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ANTIVIRAL COMPOUNDS

This invention relates to a series of tricyclic compounds comprising a pteridinone core linked to a third heterocycloalkyl ring. The compounds are useful in the treatment of Hepatitis B viral infections. The invention also relates to pharmaceutical compositions comprising these compounds and methods of using the compounds in treatment.

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Reference£º
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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Synthetic Route of 1745-07-9, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.1745-07-9, Name is 6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinoline, molecular formula is C11H15NO2. In a article£¬once mentioned of 1745-07-9

Synthesis and SAR of novel capsazepine analogs with significant anti-cancer effects in multiple cancer types

We previously demonstrated that capsazepine (CPZ), a synthetic transient receptor potential Vanilloid subtype 1 (TRPV1) antagonist, has significant anti-cancer effects in vivo. The purpose of this study was to develop more potent analogs based upon CPZ pharmacophore and structure?activity relationships (SAR) across analogs. We generated 30 novel compounds and screened for their anti-proliferative effects in cultured HeLa cervical cancer cells. Cell viability assays identified multiple compounds with IC50s < 15 muM and one compound, 29 with an IC50 < 5 muM; six fold more potent than CPZ. We validated the anti-proliferative efficacy of two lead compounds, 17 and 29, in vivo using HeLa-derived xenografts in athymic nude mice. Both analogs significantly reduced tumor volumes by day 8 compared to control treated animals (p < 0.001) with no observable adverse effects. Calcium imaging determined that compound 17 activates TRPV1 whereas 29 neither activates nor inhibits TRPV1; indicating a unique mechanism-of-action that does not involve TRPV1 signaling. Cell viability assays using a panel of additional tumor types including oral squamous cell carcinoma, non-small cell lung cancer (NSCLC), breast cancer, and prostate cancer cell lines (HSC-3, H460, MDA-231, and PC-3 respectively) demonstrated that both lead compounds were efficacious against every cancer type tested. Compounds 29 displayed IC50s of 1?2.5 muM in HSC-3and PC-3cells. Thus, we propose that these novel CPZ analogs may serve as efficacious therapeutic agents against multiple tumor types that warrant further development for clinical application. A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 1745-07-9 Reference£º
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Final Thoughts on Chemistry for 1612-65-3

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Synthetic Route of 1612-65-3, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.1612-65-3, Name is 2-Methyl-1,2,3,4-tetrahydroisoquinoline, molecular formula is C10H13N. In a Article£¬once mentioned of 1612-65-3

Computational spectroscopy of a bichromophoric molecule, 2-methyl-1,2,3,4-tetrahydroisoquinoline, in solutions

An ab initio calculation of the title molecule was performed to interpret previously observed electronic spectra of the title system. Since the computation concerns the isolated molecule, possible effects of solvent molecules had to be taken into account, especially for such as Rydberg states. The S3 ? S0, S2 ? S1 n, and S1n ? S0 absorption bands are (re)assigned to the excited states of the Lb, L a/CT, and nNsigma (3s) states, respectively. The minor S1a ? S0 absorption observed at the red area of the S1n ? S0 band in acetonitrile is reinterpreted as being a nNpi (CT) state. Correspondingly, the pi, nN, and aN fluorescence spectra are (re)ascribed to the excited states of the Lb, nNsigma*, and nNpi states, respectively. The nNsigma* and nN* states are found to be restricted to the equatorial and axial conformers, respectively. The exceptionally long progression of the pi fluorescence in hexane is interpreted as being due to the closeness of the La and Lb states.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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STEREOCHIMIE DE LA CYCLOADDITION DES DIARYLNITRILIMINES SUR LES N-ALKYL ET LES DIALKYL-1,2 DIHYDRO-1,2 ISOQUINOLEINES

The PMR spectroscopic properties (60 MHz) of cycloadducts of diarylnitrilimins towards 1,2-dihydroisoquinolines mono alkylated at the N-atom or dialkylated at the C1-carbon and N-atoms have been studied.Date allow us to determine the stereochemistry of the cycloaddition reaction which is regio and diastereospecific.Configuration and conformation of the cycloadducts are specified.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Extracurricular laboratory:new discovery of 1745-07-9

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Synthesis and evaluation of furoxan-based nitric oxide-releasing derivatives of tetrahydroisoquinoline as anticancer and multidrug resistance reversal agents

Multidrug resistance in tumor cells poses a major obstacle to efficient chemotherapy. Several types of agents have been recognized as multidrug resistance inhibitors, among which the tetrahydroisoquinolines is the most studied. In current study 16 furoxan-based nitric oxide-releasing derivatives of tetrahydroisoquinoline were synthesized. Their cytotoxic activities and effects in reversing multidrug resistance have been evaluated. The results revealed that these compounds had moderate cytotoxic effects. Compounds 7a-f, 7h, and 7l showed higher cytotoxicities than the rest, but lower than adriamycin on K562 cell line. Compounds 7d, 7f, and 7l exhibited potent MDR reversal activities on K562/A02 cell line. The accumulation assay indicated that compounds 7d, 7f, and 7l significantly increased the intracellular accumulation of rhodamine123 in K562/A02 cells. Furthermore, these three compounds produced high concentrations of NO in K562/A02 cells. Potentially, the high concentrations of NO produced by NO donor moieties will lead to an increased cytotoxicity to K562/A02 cells. Our results suggested that compounds 7d, 7f, and 7l had anticancer effects, as well as multidrug resistance reversal effects.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Can You Really Do Chemisty Experiments About 2-Phenyl-1,2,3,4-tetrahydroisoquinoline

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Reference of 3340-78-1, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 3340-78-1, Name is 2-Phenyl-1,2,3,4-tetrahydroisoquinoline, molecular formula is C15H15N. In a Article£¬once mentioned of 3340-78-1

Luminescent organogold(III) complexes with long-lived triplet excited states for light-induced oxidative C-H bond functionalization and hydrogen production

All that glitters is gold: Highly phosphorescent gold(III) complexes (see picture) with extended pi-conjugated cyclometalating ligands exhibit rich photophysical and photochemical properties. They act as efficient photocatalysts/photosensitizers for oxidative functionalizations of secondary and tertiary benzylic amines and homogeneous hydrogen production from a water/acetonitrile mixture. Copyright

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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Dual C-H functionalization of N-aryl tetrahydroisoquinolines: A highly diastereoselective synthesis of dibenzo[a,f]quinolizines via visible-light induced oxidation and inverse electron-demand aza-Diels-Alder reaction

Described herein is the first example of the application of an iminium intermediate generated by visible-light photocatalyzed oxidation in an inverse electron-demand aza-Diels-Alder reaction. This dual functionalization of both C(sp3)-H and C(sp2)-H bonds of N-aryl tetrahydroisoquinolines represents a valuable example for access to polycycles with high diastereoselectivity.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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Synthetic Route of 166591-85-1, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 166591-85-1, molcular formula is C15H19NO4, introducing its new discovery.

Pyrazolopyridine compound and use thereof (by machine translation)

The invention relates to a pyrazolopyridine compound and its use, further relates to the pharmaceutical composition. The compound of the invention or the pharmaceutical composition can be used as soluble guanylate cyclase stimulant. (by machine translation)

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Reference£º
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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Synthetic Route of 1745-07-9, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.1745-07-9, Name is 6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinoline, molecular formula is C11H15NO2. In a Article£¬once mentioned of 1745-07-9

Affinity of 2-(tetrahydroisoquinolin-2-methyl)- and 2-(isoindolin-2-ylmethyl)imidazolines for alpha-adrenoceptors. Differential affinity of imidazolines for the [3H]idazoxan-labeled alpha2-adrenoceptor vs the [3H]yohimbine-labeled site

A series of 2-(tetrahydroisoquinolin-2-ylmethyl)- and 2-(isoindolin-2-ylmethyl)imidazolines were prepared and tested for alpha1- and alpha2-adrenoceptor affinity with radioligand binding. Several compounds, 5-fluoro- (5h), 5-chloro- (5j), 5,8-dimethoxy- (5r), and 5,8-dimethoxy-1-methyl- (5s) 2-(tetrahydroisoquinolin-2-ylmethyl)imidazoline, were found to be selective alpha2-adrenoceptor ligands on the basis of displacement of [3H]yohimbine from rat cerebral cortical membranes. One compound, 2-[(8-chloro tetrahydroisoquinolin-2-yl)methyl]imidazoline (5m), showed a 36-fold difference in affinity for the [3H]idazoxan-labeled alpha2-adrenoceptor relative to the [3H]yohimbine-labeled site, which may be evidence for alpha2-adrenoceptor subtypes.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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NOVEL MONOAMINE RE-UPTAKE INHIBITOR

The present invention relates to novel compounds of Formula (I), their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention further provides pharmaceutical compositions comprising compounds of Formula I and methods of treating or preventing one or more disorders of the central and/or peripheral nervous system that are responsive to inhibition of biogenic amines, in particular one or more, or any combination of serotonin, norepinephrine and dopamine.

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Reference£º
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem