Tag: M.W=100-150

Application In Synthesis of 3-Pyridinecarboxaldehyde. Authors Gein, VL; Rubtsova, DD; Bobyleva, AA; Yankin, AN in MAIK NAUKA/INTERPERIODICA/SPRINGER published article about in [Gein, V. L.; Rubtsova, D. D.; Bobyleva, A. A.] Perm State Pharmaceut Acad, Perm 614990, Russia; [Yankin, A. N.] Natl Res Univ ITMO, St Petersburg 197101, Russia in 2020.0, Cited 5.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1

5-Aryl(heteryl)-1-hydroxyethyl-4-(furyl-2-carbonyl)-3-hydroxy-3-pyrroline-2-ones were synthesized via reactions of methyl ester of furyl-2-carbonylpyruvic acid with a mixture of aromatic or heterocyclic aldehyde and ethanolamine in dioxane. Antibacterial and antifungal activities of the synthesized compounds was studied.

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Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

An article Design, synthesis, and biological evaluation of 5-((8-methoxy-2-methylquinolin-4-yl)amino)-1H-indole-2-carbohydrazide derivatives as novel Nur77 modulators WOS:000573916100021 published article about CELL-DEATH; ENDOPLASMIC-RETICULUM; DUAL ROLES; APOPTOSIS; EXPRESSION; STRESS; UBIQUITINATION; METABOLISM; ACTIVATION; INDUCTION in [Li, Baicun; Yao, Jie; Guo, Kaiqiang; He, Fengming; Chen, Kun; Lin, Zongxin; Liu, Shunzhi; Huang, Jiangang; Wu, Qiaoqiong; Fang, Meijuan; Zeng, Jinzhang; Wu, Zhen] Xiamen Univ, Sch Pharmaceut Sci, Fujian Prov Key Lab Innovat Drug Target Res, Xiamen 361102, Peoples R China; [Li, Baicun; Yao, Jie; Guo, Kaiqiang; He, Fengming; Chen, Kun; Lin, Zongxin; Liu, Shunzhi; Huang, Jiangang; Wu, Qiaoqiong; Fang, Meijuan; Zeng, Jinzhang; Wu, Zhen] Xiamen Univ, Sch Pharmaceut Sci, State Key Lab Cellular Stress Biol, Xiamen 361102, Peoples R China; [Li, Baicun] Chinese Acad Med Sci, Inst Basic Med Sci, Dept Physiol, State Key Lab Med Mol Biol, Beijing 100005, Peoples R China; [Li, Baicun] Peking Union Med Coll, Sch Basic Med, Beijing 100005, Peoples R China in 2020.0, Cited 74.0. Recommanded Product: 500-22-1. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1

Nur77 is a potential target for the treatment of cancer such as HCC. Herein, we detailed the discovery of a novel series of 5-((8-methoxy-2-methylquinolin-4-yl)amino)-1H-indole-2-carbohydrazide derivatives as potential Nur77 modulators. The studies of antiproliferative activity and Nur77-binding affinity of target compounds resulted in the discovery of a lead candidate (10g), which was a good Nur77 binder (K-D = 3.58 +/- 0.16 mu M) with a broad-spectrum antiproliferative activity against all tested hepatoma cells (IC50 < 2.0 mu M) and was low toxic to normal LO2 cells. 10g could up-regulate Nur77 expression and mediate sub-cellular localization of Nur77 to induce apoptosis in hepatocellular carcinoma cell lines, which relied on 10g inducing Nur77-dependent autophagy and endoplasmic reticulum stress as the upstream of apoptosis. Moreover, the in vivo assays verified that 10g significantly inhibited xenograft tumor growth. These results indicate that 10g has the potential to be developed as a novel Nur77-targeting anti-hepatoma drug. (C) 2020 Elsevier Masson SAS. All rights reserved. Recommanded Product: 500-22-1. About 3-Pyridinecarboxaldehyde, If you have any questions, you can contact Li, BC; Yao, J; Guo, KQ; He, FM; Chen, K; Lin, ZX; Liu, SZ; Huang, JG; Wu, QQ; Fang, MJ; Zeng, JZ; Wu, Z or concate me.

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

An article Structure-based design and synthesis of novel furan-diketopiperazine-type derivatives as potent microtubule inhibitors for treating cancer WOS:000526982300002 published article about IN-VITRO; AGENT; MECHANISM; INSIGHTS in [Ding, Zhongpeng; Li, Feifei; Zhong, Changjiang; Liu, Yuqian; Zhao, Jianchun; Li, Wenbao] Ocean Univ China, Sch Med & Pharm, Qingdao 266003, Peoples R China; [Li, Wenbao] Qingdao Natl Lab Marine Sci & Technol, Innovat Ctr Marine Drug Screening & Evaluat, Qingdao 266071, Peoples R China; [Li, Feng] Weifang Univ Sci & Technol, Shandong Peninsula Engn Res Ctr Comprehens Brine, Weifang 262700, Shandong, Peoples R China; [Wang, Shixiao; Zhao, Jianchun; Li, Wenbao] Marine Biomed Res Inst Qingdao, Qingdao 266071, Peoples R China in 2020.0, Cited 24.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1. Recommanded Product: 3-Pyridinecarboxaldehyde

Plinabulin, a synthetic analog of the marine natural product diketopiperazine phenylahistin, displayed depolymerization effects on microtubules and targeted the colchicine site, which has been moved into phase III clinical trials for the treatment of non-small cell lung cancer (NSCLC) and the prevention of chemotherapy-induced neutropenia (CIN). To develop more potent anti-microtubule and cytotoxic derivatives, the co-crystal complexes of plinabulin derivatives were summarized and analyzed. We performed further modifications of the tert-butyl moiety or C-ring of imidazole-type derivatives to build a library of molecules through the introduction of different groups for novel skeletons. Our structure-activity relationship study indicated that compounds 17o (IC50 = 14.0 nM, NCI-H460) and 17p (IC50 = 2.9 nM, NCI-H460) with furan groups exhibited potent cytotoxic activities at the nanomolar level against various human cancer cell lines. In particular, the 5-methyl or methoxymethyl substituent of furan group could replace the alkyl group of imidazole at the 5-position to maintain cytotoxic activity, contradicting previous reports that the tert-butyl moiety at the 5-position of imidazole was essential for the activity of such compounds. Immunofluorescence assay indicated that compounds 17o and 17p could efficiently inhibit microtubule polymerization. Overall, the novel furan-diketopiperazine-type derivatives could be considered as a potential scaffold for the development of anti-cancer drugs.

Recommanded Product: 3-Pyridinecarboxaldehyde. Bye, fridends, I hope you can learn more about C6H5NO, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

In 2019.0 CHEM-EUR J published article about SITU CLICK-CHEMISTRY; BENZOTRIAZOLE-ASSISTED SYNTHESIS; PLASMINOGEN-ACTIVATOR SYSTEM; IN-SITU; MULTICOMPONENT REACTIONS; COMBINATORIAL CHEMISTRY; GUIDED SYNTHESIS; PROTEASE; ACETYLCHOLINESTERASE; AMINOALKYLATION in [Gladysz, Rafaela; Vrijdag, Johannes; Van Rompaey, Dries; Augustyns, Koen; De Winter, Hans; Van der Veken, Pieter] Univ Antwerp, Dept Pharmaceut Sci, Lab Med Chem UAMC, Univ Pl 1, B-2610 Antwerp, Belgium; [Vrijdag, Johannes; Lambeir, Anne-Marie] Univ Antwerp, Dept Pharmaceut Sci, Lab Med Biochem, Univ Pl 1, B-2610 Antwerp, Belgium in 2019.0, Cited 72.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1. Computed Properties of C6H5NO

Target-guided synthesis (TGS) has emerged as a promising strategy in drug discovery. Although reported examples of TGS generally involve two-component reactions, there is a strong case for developing target-guided versions of three-component reactions (3CRs) because of their potential to deliver highly diversified druglike molecules. To this end, the Groebke-Blackburn-Bienayme reaction was selected as a model 3CR. We recently reported a series of druglike urokinase inhibitors, and these serve as reference compounds in the present study. Due to the limited number of literature reports on target-guided 3CRs, multiple experimental parameters were optimized here. Most challenging was the formation of imine intermediates under near-physiological conditions. This aspect was addressed by exploring chemical imine stabilization strategies. Notably, imines are also crucial intermediates of other 3CRs. Such systematic studies are strongly required for further development of the TGS domain but are largely absent in the literature. Hence, this work is intended as a reference for future multicomponent-based TGS studies.

Bye, fridends, I hope you can learn more about C6H5NO, If you have any questions, you can browse other blog as well. See you lster.. Computed Properties of C6H5NO

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

Galli, U; Hysenlika, R; Meneghetti, F; Del Grosso, E; Pelliccia, S; Novellino, E; Giustiniano, M; Tron, GC in [Galli, Ubaldina; Hysenlika, Rejdia; Del Grosso, Erika; Tron, Gian Cesare] Univ Piemonte Orientale, Dipartimento Sci Farmaco, I-28100 Novara, Italy; [Meneghetti, Fiorella] Univ Milan, Dipartimento Sci Farmaceut, I-20133 Milan, Italy; [Pelliccia, Sveva; Novellino, Ettore; Giustiniano, Mariateresa] Univ Napoli Federico II, Dipartimento Farm, I-80131 Naples, Italy published Exploiting the Nucleophilicity of the Nitrogen Atom of Imidazoles: One-Pot Three-Component Synthesis of Imidazo-Pyrazines in 2019.0, Cited 38.0. Category: pyridine-derivatives. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1.

A novel one-pot multicomponent reaction to synthesize substituted imidazopyrazines is described. In brief, 1H-(imidazol-5-yl)-N-substituted methanamines react with aldehydes and isocyanides in methanol at room temperature to give imidazopyrazine derivatives in excellent yields. The imidazole nitrogen atom was able to intercept the nascent nitrilium ion, channeling the reaction toward to the sole formation of imidazopyrazines, suppressing the competitive formation of other possible side products deriving from the reaction with the high-energy nitrilium ion. The number of examples and the variability of the nature of isocyanides, aldehydes, and amine components herein employed, witness the robustness of this novel methodology.

Category: pyridine-derivatives. Bye, fridends, I hope you can learn more about C6H5NO, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

In 2019.0 TETRAHEDRON published article about HYPOPHOSPHITE COMBINATION SYSTEM; PHENYL SULFONE; NUCLEOPHILIC DIFLUOROMETHYLATION; CARBONYL-COMPOUNDS; SULFIDE OXIDATION; RANEY-NICKEL; REDUCTIVE DESULFURIZATION; STEREOSELECTIVE-SYNTHESIS; HIGH ENANTIOSELECTIVITY; REFORMATSKY REACTION in [Batisse, Chloe; Davila, Maria F. Cespedes; Messara, Amelia; Panossian, Armen; Hanquet, Gilles; Leroux, Frederic R.] Univ Strasbourg, Univ Haute Alsace, CNRS, ECPM,UMR LIMA 7042, 25 Rue Becquerel, F-67087 Strasbourg, France; [Castello, Marco] Univ Basilicata, Dipartimento Sci, Via Nazario Sauro 85, I-85100 Potenza, Italy; [Davila, Maria F. Cespedes; Vivet, Bertrand; Marciniak, Gilbert] Sanofi Aventis R&D, 16 Rue Ankara, F-67080 Strasbourg, France in 2019.0, Cited 143.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1. Recommanded Product: 3-Pyridinecarboxaldehyde

The -CHF2 moiety has shown a growing interest in pharmaceutical and agrochemical applications over the last few years. Its introduction is therefore a current research topic for organic chemists. Several groups have reported the synthesis of difluoromethylated compounds. However, the more challenging enantioselective introduction of the difluoromethyl group has been scarcely described yet. We recently developed a new strategy, based on the use of an enantiopure difluoromethyl sulfoxide used as chiral and traceless auxiliary, for the synthesis of highly enantioenriched alpha-difluoromethyl alcohols. The first method developed in our laboratory aims to access highly stereoenriched alpha,alpha-difluoro-beta-hydroxysulfoxides through the condensation of the enantiopure difluoromethyl sulfoxide on carbonyl derivatives. It is noteworthy that highly diastereo- and enantioenriched alpha,alpha-difluoro-beta-hydroxysulfoxides can also be accessed after the diastereoselective reduction of highly enantioenriched alpha,alpha-difluoro-beta-ketosulfoxides. Finally, the expected difluoromethyl-substituted alcohols can be obtained after removal of the chiral auxiliary with complete retention of stereoenrichment at carbon. (C) 2019 Elsevier Ltd. All rights reserved.

Bye, fridends, I hope you can learn more about C6H5NO, If you have any questions, you can browse other blog as well. See you lster.. Recommanded Product: 3-Pyridinecarboxaldehyde

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

Application In Synthesis of 3-Pyridinecarboxaldehyde. Authors Gein, VL; Rubtsova, DD; Bobyleva, AA; Yankin, AN in MAIK NAUKA/INTERPERIODICA/SPRINGER published article about in [Gein, V. L.; Rubtsova, D. D.; Bobyleva, A. A.] Perm State Pharmaceut Acad, Perm 614990, Russia; [Yankin, A. N.] Natl Res Univ ITMO, St Petersburg 197101, Russia in 2020.0, Cited 5.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1

5-Aryl(heteryl)-1-hydroxyethyl-4-(furyl-2-carbonyl)-3-hydroxy-3-pyrroline-2-ones were synthesized via reactions of methyl ester of furyl-2-carbonylpyruvic acid with a mixture of aromatic or heterocyclic aldehyde and ethanolamine in dioxane. Antibacterial and antifungal activities of the synthesized compounds was studied.

Bye, fridends, I hope you can learn more about C6H5NO, If you have any questions, you can browse other blog as well. See you lster.. Application In Synthesis of 3-Pyridinecarboxaldehyde

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

An article Design, synthesis, and biological evaluation of 5-((8-methoxy-2-methylquinolin-4-yl)amino)-1H-indole-2-carbohydrazide derivatives as novel Nur77 modulators WOS:000573916100021 published article about CELL-DEATH; ENDOPLASMIC-RETICULUM; DUAL ROLES; APOPTOSIS; EXPRESSION; STRESS; UBIQUITINATION; METABOLISM; ACTIVATION; INDUCTION in [Li, Baicun; Yao, Jie; Guo, Kaiqiang; He, Fengming; Chen, Kun; Lin, Zongxin; Liu, Shunzhi; Huang, Jiangang; Wu, Qiaoqiong; Fang, Meijuan; Zeng, Jinzhang; Wu, Zhen] Xiamen Univ, Sch Pharmaceut Sci, Fujian Prov Key Lab Innovat Drug Target Res, Xiamen 361102, Peoples R China; [Li, Baicun; Yao, Jie; Guo, Kaiqiang; He, Fengming; Chen, Kun; Lin, Zongxin; Liu, Shunzhi; Huang, Jiangang; Wu, Qiaoqiong; Fang, Meijuan; Zeng, Jinzhang; Wu, Zhen] Xiamen Univ, Sch Pharmaceut Sci, State Key Lab Cellular Stress Biol, Xiamen 361102, Peoples R China; [Li, Baicun] Chinese Acad Med Sci, Inst Basic Med Sci, Dept Physiol, State Key Lab Med Mol Biol, Beijing 100005, Peoples R China; [Li, Baicun] Peking Union Med Coll, Sch Basic Med, Beijing 100005, Peoples R China in 2020.0, Cited 74.0. Recommanded Product: 500-22-1. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1

Nur77 is a potential target for the treatment of cancer such as HCC. Herein, we detailed the discovery of a novel series of 5-((8-methoxy-2-methylquinolin-4-yl)amino)-1H-indole-2-carbohydrazide derivatives as potential Nur77 modulators. The studies of antiproliferative activity and Nur77-binding affinity of target compounds resulted in the discovery of a lead candidate (10g), which was a good Nur77 binder (K-D = 3.58 +/- 0.16 mu M) with a broad-spectrum antiproliferative activity against all tested hepatoma cells (IC50 < 2.0 mu M) and was low toxic to normal LO2 cells. 10g could up-regulate Nur77 expression and mediate sub-cellular localization of Nur77 to induce apoptosis in hepatocellular carcinoma cell lines, which relied on 10g inducing Nur77-dependent autophagy and endoplasmic reticulum stress as the upstream of apoptosis. Moreover, the in vivo assays verified that 10g significantly inhibited xenograft tumor growth. These results indicate that 10g has the potential to be developed as a novel Nur77-targeting anti-hepatoma drug. (C) 2020 Elsevier Masson SAS. All rights reserved. Recommanded Product: 500-22-1. About 3-Pyridinecarboxaldehyde, If you have any questions, you can contact Li, BC; Yao, J; Guo, KQ; He, FM; Chen, K; Lin, ZX; Liu, SZ; Huang, JG; Wu, QQ; Fang, MJ; Zeng, JZ; Wu, Z or concate me.

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

An article Structure-based design and synthesis of novel furan-diketopiperazine-type derivatives as potent microtubule inhibitors for treating cancer WOS:000526982300002 published article about IN-VITRO; AGENT; MECHANISM; INSIGHTS in [Ding, Zhongpeng; Li, Feifei; Zhong, Changjiang; Liu, Yuqian; Zhao, Jianchun; Li, Wenbao] Ocean Univ China, Sch Med & Pharm, Qingdao 266003, Peoples R China; [Li, Wenbao] Qingdao Natl Lab Marine Sci & Technol, Innovat Ctr Marine Drug Screening & Evaluat, Qingdao 266071, Peoples R China; [Li, Feng] Weifang Univ Sci & Technol, Shandong Peninsula Engn Res Ctr Comprehens Brine, Weifang 262700, Shandong, Peoples R China; [Wang, Shixiao; Zhao, Jianchun; Li, Wenbao] Marine Biomed Res Inst Qingdao, Qingdao 266071, Peoples R China in 2020.0, Cited 24.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1. Recommanded Product: 3-Pyridinecarboxaldehyde

Plinabulin, a synthetic analog of the marine natural product diketopiperazine phenylahistin, displayed depolymerization effects on microtubules and targeted the colchicine site, which has been moved into phase III clinical trials for the treatment of non-small cell lung cancer (NSCLC) and the prevention of chemotherapy-induced neutropenia (CIN). To develop more potent anti-microtubule and cytotoxic derivatives, the co-crystal complexes of plinabulin derivatives were summarized and analyzed. We performed further modifications of the tert-butyl moiety or C-ring of imidazole-type derivatives to build a library of molecules through the introduction of different groups for novel skeletons. Our structure-activity relationship study indicated that compounds 17o (IC50 = 14.0 nM, NCI-H460) and 17p (IC50 = 2.9 nM, NCI-H460) with furan groups exhibited potent cytotoxic activities at the nanomolar level against various human cancer cell lines. In particular, the 5-methyl or methoxymethyl substituent of furan group could replace the alkyl group of imidazole at the 5-position to maintain cytotoxic activity, contradicting previous reports that the tert-butyl moiety at the 5-position of imidazole was essential for the activity of such compounds. Immunofluorescence assay indicated that compounds 17o and 17p could efficiently inhibit microtubule polymerization. Overall, the novel furan-diketopiperazine-type derivatives could be considered as a potential scaffold for the development of anti-cancer drugs.

Recommanded Product: 3-Pyridinecarboxaldehyde. Bye, fridends, I hope you can learn more about C6H5NO, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

In 2019.0 CHEM-EUR J published article about SITU CLICK-CHEMISTRY; BENZOTRIAZOLE-ASSISTED SYNTHESIS; PLASMINOGEN-ACTIVATOR SYSTEM; IN-SITU; MULTICOMPONENT REACTIONS; COMBINATORIAL CHEMISTRY; GUIDED SYNTHESIS; PROTEASE; ACETYLCHOLINESTERASE; AMINOALKYLATION in [Gladysz, Rafaela; Vrijdag, Johannes; Van Rompaey, Dries; Augustyns, Koen; De Winter, Hans; Van der Veken, Pieter] Univ Antwerp, Dept Pharmaceut Sci, Lab Med Chem UAMC, Univ Pl 1, B-2610 Antwerp, Belgium; [Vrijdag, Johannes; Lambeir, Anne-Marie] Univ Antwerp, Dept Pharmaceut Sci, Lab Med Biochem, Univ Pl 1, B-2610 Antwerp, Belgium in 2019.0, Cited 72.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1. Computed Properties of C6H5NO

Target-guided synthesis (TGS) has emerged as a promising strategy in drug discovery. Although reported examples of TGS generally involve two-component reactions, there is a strong case for developing target-guided versions of three-component reactions (3CRs) because of their potential to deliver highly diversified druglike molecules. To this end, the Groebke-Blackburn-Bienayme reaction was selected as a model 3CR. We recently reported a series of druglike urokinase inhibitors, and these serve as reference compounds in the present study. Due to the limited number of literature reports on target-guided 3CRs, multiple experimental parameters were optimized here. Most challenging was the formation of imine intermediates under near-physiological conditions. This aspect was addressed by exploring chemical imine stabilization strategies. Notably, imines are also crucial intermediates of other 3CRs. Such systematic studies are strongly required for further development of the TGS domain but are largely absent in the literature. Hence, this work is intended as a reference for future multicomponent-based TGS studies.

Bye, fridends, I hope you can learn more about C6H5NO, If you have any questions, you can browse other blog as well. See you lster.. Computed Properties of C6H5NO

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem