Category: 254905-58-3

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: 254905-58-3, is researched, Molecular C13H24N2O3, about Conformationally restrained carbamoylcholine homologues. Synthesis, pharmacology at neuronal nicotinic acetylcholine receptors and biostructural considerations, the main research direction is carbamoylcholine homolog pharmacol neuron nicotinic receptor ligand; Acetylcholine; Agonist; Conformational restriction; Docking; Nicotinic acetylcholine receptor.COA of Formula: C13H24N2O3.

Exploration of small selective ligands for the nicotinic acetylcholine receptors (nAChRs) based on acetylcholine (ACh) has led to the development of potent agonists with clear preference for the α4β2 nAChR, the most prevalent nAChR subtype in the central nervous system. In this work the authors present the continuation of these efforts aimed at increasing this subtype selectivity by introduction of conformational restriction in the carbamoylcholine homolog, 3-(dimethylaminobutyl) dimethylcarbamate (DMABC). The results highlight the importance of the N-carbamoyl substitution in α4β2-subtype selectivity. Moreover, the authors have confirmed the non-linear conformation of DMABC bound to nAChRs suggested by recent crystal structures of the compound in complex with the Lymnaea stagnalis ACh binding protein.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

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.Mallinger, Aurelie; Crumpler, Simon; Pichowicz, Mark; Waalboer, Dennis; Stubbs, Mark; Adeniji-Popoola, Olajumoke; Wood, Bozena; Smith, Elizabeth; Thai, Ching; Henley, Alan T.; Georgi, Katrin; Court, William; Hobbs, Steve; Box, Gary; Ortiz-Ruiz, Maria-Jesus; Valenti, Melanie; De Haven Brandon, Alexis; Te Poele, Robert; Leuthner, Birgitta; Workman, Paul; Aherne, Wynne; Poeschke, Oliver; Dale, Trevor; Wienke, Dirk; Esdar, Christina; Rohdich, Felix; Raynaud, Florence; Clarke, Paul A.; Eccles, Suzanne A.; Stieber, Frank; Schiemann, Kai; Blagg, Julian researched the compound: tert-Butyl 4-(dimethylcarbamoyl)piperidine-1-carboxylate( cas:254905-58-3 ).Synthetic Route of C13H24N2O3.They published the article 《Discovery of Potent, Orally Bioavailable, Small-Molecule Inhibitors of WNT Signaling from a Cell-Based Pathway Screen》 about this compound( cas:254905-58-3 ) in Journal of Medicinal Chemistry. Keywords: trisubstituted pyridine preparation bioavailability WNT signaling inhibitor antitumor. We’ll tell you more about this compound (cas:254905-58-3).

WNT signaling is frequently deregulated in malignancy, particularly in colon cancer, and plays a key role in the generation and maintenance of cancer stem cells. The authors report the discovery and optimization of a 3,4,5-trisubstituted pyridine, 1-(3,5-Dichloropyridin-4-yl)piperidine-4-carboxamide (9), using a high-throughput cell-based reporter assay of WNT pathway activity. The authors demonstrate a twisted conformation about the pyridine-piperidine bond of (9) by small-mol. x-ray crystallog. Medicinal chem. optimization to maintain this twisted conformation, cognisant of physicochem. properties likely to maintain good cell permeability, led to 8-[3-Chloro-5-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]pyridin-4-yl]-2,8-diazaspiro[4,5]decan-1-one (74) (CCT251545), a potent small-mol. inhibitor of WNT signaling with good oral pharmacokinetics. The authors demonstrate inhibition of WNT pathway activity in a solid human tumor xenograft model with evidence for tumor growth inhibition following oral dosing. This work provides a successful example of hypothesis-driven medicinal chem. optimization from a singleton hit against a cell-based pathway assay without knowledge of the biochem. target.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Recommanded Product: 254905-58-3. 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: tert-Butyl 4-(dimethylcarbamoyl)piperidine-1-carboxylate, is researched, Molecular C13H24N2O3, CAS is 254905-58-3, about The influence of conformational restriction in the C-terminus of growth hormone secretagogues on their potency.

In order to obtain more potent growth hormone secretagogues, a comparison of ipamorelin and NN703 suggested the addition of a polar group at the C-terminus of NN703. A study was conducted using constrained amines for this purpose. Here, substituted 4-piperidinylamino- and 4-dimethylaminopiperidino-substituents were found to give the most active compounds A replacement of the 4-dimethylaminopiperidino-substituent with 4-hydroxypiperidino resulted in a series of compounds, which showed in vitro activity with EC50 values in the low nanomolar range, and favorable kinetic properties, such as 40% oral bioavailability. The most promising compound was also tested in a swine in vivo model, resulting in a growth hormone level with a Cmax of over 40 ng mL-1.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Discovery of Potent, Orally Bioavailable, Small-Molecule Inhibitors of WNT Signaling from a Cell-Based Pathway Screen, published in 2015-02-26, which mentions a compound: 254905-58-3, mainly applied to trisubstituted pyridine preparation bioavailability WNT signaling inhibitor antitumor, SDS of cas: 254905-58-3.

WNT signaling is frequently deregulated in malignancy, particularly in colon cancer, and plays a key role in the generation and maintenance of cancer stem cells. The authors report the discovery and optimization of a 3,4,5-trisubstituted pyridine, 1-(3,5-Dichloropyridin-4-yl)piperidine-4-carboxamide (9), using a high-throughput cell-based reporter assay of WNT pathway activity. The authors demonstrate a twisted conformation about the pyridine-piperidine bond of (9) by small-mol. x-ray crystallog. Medicinal chem. optimization to maintain this twisted conformation, cognisant of physicochem. properties likely to maintain good cell permeability, led to 8-[3-Chloro-5-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]pyridin-4-yl]-2,8-diazaspiro[4,5]decan-1-one (74) (CCT251545), a potent small-mol. inhibitor of WNT signaling with good oral pharmacokinetics. The authors demonstrate inhibition of WNT pathway activity in a solid human tumor xenograft model with evidence for tumor growth inhibition following oral dosing. This work provides a successful example of hypothesis-driven medicinal chem. optimization from a singleton hit against a cell-based pathway assay without knowledge of the biochem. target.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Category: benzothiophene. 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: tert-Butyl 4-(dimethylcarbamoyl)piperidine-1-carboxylate, is researched, Molecular C13H24N2O3, CAS is 254905-58-3, about The influence of conformational restriction in the C-terminus of growth hormone secretagogues on their potency.

In order to obtain more potent growth hormone secretagogues, a comparison of ipamorelin and NN703 suggested the addition of a polar group at the C-terminus of NN703. A study was conducted using constrained amines for this purpose. Here, substituted 4-piperidinylamino- and 4-dimethylaminopiperidino-substituents were found to give the most active compounds A replacement of the 4-dimethylaminopiperidino-substituent with 4-hydroxypiperidino resulted in a series of compounds, which showed in vitro activity with EC50 values in the low nanomolar range, and favorable kinetic properties, such as 40% oral bioavailability. The most promising compound was also tested in a swine in vivo model, resulting in a growth hormone level with a Cmax of over 40 ng mL-1.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Recommanded Product: 254905-58-3. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: tert-Butyl 4-(dimethylcarbamoyl)piperidine-1-carboxylate, is researched, Molecular C13H24N2O3, CAS is 254905-58-3, about Discovery of Potent, Orally Bioavailable, Small-Molecule Inhibitors of WNT Signaling from a Cell-Based Pathway Screen. Author is Mallinger, Aurelie; Crumpler, Simon; Pichowicz, Mark; Waalboer, Dennis; Stubbs, Mark; Adeniji-Popoola, Olajumoke; Wood, Bozena; Smith, Elizabeth; Thai, Ching; Henley, Alan T.; Georgi, Katrin; Court, William; Hobbs, Steve; Box, Gary; Ortiz-Ruiz, Maria-Jesus; Valenti, Melanie; De Haven Brandon, Alexis; Te Poele, Robert; Leuthner, Birgitta; Workman, Paul; Aherne, Wynne; Poeschke, Oliver; Dale, Trevor; Wienke, Dirk; Esdar, Christina; Rohdich, Felix; Raynaud, Florence; Clarke, Paul A.; Eccles, Suzanne A.; Stieber, Frank; Schiemann, Kai; Blagg, Julian.

WNT signaling is frequently deregulated in malignancy, particularly in colon cancer, and plays a key role in the generation and maintenance of cancer stem cells. The authors report the discovery and optimization of a 3,4,5-trisubstituted pyridine, 1-(3,5-Dichloropyridin-4-yl)piperidine-4-carboxamide (9), using a high-throughput cell-based reporter assay of WNT pathway activity. The authors demonstrate a twisted conformation about the pyridine-piperidine bond of (9) by small-mol. x-ray crystallog. Medicinal chem. optimization to maintain this twisted conformation, cognisant of physicochem. properties likely to maintain good cell permeability, led to 8-[3-Chloro-5-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]pyridin-4-yl]-2,8-diazaspiro[4,5]decan-1-one (74) (CCT251545), a potent small-mol. inhibitor of WNT signaling with good oral pharmacokinetics. The authors demonstrate inhibition of WNT pathway activity in a solid human tumor xenograft model with evidence for tumor growth inhibition following oral dosing. This work provides a successful example of hypothesis-driven medicinal chem. optimization from a singleton hit against a cell-based pathway assay without knowledge of the biochem. target.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

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: 254905-58-3, is researched, Molecular C13H24N2O3, about Discovery of Potent, Orally Bioavailable, Small-Molecule Inhibitors of WNT Signaling from a Cell-Based Pathway Screen, the main research direction is trisubstituted pyridine preparation bioavailability WNT signaling inhibitor antitumor.Recommanded Product: 254905-58-3.

WNT signaling is frequently deregulated in malignancy, particularly in colon cancer, and plays a key role in the generation and maintenance of cancer stem cells. The authors report the discovery and optimization of a 3,4,5-trisubstituted pyridine, 1-(3,5-Dichloropyridin-4-yl)piperidine-4-carboxamide (9), using a high-throughput cell-based reporter assay of WNT pathway activity. The authors demonstrate a twisted conformation about the pyridine-piperidine bond of (9) by small-mol. x-ray crystallog. Medicinal chem. optimization to maintain this twisted conformation, cognisant of physicochem. properties likely to maintain good cell permeability, led to 8-[3-Chloro-5-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]pyridin-4-yl]-2,8-diazaspiro[4,5]decan-1-one (74) (CCT251545), a potent small-mol. inhibitor of WNT signaling with good oral pharmacokinetics. The authors demonstrate inhibition of WNT pathway activity in a solid human tumor xenograft model with evidence for tumor growth inhibition following oral dosing. This work provides a successful example of hypothesis-driven medicinal chem. optimization from a singleton hit against a cell-based pathway assay without knowledge of the biochem. target.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Related Products of 254905-58-3. 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: tert-Butyl 4-(dimethylcarbamoyl)piperidine-1-carboxylate, is researched, Molecular C13H24N2O3, CAS is 254905-58-3, about Conformationally restrained carbamoylcholine homologues. Synthesis, pharmacology at neuronal nicotinic acetylcholine receptors and biostructural considerations. Author is de la Fuente Revenga, Mario; Balle, Thomas; Jensen, Anders A.; Froelund, Bente.

Exploration of small selective ligands for the nicotinic acetylcholine receptors (nAChRs) based on acetylcholine (ACh) has led to the development of potent agonists with clear preference for the α4β2 nAChR, the most prevalent nAChR subtype in the central nervous system. In this work the authors present the continuation of these efforts aimed at increasing this subtype selectivity by introduction of conformational restriction in the carbamoylcholine homolog, 3-(dimethylaminobutyl) dimethylcarbamate (DMABC). The results highlight the importance of the N-carbamoyl substitution in α4β2-subtype selectivity. Moreover, the authors have confirmed the non-linear conformation of DMABC bound to nAChRs suggested by recent crystal structures of the compound in complex with the Lymnaea stagnalis ACh binding protein.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

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: 254905-58-3, is researched, Molecular C13H24N2O3, about Conformationally restrained carbamoylcholine homologues. Synthesis, pharmacology at neuronal nicotinic acetylcholine receptors and biostructural considerations, the main research direction is carbamoylcholine homolog pharmacol neuron nicotinic receptor ligand; Acetylcholine; Agonist; Conformational restriction; Docking; Nicotinic acetylcholine receptor.Recommanded Product: tert-Butyl 4-(dimethylcarbamoyl)piperidine-1-carboxylate.

Exploration of small selective ligands for the nicotinic acetylcholine receptors (nAChRs) based on acetylcholine (ACh) has led to the development of potent agonists with clear preference for the α4β2 nAChR, the most prevalent nAChR subtype in the central nervous system. In this work the authors present the continuation of these efforts aimed at increasing this subtype selectivity by introduction of conformational restriction in the carbamoylcholine homolog, 3-(dimethylaminobutyl) dimethylcarbamate (DMABC). The results highlight the importance of the N-carbamoyl substitution in α4β2-subtype selectivity. Moreover, the authors have confirmed the non-linear conformation of DMABC bound to nAChRs suggested by recent crystal structures of the compound in complex with the Lymnaea stagnalis ACh binding protein.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 254905-58-3, is researched, SMILESS is O=C(N1CCC(C(N(C)C)=O)CC1)OC(C)(C)C, Molecular C13H24N2O3Journal, Article, European Journal of Medicinal Chemistry called The influence of conformational restriction in the C-terminus of growth hormone secretagogues on their potency, Author is Peschke, Bernd; Ankersen, Michael; Bauer, Michael; Hansen, Thomas Kruse; Hansen, Birgit Sehested; Nielsen, Karin Kramer; Raun, Kirsten; Richter, Lutz; Westergaard, Lisbet, the main research direction is growth hormone secretagogue structure activity C terminal conformation.Application of 254905-58-3.

In order to obtain more potent growth hormone secretagogues, a comparison of ipamorelin and NN703 suggested the addition of a polar group at the C-terminus of NN703. A study was conducted using constrained amines for this purpose. Here, substituted 4-piperidinylamino- and 4-dimethylaminopiperidino-substituents were found to give the most active compounds A replacement of the 4-dimethylaminopiperidino-substituent with 4-hydroxypiperidino resulted in a series of compounds, which showed in vitro activity with EC50 values in the low nanomolar range, and favorable kinetic properties, such as 40% oral bioavailability. The most promising compound was also tested in a swine in vivo model, resulting in a growth hormone level with a Cmax of over 40 ng mL-1.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem