Compound 10 significantly increased interferon γrelease and apoptotic induction of cancer cells, with low cytotoxicity in healthy cells when compared to 1, thus paving the way for subsequent preclinical optimization and medical applications.
Triazine natural gas drag reducer as well as synthesis method and application thereof
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Paragraph 0020; 0036-0039, (2020/04/29)
The invention discloses a triazine natural gas drag reducer. The molecular structural formula of the drag reducer is shown in the description. A synthesis method of the drag reducer comprises the following steps: dissolving cyanuric chloride in a solvent, dropwise adding an alcohol and an inorganic alkali at -15-0 DEG C, carrying out a reaction at -15-0 DEG C for 2-6 h, adding morpholine and the inorganic alkali after the reaction ends, carrying out a reaction at 50-100 DEG C for 6-12 h, washing the obtained reaction product with water after the reaction ends, and drying the washed reaction product to obtain the product. The drag reducer has a multi-polar end and a non-polar end, and has a good adsorption performance and excellent drag reducing and transportation increasing effects. The synthesis method has the advantages of simplicity, mild conditions, short time, low device requirements, and easiness in realization of large-scale industrial production.
METHOD FOR PRODUCING ISOCYANURIC ACID DERIVATIVE HAVING TWO HYDROCARBON GROUPS
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Paragraph 0051-0058, (2019/03/14)
A method for producing an isocyanuric acid derivative having two hydrocarbon groups including: a first step of obtaining a compound of Formula (1); a second step of obtaining a compound of Formula (2) from the compound of Formula (1); a third step of obtaining a compound of Formula (3) from the compound of Formula (2); and a fourth step of obtaining a compound of Formula (4) from the compound of Formula (3), wherein Bn is a benzyl group, and two Rs are each a C1-10 hydrocarbon group, wherein all the steps are carried out at a temperature not exceeding 100° C.
TRIAZINE DIONE COMPOUND
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Paragraph 0063; 0095-0097, (2017/07/11)
PROBLEM TO BE SOLVED: To provide a novel triazine dione compound useful as an alkylating agent for a nucleophilic compound. SOLUTION: This invention relates to a compound represented by formula (I) [where each symbol is as defined in the specification] and an alkylating agent comprising the compound, and a method for alkylating a nucleophilic compound using the alkylating agent. SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT
Study of the Reactivities of Acid-Catalyzed O-Benzylating Reagents Based on Structural Isomers of 1,3,5-Triazine
Fujita, Hikaru,Hayakawa, Naoko,Kunishima, Munetaka
, p. 11200 - 11205 (2015/11/18)
We have demonstrated O-benzylating abilities of both 4,6-bis(benzyloxy)-1,3,5-triazin-2(1H)-one (DiBOT) and 6-(benzyloxy)-1,3,5-triazine-2,4(1H,3H)-dione (MonoBOT), which have been previously suggested as reaction intermediates of the acid-catalyzed benzylation of 2,4,6-tris(benzyloxy)-1,3,5-triazine (TriBOT). We studied the effect on the reactivity of acid-catalyzed O-benzylation caused by the isomeric core triazine structures in these compounds by carrying out a kinetic study and estimating relative basicities using model compounds. Since MonoBOT showed superior reactivity, 1,3,5-triazine-2,4(1H,3H)-dione is a promising core structure for acid-catalyzed alkylating reagents.
HYDROXY GROUP PROTECTING AGENT AND HYDROXY GROUP PROTECTION METHOD
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Paragraph 0043, (2015/01/07)
To provide: a hydroxy group protecting agent which is stable and easy to use, does not have carcinogenicity, a tearing property or the like, and is inexpensive; and a hydroxy group protection method which enables the protection of a hydroxy group under acidic conditions. [Solution] A hydroxy group protecting agent in which at least one protecting group is bound to a nitrogen-containing electron-withdrawing heterocyclic ring through any one of an oxygen atom, a sulfur atom and a nitrogen atom. The heterocyclic ring is a triazine ring or the like, and the protecting group is a benzyl group or the like. Specifically, the hydroxy group protecting agent is 2,4,6-tribenzyloxy-1,3,5-triazine, 2,4,6-tris(4-methoxybenzyloxy)-1,3,5-triazine or the like. In addition, 2,4,6-tris(t-butoxy)-1,3,5-triazine or the like can also be used. For protecting a hydroxy group, a compound of interest which has a hydroxy group is reacted with the hydroxy group protecting agent under acidic conditions.
GUANIDINE DERIVATIVES FOR THE TREATMENT OF HEPATITIS C
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Page/Page column 41, (2014/08/07)
Compounds of Formula I, including pharmaceutically acceptable salts thereof, are set forth, in addition to compositions and methods of using these compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
4,6-DIAMINOSUBSTITUTED-2-[OXY OR AMINOXY]-[1,3,5]TRIAZINES AS PROTEIN TYROSINE KINASE INHIBITORS
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Page 36-37, (2010/02/06)
The invention is directed to compounds of Formulae (I, II, III) or (IV): wherein R, R1, R2, R3, A1 and A2 are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially VEGFR-2 (KDR), c-fms, c-met and tie-2 kinases. The invention is also directed toward methods of preparation of the compounds of Formulae (I, II, III) and (IV).
Selective mono- or dialkoxylation of 2,4,6-trichloro-1,3,5-triazine in solid-liquid phase transfer conditions
Menicagli,Malanga,Peluso
, p. 2153 - 2158 (2007/10/02)
In solid-liquid phase transfer conditions, both the primary and the secondary alcohols react cleanly with 2,4, 6-trichloro-1,3,5-triazine to give the corresponding mono or dialkoxy derivatives depending on the reagent molar ratio.
