Category: 120099-61-8

COA of Formula: C5H11NO. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: (S)-3-Methoxypyrrolidine, is researched, Molecular C5H11NO, CAS is 120099-61-8, about Design, synthesis and biological evaluation of benzo[cd]indol-2(1H)-one derivatives as BRD4 inhibitors. Author is Feng, Yuxin; Xiao, Senhao; Chen, Yantao; Jiang, Hao; Liu, Na; Luo, Cheng; Chen, Shijie; Chen, Hua.

A series of benzo[cd]indol-2(1H)-one derivatives were designed by structural optimization based on compound I and evaluated for their BRD4 (bromodomain-containing protein 4) inhibitory activity. The results showed that four compounds are the most potential ones with the IC50 values of 1.02 μM, 1.43 μM, 1.55 μM and 3.02 μM. According to their co-crystal structures in complex with BRD4_BD1 and the protein thermal shift assays, the binding modes were revealed that the addnl. indirect hydrogen bonds and hydrophobic interactions make such four compounds more active than I against BRD4. Furthermore, compounds I, 1-((1-ethyl-2-oxo-1,2-dihydrobenzo[cd]indol-6-yl)sulfonyl)pyrrolidine-2-carbohydrazide and 1-((1-ethyl-2-oxo-1,2-dihydrobenzo[cd]indol-6-yl)sulfonyl)pyrrolidine-2-carboxylic acid were chosen to evaluate for their antiproliferative activities on the MLL-AF4-expression acute leukemia cell line (MV4-11), other cancer cell lines and the non-cancer cell lines. The results showed that these compounds exhibited good and selective inhibitory activities against MV4-11 cells with the IC50 values of 11.67 μM, 5.55 μM, and 11.54 μM, resp., and could act on the cell proliferation by blocking cell cycle at G1 phase. They could markedly down-regulate the expressions of the c-Myc, Bcl-2 and CDK6 oncogenes in MV4-11 in the qRT-PCR and western blot studies, which further demonstrated that compound I and its derivatives could serve as a promising therapeutic strategy for MLL leukemia by targeting BRD4_BD1 protein.

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Category: pyrimidines. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: (S)-3-Methoxypyrrolidine, is researched, Molecular C5H11NO, CAS is 120099-61-8, about Identification of a New Series of Potent Adenosine A2A Receptor Antagonists Based on 4-Amino-5-carbonitrile Pyrimidine Template for the Treatment of Parkinson’s Disease.

Adenosine receptor A2A antagonists have emerged as potential treatment for Parkinson’s disease in the past decade. The authors have recently reported a series of adenosine receptor antagonists using heterocycles as bioisosteres for a potentially unstable acetamide. These compounds, while showing excellent potency and ligand efficiency, suffered from moderate cytochrome P 450 inhibition and high clearance. Here the authors report a new series of adenosine receptor A2A antagonists based on a 4-amino-5-carbonitrile pyrimidine template. Compounds from this new template exhibit excellent potency and ligand efficiency with low cytochrome P 450 inhibition. Although the clearance remains moderate to high, the leading compound, when dosed orally as low as 3 mg/kg, demonstrated excellent efficacy in the haloperidol induced catalepsy rat model for Parkinson’s disease.

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Pyrimidine | C4H4N2 – PubChem,
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Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: (S)-3-Methoxypyrrolidine, is researched, Molecular C5H11NO, CAS is 120099-61-8, about Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators.Electric Literature of C5H11NO.

Neurotensin receptor 1 (NTR1) is a G protein coupled receptor that is widely expressed throughout the central nervous system where it acts as a neuromodulator. Neurotensin receptors have been implicated in a wide variety of CNS disorders but despite extensive efforts to develop small mol. ligands there are few reports of such compounds Herein we describe the optimization of a quinazoline based lead to give 18 (SBI-553(I)), a potent and brain penetrant NTR1 allosteric modulator.

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Pyrimidine | C4H4N2 – PubChem,
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Electric Literature of C5H11NO. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: (S)-3-Methoxypyrrolidine, is researched, Molecular C5H11NO, CAS is 120099-61-8, about Ultrapotent vinblastines in which added molecular complexity further disrupts the target tubulin dimer-dimer interface. Author is Carney, Daniel W.; Lukesh, John C. III; Brody, Daniel M.; Brutsch, Manuela M.; Boger, Dale L..

Approaches to improving the biol. properties of natural products typically strive to modify their structures to identify the essential pharmacophore, or make functional group changes to improve biol. target affinity or functional activity, change phys. properties, enhance stability, or introduce conformational constraints. Aside from accessible semisynthetic modifications of existing functional groups, rarely does one consider using chem. synthesis to add mol. complexity to the natural product. In part, this may be attributed to the added challenge intrinsic in the synthesis of an even more complex compound Herein, we report synthetically derived, structurally more complex vinblastines inaccessible from the natural product itself that are a stunning 100-fold more active (IC50 values, 50-75 pM vs. 7 nM; HCT116), and that are now accessible because of advances in the total synthesis of the natural product. The newly discovered ultrapotent vinblastines, which may look highly unusual upon first inspection, bind tubulin with much higher affinity and likely further disrupt the tubulin head-to-tail α/β dimer-dimer interaction by virtue of the strategic placement of an added conformationally well-defined, rigid, and extended C20′ urea along the adjacent continuing protein-protein interface. In this case, the added mol. complexity was used to markedly enhance target binding and functional biol. activity (100-fold), and likely represents a general approach to improving the properties of other natural products targeting a protein-protein interaction.

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Electric Literature of C5H11NO. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: (S)-3-Methoxypyrrolidine, is researched, Molecular C5H11NO, CAS is 120099-61-8, about Ultrapotent vinblastines in which added molecular complexity further disrupts the target tubulin dimer-dimer interface. Author is Carney, Daniel W.; Lukesh, John C. III; Brody, Daniel M.; Brutsch, Manuela M.; Boger, Dale L..

Approaches to improving the biol. properties of natural products typically strive to modify their structures to identify the essential pharmacophore, or make functional group changes to improve biol. target affinity or functional activity, change phys. properties, enhance stability, or introduce conformational constraints. Aside from accessible semisynthetic modifications of existing functional groups, rarely does one consider using chem. synthesis to add mol. complexity to the natural product. In part, this may be attributed to the added challenge intrinsic in the synthesis of an even more complex compound Herein, we report synthetically derived, structurally more complex vinblastines inaccessible from the natural product itself that are a stunning 100-fold more active (IC50 values, 50-75 pM vs. 7 nM; HCT116), and that are now accessible because of advances in the total synthesis of the natural product. The newly discovered ultrapotent vinblastines, which may look highly unusual upon first inspection, bind tubulin with much higher affinity and likely further disrupt the tubulin head-to-tail α/β dimer-dimer interaction by virtue of the strategic placement of an added conformationally well-defined, rigid, and extended C20′ urea along the adjacent continuing protein-protein interface. In this case, the added mol. complexity was used to markedly enhance target binding and functional biol. activity (100-fold), and likely represents a general approach to improving the properties of other natural products targeting a protein-protein interaction.

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Reference:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pinkerton, Anthony B.; Peddibhotla, Satyamaheshwar; Yamamoto, Fusayo; Slosky, Lauren M.; Bai, Yushi; Maloney, Patrick; Hershberger, Paul; Hedrick, Michael P.; Falter, Bekhi; Ardecky, Robert J.; Smith, Layton H.; Chung, Thomas D. Y.; Jackson, Michael R.; Caron, Marc G.; Barak, Lawrence S. published an article about the compound: (S)-3-Methoxypyrrolidine( cas:120099-61-8,SMILESS:CO[C@@H]1CNCC1 ).COA of Formula: C5H11NO. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:120099-61-8) through the article.

Neurotensin receptor 1 (NTR1) is a G protein coupled receptor that is widely expressed throughout the central nervous system where it acts as a neuromodulator. Neurotensin receptors have been implicated in a wide variety of CNS disorders but despite extensive efforts to develop small mol. ligands there are few reports of such compounds Herein we describe the optimization of a quinazoline based lead to give 18 (SBI-553(I)), a potent and brain penetrant NTR1 allosteric modulator.

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Pyrimidine | C4H4N2 – PubChem,
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Product Details of 120099-61-8. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: (S)-3-Methoxypyrrolidine, is researched, Molecular C5H11NO, CAS is 120099-61-8, about Identification of a New Series of Potent Adenosine A2A Receptor Antagonists Based on 4-Amino-5-carbonitrile Pyrimidine Template for the Treatment of Parkinson’s Disease. Author is Yang, Zhaohui; Li, Linlang; Zheng, Jiyue; Ma, Haikuo; Tian, Sheng; Li, Jiajun; Zhang, Hongjian; Zhen, Xuechu; Zhang, Xiaohu.

Adenosine receptor A2A antagonists have emerged as potential treatment for Parkinson’s disease in the past decade. The authors have recently reported a series of adenosine receptor antagonists using heterocycles as bioisosteres for a potentially unstable acetamide. These compounds, while showing excellent potency and ligand efficiency, suffered from moderate cytochrome P 450 inhibition and high clearance. Here the authors report a new series of adenosine receptor A2A antagonists based on a 4-amino-5-carbonitrile pyrimidine template. Compounds from this new template exhibit excellent potency and ligand efficiency with low cytochrome P 450 inhibition. Although the clearance remains moderate to high, the leading compound, when dosed orally as low as 3 mg/kg, demonstrated excellent efficacy in the haloperidol induced catalepsy rat model for Parkinson’s disease.

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, European Journal of Medicinal Chemistry called Development of peptide epoxyketones as selective immunoproteasome inhibitors, Author is Li, Xuemei; Hong, Duidui; Zhang, Mengmeng; Xu, Lei; Zhou, Yubo; Li, Jia; Liu, Tao, which mentions a compound: 120099-61-8, SMILESS is CO[C@@H]1CNCC1, Molecular C5H11NO, Safety of (S)-3-Methoxypyrrolidine.

A series of epoxyketone analogs with varying N-caps and P3-configurations were designed, synthesized and evaluated. We found that D-Ala in P3 was crucial for β5i selectivity over β5c. Notably, compounds (I) (R1 = II) (β5i IC50 = 26.0 nM, 25-fold selectivity) and I (r1 = III) (β5i IC50 = 25.1 nM, 24-fold selectivity) with the D-configuration at P3 were the most selective inhibitors. Although I (R1 = II and III) showed only moderate anti-proliferative activity against RPMI-8226 and MM.1S cell lines, based on our experiments, it indicates that the inhibition of β5i alone is not sufficient to exert anticancer effects and may rely on the complementary inhibition of β1i, β5c and β5i. These data further increase our understanding of immunoproteasome inhibitors in hematol. malignancies.

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Product Details of 120099-61-8. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: (S)-3-Methoxypyrrolidine, is researched, Molecular C5H11NO, CAS is 120099-61-8, about Identification of a New Series of Potent Adenosine A2A Receptor Antagonists Based on 4-Amino-5-carbonitrile Pyrimidine Template for the Treatment of Parkinson’s Disease. Author is Yang, Zhaohui; Li, Linlang; Zheng, Jiyue; Ma, Haikuo; Tian, Sheng; Li, Jiajun; Zhang, Hongjian; Zhen, Xuechu; Zhang, Xiaohu.

Adenosine receptor A2A antagonists have emerged as potential treatment for Parkinson’s disease in the past decade. The authors have recently reported a series of adenosine receptor antagonists using heterocycles as bioisosteres for a potentially unstable acetamide. These compounds, while showing excellent potency and ligand efficiency, suffered from moderate cytochrome P 450 inhibition and high clearance. Here the authors report a new series of adenosine receptor A2A antagonists based on a 4-amino-5-carbonitrile pyrimidine template. Compounds from this new template exhibit excellent potency and ligand efficiency with low cytochrome P 450 inhibition. Although the clearance remains moderate to high, the leading compound, when dosed orally as low as 3 mg/kg, demonstrated excellent efficacy in the haloperidol induced catalepsy rat model for Parkinson’s disease.

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Recommanded Product: 120099-61-8. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: (S)-3-Methoxypyrrolidine, is researched, Molecular C5H11NO, CAS is 120099-61-8, about Novel 7-formyl-naphthyridyl-ureas derivatives as potential selective FGFR4 inhibitors: Design, synthesis, and biological activity studies. Author is Sun, Chang’an; Fang, Lei; Zhang, Xiaobing; Gao, Peng; Gou, Shaohua.

Total twenty-five 7-formyl-naphthyridyl-urea derivatives were designed, synthesized and evaluated for their inhibition of FGFR4 kinase and antitumor activity. The pharmacol. data indicated that most of the tested compounds showed high selectivity towards FGFR4 kinase and could significantly inhibit FGFR4 and the tumor cells lines with the high expression of FGFR4. In particular, compounds 6f, 6g, 6h, 6l, 6m and 6s showed a good performance in pharmacokinetic tests. When tested in mice, the representative compound 6f was found to have good pharmacokinetic parameters, low toxicity, and better tumor inhibiting activity in vivo.

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