Tag: M.W=100-150

An article Structure-guided design of anti-cancer ribonucleotide reductase inhibitors WOS:000454985100001 published article about ACCURATE DOCKING; DNA-REPLICATION; NITRIC-OXIDE; MECHANISM; GEMCITABINE; 2-CHLORO-9-(2-DEOXY-2-FLUORO-BETA-D-ARABINOFURANOSYL)ADENINE; METABOLISM; DAMAGE; GLIDE; 2′,2′-DIFLUORO-2′-DEOXYCYTIDINE in [Misko, Tessianna A.; Dealwis, Chris G.] Case Western Reserve Univ, Sch Med, Dept Pharmacol, 10900 Euclid Ave, Cleveland, OH 44106 USA; [Liu, Yi-Ting; Lee, Hsueh-Yun] Taipei Med Univ, Coll Pharm, Sch Pharm, 250 Wuxing St, Taipei 11031, Taiwan; [Harris, Michael E.] Univ Florida, Dept Chem, Gainesville, FL 32611 USA; [Oleinick, Nancy L.] Case Western Reserve Univ, Sch Med, Dept Radiat Oncol, Cleveland, OH 44106 USA; [Pink, John] Case Western Reserve Univ, Case Comprehens Canc Ctr, Sch Med, Cleveland, OH 44106 USA; [Lee, Hsueh-Yun] Taipei Med Univ, Coll Pharm, PhD Program Biotechnol Res & Dev, Taipei, Taiwan; [Dealwis, Chris G.] Case Western Reserve Univ, Ctr Prote, Dept Chem, Cleveland, OH 44106 USA in 2019.0, Cited 50.0. Name: 3-Pyridinecarboxaldehyde. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1

Ribonucleotide reductase (RR) catalyses the rate-limiting step of dNTP synthesis, establishing it as an important cancer target. While RR is traditionally inhibited by nucleoside-based antimetabolites, we recently discovered a naphthyl salicyl acyl hydrazone-based inhibitor (NSAH) that binds reversibly to the catalytic site (C-site). Here we report the synthesis and in vitro evaluation of 13 distinct compounds (TP1-13) with improved binding to hRR over NSAH (TP8), with lower K-D’s and more predicted residue interactions. Moreover, TP6 displayed the greatest growth inhibiting effect in the Panc1 pancreatic cancer cell line with an IC50 of 0.393 mu M. This represents more than a 2-fold improvement over NSAH, making TP6 the most potent compound against pancreatic cancer emerging from the hydrazone inhibitors. NSAH was optimised by the addition of cyclic and polar groups replacing the naphthyl moiety, which occupies the phosphate-binding pocket in the C-site, establishing a new direction in inhibitor design.

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

SDS of cas: 500-22-1. In 2020.0 ORG LETT published article about PHOSPHINE-PHOSPHITE LIGANDS; CHEMISTRY; OLEFINS; STEREOCHEMISTRY; INTERCONVERSION; DERIVATIVES; MECHANISM; NITRILES; ALKENES in [Frye, Nils L.; Bhunia, Anup; Studer, Armido] Westfalische Wilhelms Univ, Organ Chem Inst, D-48149 Munster, Germany in 2020.0, Cited 45.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1.

Hydrocyanation in the absence of toxic HCN gas is highly desirable. Addressing that challenge, transition-metal-catalyzed transfer hydrocyanation using safe HCN precursors has been developed, but these reagents generally require a Lewis acid for activation, and the control of regioselectivity often remains problematic. In this Letter, a Ni-catalyzed highly Markovnikov-selective transfer hydrocyanation that operates in the absence of any Lewis acid is reported. The readily prepared pro-aromatic 1-isopropylcyclohexa-2,5-diene-1-carbonitrile is used as the HCN source, and the reaction shows a broad substrate scope and high functional group tolerance. Terminal styrene derivatives, dienes, and internal alkynes are converted with good to excellent selectivities. Mechanistic studies provide insights into the origin of the regioselectivity.

SDS of cas: 500-22-1. Welcome to talk about 500-22-1, If you have any questions, you can contact Frye, NL; Bhunia, A; Studer, A or send Email.

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

An article 1,8-Diazabicyclo[5.4.0]undec-7-ene-mediated formation of N-sulfinyl imines WOS:000509575100010 published article about TERT-BUTANESULFINYL IMINES; ASYMMETRIC-SYNTHESIS; DIASTEREOSELECTIVE SYNTHESIS; DIRECT CONDENSATION; ALDEHYDES; SULFINIMINES in [Ramaiah, Manjunatha M.; Shubha, Priya Babu] Univ Mysore, Dept Studies Chem, Synthet Lab, Mysore 570006, Karnataka, India; [Prabhala, Pavan Kumar] Acharya Nagarjuna Univ, SVRM Coll, Dept Chem, Guntur, Andhra Pradesh, India; [Shivananju, Nanjunda Swamy] JSS Sci & Technol Univ, Dept Biotechnol, Mysore, Karnataka, India in 2020.0, Cited 31.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1. Category: pyridine-derivatives

A facile and efficient method was developed for the preparation of a variety of aryl, heteroaryl, and alkyl N-sulfinyl imines using 1,8-diazabicyclo[5.4.0]undec-7-ene. In addition to tert-butanesulfinamide, the condensation is also effective with p-toluenesulfinamide. The reaction was performed at room temperature and produces the corresponding N-sulfinyl imines in excellent yields in the absence of acids, metals, and additives. This methodology is also useful for the preparation of N-sulfinyl imines on gram scale. A one-pot synthesis was developed using aryl and heteroaryl alcohols with both tert-butanesulfinamide and p-toluenesulfinamide at room temperature, resulting in the corresponding N-sulfinyl imines with good yields.

Category: pyridine-derivatives. Welcome to talk about 500-22-1, If you have any questions, you can contact Ramaiah, MM; Shubha, PB; Prabhala, PK; Shivananju, NS or send Email.

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

An article Synthesis of novel quinoline-based thiadiazole, evaluation of their antileishmanial potential and molecular docking studies WOS:000462472500011 published article about ALPHA-GLUCOSIDASE INHIBITORS; IN-VITRO EVALUATION; DERIVATIVES; BENZOTHIADIAZOLE; COMPLEXES; POLYMERS; DESIGN in [Almandil, Noor Barak; Taha, Muhammad; Ibrahim, Mohamed; Mosaddik, Ashik] Imam Abdulrahman Bin Faisal Univ, Inst Res & Med Consultat, Dept Clin Pharm, POB 1982, Dammam 31441, Saudi Arabia; [Rahim, Fazal] Hazara Univ, Dept Chem, Mansehra 21300, Pakistan; [Wadood, Abdul] Abdul Wali Khan Univ Mardan, Dept Biochem, Mardan 23200, Pakistan; [Imran, Syahrul] Univ Teknol MARA UiTM, Atta ur Rahman Inst Nat Prod Discovery, Puncak Alam Campus, Bandar Puncak Alam 42300, Selangor De, Malaysia; [Alqahtani, Mohammed A.; Bamarouf, Yasser A.; Gollapalli, Mohammed] Imam Abdulrahman Bin Faisal Univ, CCSIT, POB 1982, Dammam 31441, Saudi Arabia in 2019.0, Cited 54.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1. Safety of 3-Pyridinecarboxaldehyde

New series of quinoline-based thiadiazole analogs (1-20) were synthesized, characterized by EI-MS, H-1 NMR and C-13 NMR. All synthesized compounds were subjected to their antileishmanial potential. Sixteen analogs 1-10, 12, 13, 16, 17, 18 and 19 with IC50 values in the range of 0.04 +/- 0.01 to 5.60 +/- 0.21 mu M showed tremendously potent inhibition as compared to the standard pentamidine with IC50 value 7.02 +/- 0.09 mu M. Analogs 11, 14, 15 and 20 with IC50 8.20 +/- 0.35, 9.20 +/- 0.40, 7.20 +/- 0.20 and 9.60 +/- 0.40 mu M respectively showed good inhibition when compared with the standard. Structure-activity relationships have been also established for all compounds. Molecular docking studies were performed to determine the binding interaction of the compounds with the active site target.

Safety of 3-Pyridinecarboxaldehyde. Welcome to talk about 500-22-1, If you have any questions, you can contact Almandil, NB; Taha, M; Rahim, F; Wadood, A; Imran, S; Alqahtani, MA; Bamarouf, YA; Ibrahim, M; Mosaddik, A; Gollapalli, M or send Email.

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

Ramaiah, MM; Shubha, PB; Prabhala, PK; Shivananju, NS in [Ramaiah, Manjunatha M.; Shubha, Priya Babu] Univ Mysore, Dept Studies Chem, Synthet Lab, Mysore 570006, Karnataka, India; [Prabhala, Pavan Kumar] Acharya Nagarjuna Univ, SVRM Coll, Dept Chem, Guntur, Andhra Pradesh, India; [Shivananju, Nanjunda Swamy] JSS Sci & Technol Univ, Dept Biotechnol, Mysore, Karnataka, India published 1,8-Diazabicyclo[5.4.0]undec-7-ene-mediated formation of N-sulfinyl imines in 2020.0, Cited 31.0. COA of Formula: C6H5NO. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1.

A facile and efficient method was developed for the preparation of a variety of aryl, heteroaryl, and alkyl N-sulfinyl imines using 1,8-diazabicyclo[5.4.0]undec-7-ene. In addition to tert-butanesulfinamide, the condensation is also effective with p-toluenesulfinamide. The reaction was performed at room temperature and produces the corresponding N-sulfinyl imines in excellent yields in the absence of acids, metals, and additives. This methodology is also useful for the preparation of N-sulfinyl imines on gram scale. A one-pot synthesis was developed using aryl and heteroaryl alcohols with both tert-butanesulfinamide and p-toluenesulfinamide at room temperature, resulting in the corresponding N-sulfinyl imines with good yields.

Welcome to talk about 500-22-1, If you have any questions, you can contact Ramaiah, MM; Shubha, PB; Prabhala, PK; Shivananju, NS or send Email.. COA of Formula: C6H5NO

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

In 2020 BEILSTEIN J ORG CHEM published article about COUPLED ELECTRON-TRANSFER; VICINAL DIAMINES; METAL-FREE; RADICAL-ADDITION; CATALYSIS; IMINES; DERIVATIVES; ARYLATION; REAGENTS; KETONES in [Tambe, Shrikant D.; Min, Kwan Hong; Iqbal, Naeem; Cho, Eun Jin] Chung Ang Univ, Dept Chem, 84 Heukseok Ro, Seoul 06974, South Korea in 2020, Cited 65. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1. Application In Synthesis of 3-Pyridinecarboxaldehyde

A simple photocatalytic method was developed for the synthesis of unsymmetrical 1,2-diamines by the unprecedented reductive coupling of N-benzylidene-[1,1′-biphenyl]-2-amines with an aliphatic amine. The presence of a phenyl substituent in the aniline moiety of the substrate was critical for the reactivity. The reaction proceeded via radical-radical cross-coupling of alpha-amino radicals generated by proton-coupled single-electron transfer in the presence of an Ir photocatalyst. On the other hand, symmetrical 1,2-diamines were selectively produced from the same starting materials by the judicious choice of the reaction conditions, showcasing the distinct reactivity of N-benzylidene-[1,1′-biphenyl]-2-amines. The developed method can be employed for the synthesis of various bulky vicinal diamines, which are potential ligands in stereoselective synthesis.

Welcome to talk about 500-22-1, If you have any questions, you can contact Tambe, SD; Min, KH; Iqbal, N; Cho, EJ or send Email.. Application In Synthesis of 3-Pyridinecarboxaldehyde

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

Authors Zhang, LJ; Yang, K; Li, CY; Sun, YQ in SPRINGER INTERNATIONAL PUBLISHING AG published article about EFFICIENT METHOD; DERIVATIVES; INHIBITOR in [Zhang, Li-Jie; Yang, Kang; Li, Chun-Yu; Sun, Ya-Quan] Yancheng Teachers Univ, Yancheng, Peoples R China; [Zhang, Li-Jie; Sun, Ya-Quan] Yancheng Tongda Pharmaceut Co Ltd, Yancheng, Peoples R China; [Sun, Ya-Quan] Jiangsu Marine Ind Res Inst, Yancheng, Peoples R China; [Sun, Ya-Quan] Jiangsu Tuoqiu Agrichem Co Ltd, Yancheng, Peoples R China in 2019.0, Cited 27.0. Safety of 3-Pyridinecarboxaldehyde. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1

In this work, a simple and green method for the convenient synthetic protocol of 2-substituted-1H-4-carboxamide benzimidazole was reported from 2,3-diaminobenzamide and a variety of aldehydes by condensation. The results showed that 2,3-diaminobenzamide and aldehydes could react under visible light irradiation at ambient temperature in the presence of PYTZ and pumping air (or other oxidant) to obtain the desired compound with simple workup. The structures of 20 synthesized compounds were determined by NMR, IR and HRMS (new compound) techniques. The method was efficient, metal free, green, and selective.

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

Recently I am researching about DISTRIBUTED DRUG DISCOVERY; PARTICLE MESH EWALD; UGI-AZIDE; MOLECULAR-DYNAMICS; M1 FAMILY; STEREOSELECTIVE-SYNTHESIS; EFFICIENT GENERATION; CRYSTAL-STRUCTURE; STRUCTURAL BASIS; ALPHA-HYDRAZINO, Saw an article supported by the International Foundation for SciencesInternational Foundation for Science [F/4730-2]; BMBF project (Germany)Federal Ministry of Education & Research (BMBF) [CUBI7WTZ-068]; DAADDeutscher Akademischer Austausch Dienst (DAAD)European Commission; Alexander von Humboldt FoundationAlexander von Humboldt Foundation. Published in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER in ISSY-LES-MOULINEAUX ,Authors: Mendez, Y; De Armas, G; Perez, I; Rojas, T; Valdes-Tresanco, ME; Izquierdo, M; del Rivero, MA; Alvarez-Ginarte, YM; Valiente, PA; Soto, C; de Leon, L; Vasco, AV; Scott, WL; Westermann, B; Gonzalez-Bacerio, J; Rivera, DG. The CAS is 500-22-1. Through research, I have a further understanding and discovery of 3-Pyridinecarboxaldehyde. Computed Properties of C6H5NO

The Escherichia coli neutral M1-aminopeptidase (ePepN) is a novel target identified for the development of antimicrobials. Here we describe a solid-phase multicomponent approach which enabled the discovery of potent ePepN inhibitors. The on-resin protocol, developed in the frame of the Distributed Drug Discovery (D3) program, comprises the implementation of parallel Ugi-azide four-component reactions with resin-bound amino acids, thus leading to the rapid preparation of a focused library of tetrazole-peptidomimetics (TPMs) suitable for biological screening. By dose-response studies, three compounds were identified as potent and selective ePepN inhibitors, as little inhibitory effect was exhibited for the porcine ortholog aminopeptidase. The study allowed for the identification of the key structural features required for a high ePepN inhibitory activity. The most potent and selective inhibitor (TPM 11) showed a non-competitive inhibition profile of ePepN. We predicted that both diastereomers of compound TPM 11 bind to a site distinct from that occupied by the substrate. Theoretical models suggested that TPM 11 has an alternative inhibition mechanism that doesn’t involve Zn coordination. On the other hand, the activity landscape analysis provided a rationale for our findings. Of note, compound TMP 2 showed in vitro antibacterial activity against Escherichia coli. Furthermore, none of the three identified inhibitors is a potent haemolytic agent, and only two compounds showed moderate cytotoxic activity toward the murine myeloma P3X63Ag cells. These results point to promising compounds for the future development of rationally designed TPMs as antibacterial agents. (C) 2018 Elsevier Masson SAS. All rights reserved.

Welcome to talk about 500-22-1, If you have any questions, you can contact Mendez, Y; De Armas, G; Perez, I; Rojas, T; Valdes-Tresanco, ME; Izquierdo, M; del Rivero, MA; Alvarez-Ginarte, YM; Valiente, PA; Soto, C; de Leon, L; Vasco, AV; Scott, WL; Westermann, B; Gonzalez-Bacerio, J; Rivera, DG or send Email.. Computed Properties of C6H5NO

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

An article Cell cycle arrest and induction of apoptosis of newly synthesized pyranoquinoline derivatives under microwave irradiation WOS:000464742900005 published article about ANTITUMOR ACTIVITIES; IN-VITRO; CONSTITUENTS; ALKALOIDS; QUINOLINE; ACIDS; ASSAY in [Fouda, Ahmed M.; Youssef, Ayman M. S.] King Khalid Univ, Fac Sci, Chem Dept, Abha 61413, Saudi Arabia; [Youssef, Ayman M. S.] Fayoum Univ, Fac Sci, Chem Dept, Al Fayyum, Egypt; [Afifi, Tarek H.] Taibah Univ, Fac Sci, Chem Dept, Al Madinah Al Munawarah 30002, Saudi Arabia; [Mora, Ahmed; El-Agrody, Ahmed M.] Al Azhar Univ, Fac Sci, Chem Dept, Nar City 11884, Cairo, Egypt in 2019, Cited 47. Recommanded Product: 500-22-1. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1

A set of 2-amino-4-aryl-4H-pyrano[3,2-h]quinoline-3-carbonitrile derivatives were prepared via a one-pot, three-component condensation reaction between the substituted hydroxyquinoline derivatives, some aryl and/or hetaryl aldehydes, and malononitrile in an ethanol/piperidine solution in a microwave irradiation environment. The structure of the prepared compounds was instituted on the foundations of their spectral data: IR, H-1 NMR, C-13 NMR, and MS. Four human cancer cell lines, MCF-7, HCT-116, HepG-2, and A549 were utilized to evaluate the antiproliferative properties of the target compounds in comparison to the positive controls, Vinblastine and Colchicine using the MTT viability assay. The cell cycle arrest behavior, detected by propidium iodide as well as the apoptosis induction, which was monitored by the flow cytometer, using the Annexin V-FITC kits, was investigated. The results illustrated that the potent cytotoxic compounds induce cell cycle arrest at the G2/M phases and trigger apoptosis in the different tested cancer cells. Finally, the structure-activity relationship (SAR) study showcases the substitution of some specific groups at the 4-, 6-, and 9-positions in the prepared 2-amino-4H-pyrano[3,2-h]quinoline derivatives, which indicates that the lipophilicity manipulates the ability of these moieties against the diverse cell lines.

Recommanded Product: 500-22-1. 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

An article An L-threonine aldolase for asymmetric synthesis of beta-hydroxy-alpha-amino acids WOS:000573599600004 published article about DYNAMIC KINETIC RESOLUTION; ESCHERICHIA-COLI; SUBSTRATE; MECHANISM in [Wang, Li-Chao; Xu, Lian; Su, Bing-Mei; Lin, Juan] Fuzhou Univ, Coll Chem Engn, Fuzhou 350116, Peoples R China; [Wang, Li-Chao; Xu, Lian; Xu, Xin-Qi; Su, Bing-Mei; Lin, Juan] Fuzhou Univ, Coll Biol Sci & Engn, Fuzhou 350116, Peoples R China in 2020.0, Cited 33.0. Formula: C6H5NO. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1

L-threonine aldolase (LTA) is a PLP-dependent enzyme that can reversibly catalyze aldol reaction of glycine and acetaldehyde to produce beta-hydroxy-alpha-amino acids. In the present work, a putative Ita gene from Actinocorallia herbida (AhLTA) was mined and over-expressed in Escherichia coli BL21 (DE3). The substrate spectrum assay indicated that AhLTA only used glycine as donor substrate and tolerated a wild range of aromatic aldehydes as acceptor substrates. It was found that the type and position of substituents in the aromatic aldehydes exerted a significant impact on the activity and stereoselectivity at beta-carbon of AhLTA. Among those substrates, AhLTA could catalyze glycine and 4-methylsulphonyl benzaldehyde (14a) to produce L-threo-4-methylsulfonylphenylserine ((2S,3R)-14b) with high conversion (94.4%) and moderate stereoselectivity (19% de). By conditional optimization, the de value of (2S, 3R)-14b was improved to 61% and the conversion was 75%. Taken together, our study suggested that AhLTA might be a promising catalyst for producing chiral beta-hydroxy-alpha-amino acids. (C) 2020 Elsevier Ltd. All rights reserved.

Formula: C6H5NO. 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