Tag: M.W:200-300

Related Products of 276684-04-9. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 5-(3,4-Dichlorophenyl)-1H-pyrazole-3-carboxylic acid, is researched, Molecular C10H6Cl2N2O2, CAS is 276684-04-9, about Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors. Author is DiMauro, Erin F.; Altmann, Stephen; Berry, Loren M.; Bregman, Howard; Chakka, Nagasree; Chu-Moyer, Margaret; Bojic, Elma Feric; Foti, Robert S.; Fremeau, Robert; Gao, Hua; Gunaydin, Hakan; Guzman-Perez, Angel; Hall, Brian E.; Huang, Hongbing; Jarosh, Michael; Kornecook, Thomas; Lee, Josie; Ligutti, Joseph; Liu, Dong; Moyer, Bryan D.; Ortuno, Daniel; Rose, Paul E.; Schenkel, Laurie B.; Taborn, Kristin; Wang, Jean; Wang, Yan; Yu, Violeta; Weiss, Matthew M..

The majority of potent and selective hNaV1.7 inhibitors possess common pharmacophoric features that include a heteroaryl sulfonamide headgroup and a lipophilic aromatic tail group. Recently, reports of similar aromatic tail groups in combination with an acyl sulfonamide headgroup have emerged, with the acyl sulfonamide bestowing levels of selectivity over hNaV1.5 comparable to the heteroaryl sulfonamide. Beginning with com. available carboxylic acids that met selected pharmacophoric requirements in the lipophilic tail, a parallel synthetic approach was applied to rapidly generate the derived acyl sulfonamides. A biaryl acyl sulfonamide hit from this library was elaborated, optimizing for potency and selectivity with attention to physicochem. properties. The resulting novel leads are potent, ligand and lipophilic efficient, and selective over hNaV1.5. Representative lead I demonstrates selectivity over other human NaV isoforms and good pharmacokinetics in rodents. The biaryl acyl sulfonamides reported herein may also offer ADME advantages over known heteroaryl sulfonamide inhibitors.

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Pyrimidine | C4H4N2 – PubChem,
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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, Phosphorus, Sulfur and Silicon and the Related Elements called Utility of β-(3,4-dichlorobenzoyl)-α-(phenylthio)propionic acid in heterocyclic synthesis, Author is Mahmoud, M. R.; Soliman, E. A.; Ibrahim, G. A.; Rabie, A. M., which mentions a compound: 276684-04-9, SMILESS is O=C(C1=NNC(C2=CC=C(Cl)C(Cl)=C2)=C1)O, Molecular C10H6Cl2N2O2, Electric Literature of C10H6Cl2N2O2.

β-(3,4-Dichlorobenzoyl)-α-(phenylthio)propionic acid (I) was prepared via the treatment of β-(3,4-dichlorobenzoyl)acrylic acid (II) with thiophenol in dry benzene. The reactivity of I and II with different nucleophilic reagents was investigated; the mass spectra of some products are discussed.

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Reference:
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, Phosphorus, Sulfur and Silicon and the Related Elements called Utility of β-(3,4-dichlorobenzoyl)-α-(phenylthio)propionic acid in heterocyclic synthesis, Author is Mahmoud, M. R.; Soliman, E. A.; Ibrahim, G. A.; Rabie, A. M., which mentions a compound: 276684-04-9, SMILESS is O=C(C1=NNC(C2=CC=C(Cl)C(Cl)=C2)=C1)O, Molecular C10H6Cl2N2O2, Electric Literature of C10H6Cl2N2O2.

β-(3,4-Dichlorobenzoyl)-α-(phenylthio)propionic acid (I) was prepared via the treatment of β-(3,4-dichlorobenzoyl)acrylic acid (II) with thiophenol in dry benzene. The reactivity of I and II with different nucleophilic reagents was investigated; the mass spectra of some products are discussed.

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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.Barlaam, Bernard; Casella, Robert; Cidado, Justin; Cook, Calum; De Savi, Chris; Dishington, Allan; Donald, Craig S.; Drew, Lisa; Ferguson, Andrew D.; Ferguson, Douglas; Glossop, Steve; Grebe, Tyler; Gu, Chungang; Hande, Sudhir; Hawkins, Janet; Hird, Alexander W.; Holmes, Jane; Horstick, James; Jiang, Yun; Lamb, Michelle L.; McGuire, Thomas M.; Moore, Jane E.; O’Connell, Nichole; Pike, Andy; Pike, Kurt G.; Proia, Theresa; Roberts, Bryan; San Martin, Maryann; Sarkar, Ujjal; Shao, Wenlin; Stead, Darren; Sumner, Neil; Thakur, Kumar; Vasbinder, Melissa M.; Varnes, Jeffrey G.; Wang, Jianyan; Wang, Lei; Wu, Dedong; Wu, Liangwei; Yang, Bin; Yao, Tieguang researched the compound: 5-Chloro-4-iodopyridin-2-amine( cas:1260667-65-9 ).Computed Properties of C5H4ClIN2.They published the article 《Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies》 about this compound( cas:1260667-65-9 ) in Journal of Medicinal Chemistry. Keywords: amidopyridine derivative AZD4573 preparation CDK9 inhibitor hematol malignancy. We’ll tell you more about this compound (cas:1260667-65-9).

A CDK9 inhibitor having short target engagement would enable a reduction of Mcl-1 activity, resulting in apoptosis in cancer cells dependent on Mcl-1 for survival. We report the optimization of a series of amidopyridines (from compound 2), focusing on properties suitable for achieving short target engagement after i.v. administration. By increasing potency and human metabolic clearance, we identified compound 24, a potent and selective CDK9 inhibitor with suitable predicted human pharmacokinetic properties to deliver transient inhibition of CDK9. Furthermore, the solubility of 24 was considered adequate to allow i.v. formulation at the anticipated ED. Short-term treatment with compound 24 led to a rapid dose- and time-dependent decrease of pSer2-RNAP2 and Mcl-1, resulting in cell apoptosis in multiple hematol. cancer cell lines. Intermittent dosing of compound 24 demonstrated efficacy in xenograft models derived from multiple hematol. tumors. Compound 24 is currently in clin. trials for the treatment of hematol. malignancies.

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Electric Literature of C10H6Cl2N2O2. 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: 5-(3,4-Dichlorophenyl)-1H-pyrazole-3-carboxylic acid, is researched, Molecular C10H6Cl2N2O2, CAS is 276684-04-9, about Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors. Author is DiMauro, Erin F.; Altmann, Stephen; Berry, Loren M.; Bregman, Howard; Chakka, Nagasree; Chu-Moyer, Margaret; Bojic, Elma Feric; Foti, Robert S.; Fremeau, Robert; Gao, Hua; Gunaydin, Hakan; Guzman-Perez, Angel; Hall, Brian E.; Huang, Hongbing; Jarosh, Michael; Kornecook, Thomas; Lee, Josie; Ligutti, Joseph; Liu, Dong; Moyer, Bryan D.; Ortuno, Daniel; Rose, Paul E.; Schenkel, Laurie B.; Taborn, Kristin; Wang, Jean; Wang, Yan; Yu, Violeta; Weiss, Matthew M..

The majority of potent and selective hNaV1.7 inhibitors possess common pharmacophoric features that include a heteroaryl sulfonamide headgroup and a lipophilic aromatic tail group. Recently, reports of similar aromatic tail groups in combination with an acyl sulfonamide headgroup have emerged, with the acyl sulfonamide bestowing levels of selectivity over hNaV1.5 comparable to the heteroaryl sulfonamide. Beginning with com. available carboxylic acids that met selected pharmacophoric requirements in the lipophilic tail, a parallel synthetic approach was applied to rapidly generate the derived acyl sulfonamides. A biaryl acyl sulfonamide hit from this library was elaborated, optimizing for potency and selectivity with attention to physicochem. properties. The resulting novel leads are potent, ligand and lipophilic efficient, and selective over hNaV1.5. Representative lead I demonstrates selectivity over other human NaV isoforms and good pharmacokinetics in rodents. The biaryl acyl sulfonamides reported herein may also offer ADME advantages over known heteroaryl sulfonamide inhibitors.

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Reference:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Electric Literature of C10H6Cl2N2O2. 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: 5-(3,4-Dichlorophenyl)-1H-pyrazole-3-carboxylic acid, is researched, Molecular C10H6Cl2N2O2, CAS is 276684-04-9, about Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors. Author is DiMauro, Erin F.; Altmann, Stephen; Berry, Loren M.; Bregman, Howard; Chakka, Nagasree; Chu-Moyer, Margaret; Bojic, Elma Feric; Foti, Robert S.; Fremeau, Robert; Gao, Hua; Gunaydin, Hakan; Guzman-Perez, Angel; Hall, Brian E.; Huang, Hongbing; Jarosh, Michael; Kornecook, Thomas; Lee, Josie; Ligutti, Joseph; Liu, Dong; Moyer, Bryan D.; Ortuno, Daniel; Rose, Paul E.; Schenkel, Laurie B.; Taborn, Kristin; Wang, Jean; Wang, Yan; Yu, Violeta; Weiss, Matthew M..

The majority of potent and selective hNaV1.7 inhibitors possess common pharmacophoric features that include a heteroaryl sulfonamide headgroup and a lipophilic aromatic tail group. Recently, reports of similar aromatic tail groups in combination with an acyl sulfonamide headgroup have emerged, with the acyl sulfonamide bestowing levels of selectivity over hNaV1.5 comparable to the heteroaryl sulfonamide. Beginning with com. available carboxylic acids that met selected pharmacophoric requirements in the lipophilic tail, a parallel synthetic approach was applied to rapidly generate the derived acyl sulfonamides. A biaryl acyl sulfonamide hit from this library was elaborated, optimizing for potency and selectivity with attention to physicochem. properties. The resulting novel leads are potent, ligand and lipophilic efficient, and selective over hNaV1.5. Representative lead I demonstrates selectivity over other human NaV isoforms and good pharmacokinetics in rodents. The biaryl acyl sulfonamides reported herein may also offer ADME advantages over known heteroaryl sulfonamide inhibitors.

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Synthesis and anticancer activity of heteroaromatic linked 4β-amido podophyllotoxins as apoptotic inducing agents》. Authors are Kamal, Ahmed; Tamboli, Jaki R.; Vishnuvardhan, M. V. P. S.; Adil, S. F.; Nayak, V. Lakshma; Ramakrishna, S..The article about the compound:5-(3,4-Dichlorophenyl)-1H-pyrazole-3-carboxylic acidcas:276684-04-9,SMILESS:O=C(C1=NNC(C2=CC=C(Cl)C(Cl)=C2)=C1)O).COA of Formula: C10H6Cl2N2O2. Through the article, more information about this compound (cas:276684-04-9) is conveyed.

A series of different heteroaromatic linked 4β-amidopodophyllotoxin conjugates were synthesized and evaluated for anticancer activity against five human cancer cell lines. Among the series, one of the compound I showed significant antiproliferative activity in A549 (lung cancer) cell line. Flow cytometric anal. showed that I arrested the cell cycle in the G2/M phase leading to caspase-3 dependent apoptotic cell death. Further, Hoechst 33258 staining and DNA fragmentation assay also suggests that I induces cell death by apoptosis.

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

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: 276684-04-9, is researched, SMILESS is O=C(C1=NNC(C2=CC=C(Cl)C(Cl)=C2)=C1)O, Molecular C10H6Cl2N2O2Journal, Phosphorus, Sulfur and Silicon and the Related Elements called Utility of β-(3,4-dichlorobenzoyl)-α-(phenylthio)propionic acid in heterocyclic synthesis, Author is Mahmoud, M. R.; Soliman, E. A.; Ibrahim, G. A.; Rabie, A. M., the main research direction is dichlorobenzoylphenylthiopropionic acid preparation reaction nucleophile.Category: pyrimidines.

β-(3,4-Dichlorobenzoyl)-α-(phenylthio)propionic acid (I) was prepared via the treatment of β-(3,4-dichlorobenzoyl)acrylic acid (II) with thiophenol in dry benzene. The reactivity of I and II with different nucleophilic reagents was investigated; the mass spectra of some products are discussed.

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

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 AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies, published in 2020-12-24, which mentions a compound: 1260667-65-9, mainly applied to amidopyridine derivative AZD4573 preparation CDK9 inhibitor hematol malignancy, Quality Control of 5-Chloro-4-iodopyridin-2-amine.

A CDK9 inhibitor having short target engagement would enable a reduction of Mcl-1 activity, resulting in apoptosis in cancer cells dependent on Mcl-1 for survival. We report the optimization of a series of amidopyridines (from compound 2), focusing on properties suitable for achieving short target engagement after i.v. administration. By increasing potency and human metabolic clearance, we identified compound 24, a potent and selective CDK9 inhibitor with suitable predicted human pharmacokinetic properties to deliver transient inhibition of CDK9. Furthermore, the solubility of 24 was considered adequate to allow i.v. formulation at the anticipated ED. Short-term treatment with compound 24 led to a rapid dose- and time-dependent decrease of pSer2-RNAP2 and Mcl-1, resulting in cell apoptosis in multiple hematol. cancer cell lines. Intermittent dosing of compound 24 demonstrated efficacy in xenograft models derived from multiple hematol. tumors. Compound 24 is currently in clin. trials for the treatment of hematol. malignancies.

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Pyrimidine | C4H4N2 – PubChem,
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Product Details of 276684-04-9. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 5-(3,4-Dichlorophenyl)-1H-pyrazole-3-carboxylic acid, is researched, Molecular C10H6Cl2N2O2, CAS is 276684-04-9, about Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors. Author is DiMauro, Erin F.; Altmann, Stephen; Berry, Loren M.; Bregman, Howard; Chakka, Nagasree; Chu-Moyer, Margaret; Bojic, Elma Feric; Foti, Robert S.; Fremeau, Robert; Gao, Hua; Gunaydin, Hakan; Guzman-Perez, Angel; Hall, Brian E.; Huang, Hongbing; Jarosh, Michael; Kornecook, Thomas; Lee, Josie; Ligutti, Joseph; Liu, Dong; Moyer, Bryan D.; Ortuno, Daniel; Rose, Paul E.; Schenkel, Laurie B.; Taborn, Kristin; Wang, Jean; Wang, Yan; Yu, Violeta; Weiss, Matthew M..

The majority of potent and selective hNaV1.7 inhibitors possess common pharmacophoric features that include a heteroaryl sulfonamide headgroup and a lipophilic aromatic tail group. Recently, reports of similar aromatic tail groups in combination with an acyl sulfonamide headgroup have emerged, with the acyl sulfonamide bestowing levels of selectivity over hNaV1.5 comparable to the heteroaryl sulfonamide. Beginning with com. available carboxylic acids that met selected pharmacophoric requirements in the lipophilic tail, a parallel synthetic approach was applied to rapidly generate the derived acyl sulfonamides. A biaryl acyl sulfonamide hit from this library was elaborated, optimizing for potency and selectivity with attention to physicochem. properties. The resulting novel leads are potent, ligand and lipophilic efficient, and selective over hNaV1.5. Representative lead I demonstrates selectivity over other human NaV isoforms and good pharmacokinetics in rodents. The biaryl acyl sulfonamides reported herein may also offer ADME advantages over known heteroaryl sulfonamide inhibitors.

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Reference:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia