Category: 120099-61-8

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 Development of peptide epoxyketones as selective immunoproteasome inhibitors.Synthetic Route of C5H11NO.

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.

There are many compounds similar to this compound(120099-61-8)Synthetic Route of C5H11NO. if you want to know more, you can check out my other articles. I hope it will help you，maybe you’ll find some useful information.

Reference:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: (S)-3-Methoxypyrrolidine( cas:120099-61-8 ) is researched.Recommanded Product: 120099-61-8.Sun, Chang’an; Fang, Lei; Zhang, Xiaobing; Gao, Peng; Gou, Shaohua published the article 《Novel 7-formyl-naphthyridyl-ureas derivatives as potential selective FGFR4 inhibitors: Design, synthesis, and biological activity studies》 about this compound( cas:120099-61-8 ) in Bioorganic & Medicinal Chemistry. Keywords: antitumor FGFR4 selectivity pharmacokinetic profile; Antitumor; FGFR4; Pharmacokinetic profile; Selectivity. Let’s learn more about this compound (cas:120099-61-8).

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.

Here is just a brief introduction to this compound(120099-61-8)Recommanded Product: 120099-61-8, more information about the compound((S)-3-Methoxypyrrolidine) is in the article, you can click the link below.

Reference:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

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.Yang, Zhaohui; Li, Linlang; Zheng, Jiyue; Ma, Haikuo; Tian, Sheng; Li, Jiajun; Zhang, Hongjian; Zhen, Xuechu; Zhang, Xiaohu researched the compound: (S)-3-Methoxypyrrolidine( cas:120099-61-8 ).Quality Control of (S)-3-Methoxypyrrolidine.They published the article 《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》 about this compound( cas:120099-61-8 ) in ACS Chemical Neuroscience. Keywords: aminocarbonitrile pyrimidine preparation adenosine A2A receptor antagonist design antiparkinsonian; Adenosine receptor; GPCR; Parkinson’s disease; antagonist; lead identification. We’ll tell you more about this compound (cas:120099-61-8).

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.

Compound(120099-61-8)Quality Control of (S)-3-Methoxypyrrolidine received a lot of attention, and I have introduced some compounds in other articles, similar to this compound((S)-3-Methoxypyrrolidine), if you are interested, you can check out my other related articles.

Reference:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Product Details of 120099-61-8. 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 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.

There is still a lot of research devoted to this compound(SMILES：CO[C@@H]1CNCC1)Product Details of 120099-61-8, and with the development of science, more effects of this compound(120099-61-8) can be discovered.

Reference:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

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.Feng, Yuxin; Xiao, Senhao; Chen, Yantao; Jiang, Hao; Liu, Na; Luo, Cheng; Chen, Shijie; Chen, Hua researched the compound: (S)-3-Methoxypyrrolidine( cas:120099-61-8 ).Reference of (S)-3-Methoxypyrrolidine.They published the article 《Design, synthesis and biological evaluation of benzo[cd]indol-2(1H)-one derivatives as BRD4 inhibitors》 about this compound( cas:120099-61-8 ) in European Journal of Medicinal Chemistry. Keywords: benzoindolone preparation BRD4 inhibitor antitumor cancer human; Acetyl-lysine binding pocket; BRD4 inhibitor; Benzo[cd]indol-2(1H)-one; Bromodomain and extra-terminal domain; Sulfonamide. We’ll tell you more about this compound (cas:120099-61-8).

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.

In some applications, this compound(120099-61-8)Reference of (S)-3-Methoxypyrrolidine is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.

Reference:
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 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.

In some applications, this compound(120099-61-8)Recommanded Product: 120099-61-8 is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.

Reference:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Electric Literature of C5H11NO. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. 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.

In some applications, this compound(120099-61-8)Electric Literature of C5H11NO is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.

Reference:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 120099-61-8, is researched, Molecular C5H11NO, about Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators, the main research direction is neurotensin receptor 1 allosteric modulator SBI 553 pharmacokinetics.Product Details of 120099-61-8.

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.

In some applications, this compound(120099-61-8)Product Details of 120099-61-8 is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.

Reference:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Category: pyrimidines. 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 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.

In some applications, this compound(120099-61-8)Category: pyrimidines is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.

Reference:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Related Products 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 Development of peptide epoxyketones as selective immunoproteasome inhibitors. Author is Li, Xuemei; Hong, Duidui; Zhang, Mengmeng; Xu, Lei; Zhou, Yubo; Li, Jia; Liu, Tao.

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.

In some applications, this compound(120099-61-8)Related Products of 120099-61-8 is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.

Reference:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia