Category: 500-22-1

Sonawane, V; Siddique, MUM; Jadav, SS; Sinha, BN; Jayaprakash, V; Chaudhuri, B in [Sonawane, Vinay; Chaudhuri, Bhabatosh] De Montfort Univ, Leicester Sch Pharm, Leicester LE1 9BH, Leics, England; [Siddique, Mohd Usman Mohd; Sinha, Barij Nayan; Jayaprakash, Venkatesan] Birla Inst Technol, Dept Pharmaceut Sci & Technol, Ranchi 835215, Bihar, India; [Jadav, Surender Singh] Indian Inst Chem Technol, CSIR, Hyderabad 500007, Telangana, India published Cink4T, a quinazolinone-based dual inhibitor of Cdk4 and tubulin polymerization, identified via ligand-based virtual screening, for efficient anticancer therapy in 2019, Cited 79. Product Details of 500-22-1. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1.

Inhibition of cyclin dependent kinase 4 (Cdk4) prevents cancer cells from entering the early G(0)/G(1) phase of the cell division cycle whereas inhibiting tubulin polymerization blocks cancer cells’ ability to undergo mitosis (M) late in the cell cycle. We had reported earlier that two non-planar and relatively non-toxic fascaplysin derivatives, an indole and a tryptoline, inhibit Cdk4 with IC50 values of 6.2 and 10 mu M, respectively. Serendipitously, we had also found that they inhibited tubulin polymerization. The molecules were efficacious in mouse tumor models. We have now identified Cink4T in a 59-compound quinazolinone library, designed on the basis of ligand-based virtual screening, as a compound that inhibits Cdk4 and tubulin. Its IC50 value for Cdk4 inhibition is 0.47 mu M and >50 mu M for inhibition of Cdk1, Cdk2, Cdk6, Cdk9. Cink4T inhibits tubulin polymerization with an IC50 of 0.6 mu M. Molecular modelling studies on Cink4T with Cdk4 and tubulin crystal structures lend support to these observations. Cancer cell cycle analyses confirm that Cink4T blocks cells at both G(0)/G(1) and M phases as it should if it were to inhibit both Cdk4 and tubulin polymerization. Our results show, for the very first time, that virtual screening can be used to design novel inhibitors that can potently block two crucial phases of the cell division cycle. (C) 2019 Elsevier Masson SAS. All rights reserved.

Product Details of 500-22-1. About 3-Pyridinecarboxaldehyde, If you have any questions, you can contact Sonawane, V; Siddique, MUM; Jadav, SS; Sinha, BN; Jayaprakash, V; Chaudhuri, B or concate me.

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

Application In Synthesis of 3-Pyridinecarboxaldehyde. In 2019 ORG LETT published article about GRIGNARD-REAGENTS; STEREOSELECTIVE-SYNTHESIS; ARYL; ALKYL; PALLADIUM; HALIDES; COMPLEXES; CHLORIDES in [Lu, Xiao-Lin; Peng, Xiao-Shui; Wong, Henry N. C.] Chinese Univ Hong Kong, Dept Chem, Shatin, Hong Kong, Peoples R China; [Lu, Xiao-Lin; Peng, Xiao-Shui; Wong, Henry N. C.] Chinese Univ Hong Kong, State Key Lab Synthet Chem, Shatin, Hong Kong, Peoples R China; [Peng, Xiao-Shui; Wong, Henry N. C.] Chinese Univ Hong Kong, Shenzhen Res Inst, Shenzhen Municipal Key Lab Chem Synth Med Organ M, 10 Second Yuexing Rd, Shenzhen 518507, Peoples R China; [Shannon, Mark] Univ Warwick, Dept Chem, Gibbet Hill, Coventry CV4 7AL, W Midlands, England in 2019, Cited 38. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1.

An efficient synthetic protocol involving iron-catalyzed cross-coupling reactions between organolithium compounds and alkenyl iodides as key coupling partners was achieved. More than 30 examples were obtained with moderate to good yields and high stereospecificity. Gram scale and synthetic applications of this procedure are recorded herein to demonstrate its feasibility and potential utilization.

About 3-Pyridinecarboxaldehyde, If you have any questions, you can contact Lu, XL; Shannon, M; Peng, XS; Wong, HNC or concate me.. Application In Synthesis of 3-Pyridinecarboxaldehyde

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

Recently I am researching about MOLECULAR-ORBITAL METHODS; FORMAL 4+1 CYCLOADDITION; GAUSSIAN-TYPE BASIS; STEREOCONTROLLED SYNTHESIS; ALLYLIC SUBSTITUTION; ASYMMETRIC-SYNTHESIS; GOLD CATALYSIS; CYCLOISOMERIZATION; ALCOHOLS; ETHERS, Saw an article supported by the Ministry of Higher Education and Scientific Research (MHESR)Ministry of Higher Education & Scientific Research (MHESR) [CMCU 17G1207]. Published in WILEY-V C H VERLAG GMBH in WEINHEIM ,Authors: Ben Gaied, L; Fincias, N; Garrec, J; El Kaim, L. The CAS is 500-22-1. Through research, I have a further understanding and discovery of 3-Pyridinecarboxaldehyde. HPLC of Formula: C6H5NO

5-endo-dig cyclization of O-propargyloxyamides, obtained through a Passerini reaction mediated by boric acid and subsequent propargylation, affords 2,5-dihydrofurans in the presence of tert-butylate. The mechanism of the reaction was studied by using DFT calculations and the results were compared with the behavior of analogous N-propargylamide derivatives.

HPLC of Formula: C6H5NO. About 3-Pyridinecarboxaldehyde, If you have any questions, you can contact Ben Gaied, L; Fincias, N; Garrec, J; El Kaim, L or concate me.

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

Application In Synthesis of 3-Pyridinecarboxaldehyde. I found the field of Pharmacology & Pharmacy very interesting. Saw the article Discovery of potent and selective inhibitors of the Escherichia coli M1-aminopeptidase via multicomponent solid-phase synthesis of tetrazole-peptidomimetics published in 2019.0, Reprint Addresses Rivera, DG (corresponding author), Univ Havana, Fac Chem, Ctr Nat Prod Res, Havana 10400, Cuba.; Valiente, PA; Gonzalez-Bacerio, J (corresponding author), Univ Havana, Fac Biol, Ctr Prot Studies, 25 & J, Havana 10400, Cuba.. The CAS is 500-22-1. Through research, I have a further understanding and discovery of 3-Pyridinecarboxaldehyde.

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.

About 3-Pyridinecarboxaldehyde, 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 concate me.. Application In Synthesis of 3-Pyridinecarboxaldehyde

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

An article Straightforward access to complex isoindolinones from the Ugi reaction of o-nitrobenzoic acid derivatives WOS:000498709600013 published article about MULTICOMPONENT REACTIONS; CONVERTIBLE ISOCYANIDE; RAPID ACCESS; CONDENSATION in [Kurva, Mahanandaiah; Kerim, Mansour Dole; El Kaim, Laurent] Ecole Polytech, Inst Polytech Paris, Lab Synth Organ, CNRS,ENSTA Paris,UMR 7652, 828 Bd Marechaux, F-91128 Palaiseau, France; [Kurva, Mahanandaiah; Gamez-Montano, Rocio] Univ Guanajuato, Dept Quim, Noria Alta S-N, Guanajuato 36050, Gto, Mexico in 2019.0, Cited 36.0. HPLC of Formula: C6H5NO. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1

The Ugi reaction of 2-nitrobenzoic acid derivatives has been used for a diversity oriented synthesis of complex isoindolinones via a SNAr reaction involving the peptidyl position. When the cyclization is triggered by strong bases such as potassium tert-butylate, the SNAr reaction is followed by a deamidification/oxidation sequence leading to 2-hydroxyisoindolinones. The latter may be further transformed into polycyclic fused isoindolinones via Pictet-Spengler type cyclization or O-alkylation/metathesis sequences.

HPLC of Formula: C6H5NO. About 3-Pyridinecarboxaldehyde, If you have any questions, you can contact Kurva, M; Kerim, MD; Gamez-Montano, R; El Kaim, L or concate me.

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

Computed Properties of C6H5NO. In 2019.0 J IRAN CHEM SOC published article about MICHAEL-CYCLOCONDENSATION REACTION; EFFICIENT CATALYST; 3-COMPONENT SYNTHESIS; DERIVATIVES; MALONONITRILE; ALDEHYDES; SOLVENTS in [Honarmand, Moones] Birjand Univ Technol, Fac Min Civil & Chem Engn, Dept Chem Engn, Birjand 97175569, Iran; [Tzani, Andromachi; Detsi, Anastasia] Natl Tech Univ Athens, Sch Chem Engn, Organ Chem Lab, Zografou Campus, Athens 15780, Greece in 2019.0, Cited 23.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1.

2-Hydroxyethyl-1-ammonium 3-hydroxypropane-1-sulfonate HAHS’ was synthesized as a novel ionic liquid and characterized by various techniques. HAHS’ ionic liquid was efficiently applied as a multifunctional promoter for the three-component synthesis of 2-amino-3-cyano-4H-pyrans. The 2-amino-3-cyano-4H-pyrans were produced not only in high to excellent yields but also no toxic solvent or catalyst was used. HAHS’ ionic liquid was recovered and reused four times without the considerable decreasing in its activity. The effect of hydroxyl groups in the structure of HAHS’ ionic liquid on its catalytic activity was studied. Moreover, the biodegradability potential of the ionic liquid was examined using the 5-day biological oxygen demand closed bottle test and the results showed that HAHS’ has remarkable biodegradability potential.

About 3-Pyridinecarboxaldehyde, If you have any questions, you can contact Honarmand, M; Tzani, A; Detsi, A or concate me.. Computed Properties of C6H5NO

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

An article Development of Bronsted Base-Photocatalyst Hybrid Systems for Highly Efficient C-C Bond Formation Reactions of Malonates with Styrenes WOS:000574920200025 published article about CATALYTIC RADICAL-ADDITION; PHOTOCHEMICAL MONOALKYLATION; ALKENES; SUBSTITUTION; REACTIVITY in [Bas, Sebastian; Yamashita, Yasuhiro; Kobayashi, Shu] Univ Tokyo, Sch Sci, Dept Chem, Bunkyo Ku, Tokyo 1130033, Japan in 2020, Cited 31. HPLC of Formula: C6H5NO. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1

Bronsted base-photocatalyst hybrid systems have been developed for reactions of malonates with styrene derivatives. The concept of this process lies in the photo-oxidation of catalytic amounts of the enolate to form reactive radicals that react with alkene double bonds under mild reaction conditions. This is an example of visible-light-activated C-C bond formation reactions of malonates with alkenes to realize high atom economy under very mild reaction conditions without using any transition-metal catalysts.

HPLC of Formula: C6H5NO. About 3-Pyridinecarboxaldehyde, If you have any questions, you can contact Bas, S; Yamashita, Y; Kobayashi, S or concate me.

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

Computed Properties of C6H5NO. In 2019.0 ACS MED CHEM LETT published article about ASYMMETRIC 1,3-DIPOLAR CYCLOADDITION in [Garner, Philip; Rathnayake, Upendra; Holloran, Nicholas] Washington State Univ, Dept Chem, Pullman, WA 99164 USA; [Cox, Philip B.; Erdman, Paul] AbbVie Inc, Discovery Chem & Technol, 1 North Waukegan Rd, N Chicago, IL 60064 USA in 2019.0, Cited 21.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1.

Fragment-based drug discovery (FBDD) is a well- established technology for lead compound generation in drug discovery. As this technology has evolved, the design of fragments for screening has also evolved to engender not just an understanding of the role of modulating the physicochemical properties of fragments (Rule of Three, Ro3) but also the importance and implications of incorporating shape and, in particular, 3D characteristics into fragments. Herein, we describe the design and synthesis of pyrrolidine-based fragments with good fragment-like (Ro3) physicochemical properties that effectively sample three-dimensional molecular space.

Computed Properties of C6H5NO. About 3-Pyridinecarboxaldehyde, If you have any questions, you can contact Garner, P; Cox, PB; Rathnayake, U; Holloran, N; Erdman, P or concate me.

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

COA of Formula: C6H5NO. In 2019.0 J BRAZIL CHEM SOC published article about ONE-POT SYNTHESIS; 3-COMPONENT COUPLING REACTION; MULTICOMPONENT SYNTHESIS; COPPER; ALKYNE; 2-AMINOPYRIDINES; CYCLOADDITION; CYCLIZATION; PALLADIUM; ALDEHYDES in [de Salles, Helena D.; Benvenutti, Edilson, V; Schneider, Paulo H.] Univ Fed Rio Grande do Sul, Inst Quim, Av Bento Goncalves 9500, BR-91501970 Porto Alegre, RS, Brazil; [da Silva, Tiago L.] Univ Fed Rio de Janeiro, Inst Quim, Av Athos da Silveira Ramos 149,Bloco A, BR-21941909 Rio de Janeiro, RJ, Brazil; [Radatz, Catia S.] Univ Fed Pelotas UFPeI, CCQFA, BR-96010900 Pelotas, RS, Brazil; [Affeldt, Ricardo F.] Univ Fed Santa Catarina, Ctr Ciencias Fis & Matemat, Dept Quim, BR-88040970 Florianopolis, SC, Brazil in 2019.0, Cited 60.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1.

In this work, we report the preparation of a copper-silica material (Cu/SiO2) by a sol-gel methodology and its characterization concerning composition and textural properties. The Cu/SiO2 material was successfully applied as a Lewis acid heterogeneous catalyst for the A(3)-coupling from 2-aminopyridine, aldehydes and alkynes to imidazo[1,2-a]pyridines (45-82%). which are relevant pharmacological scaffolds. The synthesis shows a number of advantages, such as easy separation from the reaction media and the minimal formation of metal aqueous wastes. Investigation of the mechanism supports the involvement of the formation of reaction intermediates inside the pores of the mesoporous material prior to 5-exo-dig cyclization.

COA of Formula: C6H5NO. About 3-Pyridinecarboxaldehyde, If you have any questions, you can contact de Salles, HD; da Silva, TL; Radatz, CS; Affeldt, RF; Benvenutti, EV; Schneider, PH or concate me.

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

In 2019 CHEM-EUR J published article about CATALYZED REDUCTIVE UMPOLUNG; TITANIUM-INDUCED SYNTHESES; EFFICIENT SYNTHESIS; FACILE SYNTHESIS; BOND FORMATION; LEWIS-ACID; ALDEHYDES; PYRROLES; TOOL; AMINOPYRROLES in [Leijendekker, Leonardus H.; Weweler, Jens; Leuther, Tobias M.; Streuff, Jan] Albert Ludwigs Univ Freiburg, Inst Organ Chem, Albertstr 21, D-79104 Freiburg, Germany; [Kratz, Daniel] Albert Ludwigs Univ Freiburg, Inst Anorgan & Analyt Chem, Albertstr 21, D-79104 Freiburg, Germany in 2019, Cited 121. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1. Quality Control of 3-Pyridinecarboxaldehyde

The exceptionally mild conditions of a titanium(III)-catalyzed cyclization reaction paired with a convenient acid/base extraction have enabled the straightforward synthesis, isolation, and direct N-functionalization of amino heterocycles such as 3-aminoindoles and -pyrroles. The unprotected heterocycles are ideal building blocks for the installation of aminated indoles and pyrroles into target molecules, but their sensitivity has previously impeded their synthesis by modern catalytic methods. This full paper presents the development and extended scope of the new cyclization methodology. The transformation of the products into fused bis-indoles is also demonstrated along with the discovery of an unusual palladium-catalyzed reductive biphenyl coupling reaction. The titanium(III)-catalyzed cyclization has also been applied to the synthesis of substituted 3-iminoindolines, which are of potential interest for applications in natural product synthesis and exhibit tunable blue-to-green fluorescence properties.

Quality Control of 3-Pyridinecarboxaldehyde. About 3-Pyridinecarboxaldehyde, If you have any questions, you can contact Leijendekker, LH; Weweler, J; Leuther, TM; Kratz, D; Streuff, J or concate me.

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