Month: November 2020

5291-32-7, Chemistry can be defined as the study of matter and the changes it undergoes. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology.5291-32-7, Name is APR-246, molecular formula is C10H17NO3, introducing its new discovery.

Mutant p53 tunes the NRF2-dependent antioxidant response to support survival of cancer cells

NRF2 (NFE2L2) is one of the main regulators of the antioxidant response of the cell. Here we show that in cancer cells NRF2 targets are selectively upregulated or repressed through a mutant p53-dependent mechanism. Mechanistically, mutant p53 interacts with NRF2, increases its nuclear presence and resides with NRF2 on selected ARE containing gene promoters activating the transcription of a specific set of genes while leading to the transcriptional repression of others. We show that thioredoxin (TXN) is a mutant p53-activated NRF2 target with pro-survival and pro-migratory functions in breast cancer cells under oxidative stress, while heme oxygenase 1 (HMOX1) is a mutant p53-repressed target displaying opposite effects. A gene signature of NRF2 targets activated by mutant p53 shows a significant association with bad overall prognosis and with mutant p53 status in breast cancer patients. Concomitant inhibition of thioredoxin system with Auranofin and of mutant p53 with APR-246 synergizes in killing cancer cells expressing p53 gain-of-function mutants.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H172N | ChemSpider

123536-14-1, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.123536-14-1, Name is (R)-3-Aminoquinuclidine dihydrochloride, molecular formula is C7H16Cl2N2. In a Article, authors is Sarasamkan, Jiradanai£¬once mentioned of 123536-14-1

Varying Chirality Across Nicotinic Acetylcholine Receptor Subtypes: Selective Binding of Quinuclidine Triazole Compounds

The novel quinuclidine anti-1,2,3-triazole derivatives T1-T6 were designed based on the structure of QND8. The binding studies revealed that the stereochemistry at the C3 position of the quinuclidine scaffold plays an important role in the nAChR subtype selectivity. Whereas the (R)-enantiomers are selective to alpha7 over alpha4beta2 (by factors of 44-225) and to a smaller degree over alpha3beta4 (3-33), their (S)-counterparts prefer alpha3beta4 over alpha4beta2 (62-237) as well as over alpha7 (5-294). The (R)-derivatives were highly selective to alpha7 over alpha3beta4 subtypes compared to (RS)- and (R)-QND8. The (S)-enantiomers are 5-10 times more selective to alpha4beta2 than their (R) forms. The overall strongest affinity is observed for the (S)-enantiomer binding to alpha3beta4 (Ki, 2.25-19.5 nM) followed by their (R)-counterpart binding to alpha7 (Ki, 22.5-117 nM), with a significantly weaker (S)-enantiomer binding to alpha4beta2 (Ki, 414-1980 nM) still above the very weak respective (R)-analogue affinity (Ki, 5059-10436 nM).

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Quinuclidine – Wikipedia,
Quinuclidine | C7H154N | ChemSpider

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 a patent, 123536-14-1, molecular formula is C7H16Cl2N2, introducing its new discovery. 123536-14-1

PYRIMIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS

The present invention relates to a compound of formula (VII)I, or a pharmaceutically acceptable salt or ester thereof, wherein: X is NR7; Y is O or N-(CH2)nR19; n is 1, 2 or 3; m is 1 or 2; R1 and R2 are each independently H, alkyl or cycloalkyl; R4 and R4′ are each independently H or alkyl; or R4 and R4′ together form a spiro cycloalkyl group; R19 is H, alkyl, aryl or a cycloalkyl group; R6 is OR8 or halogen; and R7 and R8 are each independently H or alkyl. Further aspects relate to pharmaceutical compositions comprising said compounds and use therefore in the treatment of proliferative disorders and the like

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Quinuclidine – Wikipedia,
Quinuclidine | C7H108N | ChemSpider

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 5291-32-7, name is APR-246, introducing its new discovery. 5291-32-7

COMBINATION CANCER THERAPIES

Drug combinations of a heteroarotinoid (e.g., SHetA2), and an Azabicyclooctan-3-one derivative (e.g., PRIMA-1 or PRIMAMET) and/or, a CDK4/6 inhibitor (e.g., Palbociclib, Abemaciclib, or Ribociclib), which are synergistically-effective as anti-cancer treatments, and kits and methods of use of such drug combinations.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.5291-32-7, you can also check out more blogs about5291-32-7

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Quinuclidine – Wikipedia,
Quinuclidine | C7H162N | ChemSpider

123536-14-1, In an article, published in an article,authors is Bourdin, Celine M., once mentioned the application of 123536-14-1, Name is (R)-3-Aminoquinuclidine dihydrochloride,molecular formula is C7H16Cl2N2, is a conventional compound. this article was the specific content is as follows.

Pharmacological profile of zacopride and new quaternarized fluorobenzamide analogues on mammalian alpha7 nicotinic acetylcholine receptor

Abstract From quaternarization of quinuclidine enantiomers of 2-fluoro benzamide LMA10203 in dichloromethane, the corresponding N-chloromethyl derivatives LMA10227 and LMA10228 were obtained. Here, we compared the agonist action of known zacopride and its 2-fluoro benzamide analogues, LMA10203, LMA10227 and LMA10228 against mammalian homomeric alpha7 nicotinic acetylcholine receptor expressed in Xenopus oocytes. We found that LMA10203 was a partial agonist of alpha7 receptor with a pEC50 value of 4.25 ¡À 0.06 muM whereas LMA10227 and LMA10228 were poorly active on alpha7 homomeric nicotinic receptor. LMA10227 and LMA10228 were identified as antagonists of acetylcholine-induced currents with IC50 values of 28.4 muM and 39.3 muM whereas LMA10203 and zacopride possessed IC50 values of 8.07 muM and 7.04 muM, respectively. Moreover, despite their IC50 values, LMA10227 was the most potent inhibitor of nicotine-induced current amplitudes (65.7 ¡À 2.1% inhibition). LMA10203 and LMA10228 had the same inhibitory effects (26.5 ¡À 7.5% and 33.2 ¡À 4.1%, respectively), whereas zacopride had no significant inhibitory effect (4.37 ¡À 4%) on nicotine-induced responses. Our results revealed different pharmacological properties between the four compounds on acetylcholine and nicotine currents. The mode of action of benzamide compounds may need to be reinterpreted with respect to the potential role of alpha7 receptor.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H137N | ChemSpider

123536-14-1, An article , which mentions 123536-14-1, molecular formula is C7H16Cl2N2. The compound – (R)-3-Aminoquinuclidine dihydrochloride played an important role in people’s production and life.

Intriguing case of Pseudo-isomorphism between chiral and racemic crystals of rac- and (S)/(R)2-(1,8-Naphthalimido)-2-quinuclidin-3-yl, and their reactivity toward I2 and IBr

Condensation reactions between 1,8-naphthalic anhydride and racemic 3-aminoquinuclidine or chiral (S) or (R)-(-)-3-aminoquinuclidine allowed preparation of three novel racemic and enantiopure aza-donor ligands, namely NMiABCO (1), (S)NMiABCO (2a), and (R)NMiABCO (2b). Racemic NMiABCO (1) crystallizes in the monoclinic space group P21/c, Z? = 1, while enantiopure (S)NMiABCO (2a) and (R)NMiABCO (2b) crystallize in the chiral monoclinic space group P21, Z? = 2, and show significant pseudocentrosymmetry, being pseudo-isomorphous with racemic NMiABCO (1). Reactivity of both racemic and enantiopure NMiABCO toward iodine and interhalogen IBr was also investigated as a way to remove the pseudoisomorphism, yielding the three new molecular adducts [NMiABCO¡¤I2] (3), [(S)NMiABCO¡¤I2]¡¤xCHCl3 (4), [(S)NMiABCO¡¤IBr]¡¤xCHCl3 (5) and the molecular salt [HNMiABCO][IBr2] (6). Synthesis of complexes 3 and 4 was also carried out in the solid state via kneading and vapor digestion techniques. All compounds were fully characterized via single crystal and powder X-ray diffraction and Raman spectroscopy.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H142N | ChemSpider

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬Which mentioned a new discovery about 123536-14-1, molcular formula is C7H16Cl2N2, introducing its new discovery. , 123536-14-1

4-SUBSTITUTED IMIDAZOLES

Compounds of formula I: wherein A and R1 are as defined in the specification, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially in the treatment or prophylaxis of psychotic and intellectual impairment disorders.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H103N | ChemSpider

In an article, published in an article,authors is Bodnar, Alice L., once mentioned the application of 123536-14-1, Name is (R)-3-Aminoquinuclidine dihydrochloride,molecular formula is C7H16Cl2N2, is a conventional compound. this article was the specific content is as follows. 123536-14-1

Discovery and structure-activity relationship of quinuclidine benzamides as agonists of alpha7 nicotinic acetylcholine receptors

A library of benzamides was tested for alpha7 nicotinic acetylcholine receptor (nAChR) agonist activity using a chimeric receptor in a functional, cell-based, high-throughput assay. From this library, quinuclidine benzamides were found to have alpha7 nAChR agonist activity. The SAR diverged from the activity of this compound class verses the 5-HT3 receptor, a structural homologue of the alpha7 nAChR. PNU-282987, the most potent compound from this series, was also shown to open native alpha7 nAChRs in cultured rat neurons and to reverse an amphetamine-induced gating deficit in rats.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H136N | ChemSpider

827-61-2, 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.827-61-2, Name is Quinuclidin-3-yl acetate, molecular formula is C9H15NO2. In a article£¬once mentioned of 827-61-2

New Strategies for the Transition-Metal Catalyzed Synthesis of Aliphatic Amines

Transition-metal catalyzed reactions that are able to construct complex aliphatic amines from simple, readily available feedstocks have become a cornerstone of modern synthetic organic chemistry. In light of the ever-increasing importance of aliphatic amines across the range of chemical sciences, this review aims to provide a concise overview of modern transition-metal catalyzed approaches to alkylamine synthesis and their functionalization. Selected examples of amine bond forming reactions include: (a) hydroamination and hydroaminoalkylation, (b) transition-metal catalyzed C(sp3)-H functionalization, and (c) transition-metal catalyzed visible-light-mediated light photoredox catalysis.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H86N | ChemSpider

Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. 123536-14-1. Introducing a new discovery about 123536-14-1, Name is (R)-3-Aminoquinuclidine dihydrochloride

Synthesis of quinazoline-2,4-dione and naphthalimide derivatives as new 5-HT3 receptor antagonists

New potent 5-HT3 receptor antagonists have been designed from the naphthalimide moiety and a quinuclidine heterocycle and the structure-activity relationships are discussed here on the basis of the nature of the substituent on the aromatic system. The biological activity of the compounds was evaluated in binding assays with [3H]BRL-43694 and by inhibition of the Bezold-Jarisch reflex. Compound 22 with a 4-amino substituent was equipotent to the reference compounds. In contrast to the benzamide derivatives, the activity resides essentially in the (R) enantiomer (K(i) = 0.15 ¡À 0.05 nM, ID50 = 1.6 mug/kg/iv) and it is demonstrated that the additional carbonyl group is involved in the inversion of the enantioselectivity of the receptor. Conformational studies of (R)-22 demonstrated the presence of a locked structure with 4 minimal energy conformers which were compared to those of (S)-zacopride. The superimposition of the putative active conformers emphasized the presence of a second polar group in the binding site. The fluorescent properties of the compounds were studied and indicate that (R)-22 and its derivatives may be promising tools for the direct visualization of 5-HT3 receptors.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H148N | ChemSpider