Month: November 2021

An article One-Pot Regiodirected Annulations for the Rapid Synthesis of pi-Extended Oligomers WOS:000526894000079 published article about DIRECT ARYLATION; BITHIOPHENE COPOLYMERS; CONJUGATED POLYMER; HIGH-PERFORMANCE; MATERIALS DESIGN; CONVERSION in [Nitti, Andrea; Osw, Peshawa; Calcagno, Giuseppe; Pasini, Dario] Univ Pavia, Dept Chem, I-27100 Pavia, Italy; [Nitti, Andrea; Pasini, Dario] Univ Pavia, INSTM Res Unit, I-27100 Pavia, Italy; [Osw, Peshawa] Salahaddin Univ, Coll Sci, Dept Chem, Erbil 44001, Kurdistan, Iraq; [Botta, Chiara] CNR, Ist Studio Macromol ISMAC, I-20133 Milan, Italy; [Etkind, Samuel I.; Swager, Timothy M.] MIT, Dept Chem, Cambridge, MA 02139 USA; [Bianchi, Gabriele; Po, Riccardo] Ist Donegani SpA, Res Ctr Renewable Energies & Environm, I-28100 Novara, Italy in 2020.0, Cited 43.0. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3. Computed Properties of C8H7NO

We demonstrate the broad applicability of the annulation protocol combining, in one pot, a direct arylation and cross aldol condensation for the straightforward synthesis at gram-scale of pi-extended thiophene-based scaffolds. The regiospecific direct arylation drives the subsequent cross-aldol condensation proceed under the same basic conditions, and the overall protocol has broad applicability in the synthesis of extended aromatics wherein the thiophene ring is annulated with furans, pyridines, indoles, benzothiophenes, and benzofurans. These scaffolds can be further elaborated into pi-extended, highly fluorescent oligomers with a central deficient benzothiadiazole unit with up to nine aromatic rings through coupling reactions.

Welcome to talk about 59-48-3, If you have any questions, you can contact Nitti, A; Osw, P; Calcagno, G; Botta, C; Etkind, SI; Bianchi, G; Po, R; Swager, TM; Pasini, D or send Email.. Computed Properties of C8H7NO

Reference:
Indoline – Wikipedia,
,Indoline | C8H9N – PubChem

Name: Indolin-2-one. In 2020.0 J AM CHEM SOC published article about AGOUTI-RELATED PROTEIN; STRUCTURAL BASIS; CYCLIC-PEPTIDES; DISCOVERY; DESIGN; POTENT; TARGETS; SPSB2; RECOGNITION; CYCLIZATION in [Gueret, Stephanie M.] Max Planck Inst Mol Physiol, AstraZeneca, Dept Chem Biol, Max Planck Inst Satellite Unit, D-44227 Dortmund, Germany; [Gueret, Stephanie M.; Plowright, Alleyn T.; Valeur, Eric; Lemurell, Malin] AstraZeneca, Med Chem Res & Early Dev Cardiovasc Renal & Metab, BioPharmaceut R&D, S-43150 Gothenburg, Sweden; [Thavam, Sasikala; Potowski, Marco; Waldmann, Herbert] Max Planck Inst Mol Physiol, Dept Chem Biol, D-44227 Dortmund, Germany; [Carbajo, Rodrigo J.] AstraZeneca, Chem Oncol R&D, Cambridge CB2 0SL, England; [Potowski, Marco; Waldmann, Herbert] TU Dortmund Univ, Fac Chem & Chem Biol, D-44227 Dortmund, Germany; [Larsson, Niklas] AstraZeneca, Discovery Biol, BioPharmaceut R&D, Discovery Sci, S-43150 Gothenburg, Sweden; [Dahl, Goran] AstraZeneca, Struct Biophys & Fragment Based Lead Generat, Discovery Sci, BioPharmaceut R&D, S-43150 Gothenburg, Sweden; [Dellsen, Anita] AstraZeneca, BioPharmaceut R&D, Discovery Sci, Mechanist Biol & Profiling, S-43150 Gothenburg, Sweden; [Grossmann, Tom N.] Vrije Univ Amsterdam, Dept Chem & Pharmaceut Sci, NL-1081 HV Amsterdam, Netherlands in 2020.0, Cited 69.0. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3.

Hot loop protein segments have variable structure and conformation and contribute crucially to protein-protein interactions. We describe a new hot loop mimicking modality, termed PepNats, in which natural product (NP)-inspired structures are incorporated as conformation-determining and-restricting structural elements into macrocyclic hot loop-derived peptides. Macrocyclic PepNats representing hot loops of inducible nitric oxide synthase (iNOS) and human agouti-related protein (AGRP) were synthesized on solid support employing macro-cyclization by imine formation and subsequent stereoselective 1,3-dipolar cycloaddition as key steps. PepNats derived from the iNOS DINNN hot loop and the AGRP RFF hot spot sequence yielded novel and potent ligands of the SPRY domain-containing SOCS box protein 2 (SPSB2) that binds to iNOS, and selective ligands for AGRP-binding melanocortin (MC) receptors. NP-inspired fragment absolute configuration determines the conformation of the peptide part responsible for binding. These results demonstrate that combination of NP-inspired scaffolds with peptidic epitopes enables identification of novel hot loop mimics with conformationally constrained and biologically relevant structure.

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Reference:
Indoline – Wikipedia,
,Indoline | C8H9N – PubChem

Category: indolines-derivatives. Recently I am researching about MEDICINAL CHEMISTRY; PROTEIN-KINASES; DRUG DISCOVERY; DESIGN; POWERFUL; DATABASE; MUTANT; KLIFS, Saw an article supported by the Deutsche ForschungsgemeinschaftGerman Research Foundation (DFG) [VO 2353/1-1]; Bundesministerium fur Bildung und Forschung [031A262C]. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Sydow, D; Schmiel, P; Mortier, J; Volkamer, A. The CAS is 59-48-3. Through research, I have a further understanding and discovery of Indolin-2-one

Protein kinases play a crucial role in many cell signaling processes, making them one of the most important families of drug targets. In this context, fragment-based drug design strategies have been successfully applied to develop novel kinase inhibitors. These strategies usually follow a knowledge-driven approach to optimize a focused set of fragments to a potent kinase inhibitor. Alternatively, KinFragLib explores and extends the chemical space of kinase inhibitors using data-driven fragmentation and recombination. The method builds on available structural kinome data from the KLIFS database for over 2500 kinase DFG-in structures cocrystallized with noncovalent kinase ligands. The computational fragmentation method splits the ligands into fragments with respect to their 3D proximity to six predefined functionally relevant subpocket centers. The resulting fragment library consists of six subpocket pools with over 7000 fragments, available at https://github.com/volkamerlab/KinFragLib. KinFragLib offers two main applications: on the one hand, in-depth analyses of the chemical space of known kinase inhibitors, subpocket characteristics, and connections, and on the other hand, subpocket-informed recombination of fragments to generate potential novel inhibitors. The latter showed that recombining only a subset of 624 representative fragments generated 6.7 million molecules. This combinatorial library contains, besides some known kinase inhibitors, more than 99% novel chemical matter compared to ChEMBL and 63% molecules compliant with Lipinski’s rule of five.

Welcome to talk about 59-48-3, If you have any questions, you can contact Sydow, D; Schmiel, P; Mortier, J; Volkamer, A or send Email.. Category: indolines-derivatives

Reference:
Indoline – Wikipedia,
,Indoline | C8H9N – PubChem

Product Details of 59-48-3. Authors Vaidya, GN; Nagpure, M; Kumar, D in AMER CHEMICAL SOC published article about in [Vaidya, Gargi Nikhil; Nagpure, Mithilesh; Kumar, Dinesh] Natl Inst Pharmaceut Educ & Res NIPER, Dept Med Chem, Gandhinagar 382355, Gujarat, India in 2021, Cited 72. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3

A borrowing carbonate-enabled allylic cross-amination reactions employing allylic alcohol were discovered via merging acyl/allyl C-O bonds activation under nickel catalysis. The key component of this protocol is the ability of nickel [Ni(II)-Ni(0)] to execute a relay process via the nucleophilic trapping of the generated acyl Ni complex, resulting from the acyl C-O bond cleavage of dialkyl carbonates, followed by selective allylic C-O bond activations (allylic C-O vs alkyl C-O vs acyl C-O) to yield pi-allyINi-complexes. The finding truly represents Ni-catalyzed green allylic amination reactions under additive(s)-free conditions with excellent chemo- (N vs O), regio- (linear vs branched), and stereoselectivity (E vs Z) with a wide range of fundamentally challenging N-heterocycles and allylic alcohols. The reaction is scalable, does not require harmful reaction media and a globe box, and is successfully applied to the scale-up synthesis of pharmaceuticals (cinnarizine, flunarizine, and naftifine) with promising yields.

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Reference:
Indoline – Wikipedia,
,Indoline | C8H9N – PubChem

In 2020.0 CHEM COMMUN published article about PHOTOREDOX CATALYSIS; MERGING PHOTOREDOX; ARYLATION; PHOSPHONATION; ALLYLAMINE; ROUTE; GREEN; ACIDS in [Gou, Xue-Ya; Zhang, Bo-Sheng; Wang, Xin-Gang; Shi, Wei-Yu; Liu, Hong-Chao; An, Yang; Zhang, Zhe; Liang, Yong-Min] Lanzhou Univ, State Key Lab Appl Organ Chem, Lanzhou 730000, Gansu, Peoples R China in 2020.0, Cited 47.0. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3. HPLC of Formula: C8H7NO

Visible-light-induced C-H phosphorylation of para-C-Ar-H and heteroarenes was realized using cost-effective RuCl3 as a catalyst. The reaction conditions are green and environmentally friendly, using water as a solvent at room temperature and without ligands. A broad range of highly functional organophosphorus compounds were obtained via a cross-dehydrogenation-coupling (CDC) reaction. In addition, we also proved that RuCl3 is a photocatalyst via its absorption spectrum and on/off light experiments.

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Reference:
Indoline – Wikipedia,
,Indoline | C8H9N – PubChem

Authors Crotti, S; Di Iorio, N; Artusi, C; Mazzanti, A; Righi, P; Bencivenni, G in AMER CHEMICAL SOC published article about ASYMMETRIC-SYNTHESIS; ALPHA-BENZOYLOXYLATION; KINETIC RESOLUTION; CENTRAL CHIRALITY; BIARYLS; ISOMERIZATION; ATROPISOMERS; OLEFINATION; ALLENOATES; ALLENES in [Crotti, Simone; Di Iorio, Nicola; Artusi, Chiara; Mazzanti, Andrea; Righi, Paolo; Bencivenni, Giorgio] Univ Bologna, Dept Ind Chem Toso Montanari, Viale Risorgimento 4, I-40136 Bologna, Italy in 2019, Cited 65. Quality Control of Indolin-2-one. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3

The organocatalytic axially enantioselective Knoevenagel condensation between prochiral cyclohexanones and oxindoles is presented. The reaction, promoted by a primary amine, proceeded smoothly and furnished unprecedented examples of novel cyclohexylidene oxindoles displaying axial chirality.

Welcome to talk about 59-48-3, If you have any questions, you can contact Crotti, S; Di Iorio, N; Artusi, C; Mazzanti, A; Righi, P; Bencivenni, G or send Email.. Quality Control of Indolin-2-one

Reference:
Indoline – Wikipedia,
,Indoline | C8H9N – PubChem

I found the field of Pharmacology & Pharmacy very interesting. Saw the article Identification of Small-Molecule Positive Modulators of Calcitonin-like Receptor-Based Receptors published in 2020. Recommanded Product: 59-48-3, Reprint Addresses Hay, DL (corresponding author), Univ Auckland, Sch Biol Sci, Auckland 1010, New Zealand.; Flanagan, JU; Hay, MP; Hay, DL (corresponding author), Univ Auckland, Maurice Wilkins Ctr Mol Biodiscovery, Auckland 1010, New Zealand.; Flanagan, JU; Hay, MP (corresponding author), Univ Auckland, Auckland Canc Soc Res Ctr, Auckland 1023, New Zealand.. The CAS is 59-48-3. Through research, I have a further understanding and discovery of Indolin-2-one

Class B G protein-coupled receptors are highly therapeutically relevant but challenges remain in identifying suitable small-molecule drugs. The calcitonin-like receptor (CLR) in particular is linked to conditions such as migraine, cardiovascular disease, and inflammatory bowel disease. The CLR cannot act as a cell-surface receptor alone but rather must couple to one of three receptor activity-modifying proteins (RAMPs), forming heterodimeric receptors for the peptides adrenomedullin and calcitonin gene-related peptide. These peptides have extended binding sites across their receptors. This is one reason why there are few small-molecule ligands that can modulate these receptors. Here we describe small molecules that are able to positively modulate the signaling of the CLR with all three RAMPs but are not active at the related calcitonin receptor. These compounds were selected from a beta-arrestin recruitment screen, coupled with rounds of medicinal chemistry to improve their activity. Translational potential is shown as the compounds can positively modulate cAMP signaling in a vascular cell line model. Binding experiments do not support an extracellular domain binding site; however, molecular modeling reveals potential allosteric binding sites in multiple receptor regions. These are the first small-molecule positive modulators described for the CLR:RAMP complexes.

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Reference:
Indoline – Wikipedia,
,Indoline | C8H9N – PubChem

An article Discovery of novel indole derivatives containing dithioacetal as potential antiviral agents for plants WOS:000536197700011 published article about TOBACCO-MOSAIC-VIRUS; LULICONAZOLE; BIOACTIVITY; MECHANISMS; DESIGN in [Wei, Chunle; Zhao, Lei; Sun, Zhongrong; Hu, Deyu; Song, Baoan] Guizhou Univ, Minist Educ, Key Lab Green Pesticide & Agr Bioengn, State Key Lab Breeding Base Green Pesticide & Agr, Guiyang 550025, Peoples R China in 2020.0, Cited 33.0. Quality Control of Indolin-2-one. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3

Thirty unreported indole derivatives containing dithioacetal moiety were synthesized and evaluated for antiplant viral activity. Bioassay results displayed that some of the target compounds showed better activities against tobacco mosaic virus (TMV) than the commercial Ribavirin in vivo. In particular, anti-TMV curative, protective and inactivating activity of 4p were 55.1, 57.2, and 80.3%, respectively, and EC50 value for inactivating activity was 88.5 mu g/mL. The observation of transmission electron microscope showed that 4p may have a certain destructive effect on TMV particles. To further study, microscale thermophoresis analysis result also demonstrated that 4p powerfully interacted with TMV coat protein in vitro. Hence, this study provides a strong evidence suporting that indole derivatives might be applied as new antiviral agents.

Quality Control of Indolin-2-one. Welcome to talk about 59-48-3, If you have any questions, you can contact Wei, CL; Zhao, L; Sun, ZR; Hu, DY; Song, BA or send Email.

Reference:
Indoline – Wikipedia,
,Indoline | C8H9N – PubChem

An article Novel Human Aminopeptidase N Inhibitors: Discovery and Optimization of Subsite Binding Interactions WOS:000480500600023 published article about PLASMODIUM-FALCIPARUM M1; ACUTE NONLYMPHOCYTIC LEUKEMIA; MOLECULAR-DYNAMICS; CLINICAL-SIGNIFICANCE; EFFICIENT GENERATION; STRUCTURAL BASIS; AM1-BCC MODEL; CD13; BESTATIN; CANCER in [Lee, Jisook; Vinh, Natalie B.; Schembri, Luke S.; Gazdik, Michelle; Scammells, Peter J.] Monash Univ, Monash Inst Pharmaceut Sci, Med Chem, Parkville Campus, Parkville, Vic 3052, Australia; [Charman, Susan A.] Monash Univ, Monash Inst Pharmaceut Sci, Ctr Drug Candidate Optimisat, Parkville Campus, Parkville, Vic 3052, Australia; [Drinkwater, Nyssa; Yang, Wei; Sivaraman, Komagal Kannan; McGowan, Sheena] Monash Univ, Infect & Immun Program, Biomed Discovery Inst, Clayton Campus, Clayton, Vic 3800, Australia; [Drinkwater, Nyssa; Yang, Wei; Sivaraman, Komagal Kannan; McGowan, Sheena] Monash Univ, Dept Microbiol, Clayton Campus, Clayton, Vic 3800, Australia; [Grin, Peter M.; Butler, Georgina S.; Overall, Christopher M.] Univ British Columbia, Life Sci Inst, Dept Biochem & Mol Biol, Vancouver, BC V6T 1Z3, Canada; [Butler, Georgina S.; Overall, Christopher M.] Univ British Columbia, Life Sci Inst, Dept Oral Biol & Med Sci, Vancouver, BC V6T 1Z3, Canada; [Grin, Peter M.; Butler, Georgina S.; Overall, Christopher M.] Univ British Columbia, Life Sci Inst, Ctr Blood Res, Vancouver, BC V6T 1Z3, Canada in 2019, Cited 80. Computed Properties of C8H7NO. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3

Aminopeptidase N (APN/CD13) is a zinc-dependent M1 aminopeptidase that contributes to cancer progression by promoting angiogenesis, metastasis, and tumor invasion. We have previously identified hydroxamic acid-containing analogues that are potent inhibitors of the APN homologue from the malarial parasite Plasmodium falciparum M1 aminopeptidase (PfA-M1). Herein, we describe the rationale that underpins the repurposing of PfA-MI inhibitors as novel APN inhibitors. A series of novel hydroxamic acid analogues were developed using a structure-based design approach and evaluated their inhibition activities against APN. N-(2-(Hydroxyamino)-2-oxo-1-(3′,4′,5′-trifluoro-[1,1′-biphenyl]-4-yOethyl)-4(methylsulfonamido)benzamide (6ad) proved to be an extremely potent inhibitor of APN activity in vitro, selective against other zinc-dependent enzymes such as matrix metalloproteases, and possessed limited cytotoxicity against Ad293 cells and favorable physicochemical and metabolic stability properties. The combined results indicate that compound 6ad may be a useful lead for the development of anticancer agents.

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Reference:
Indoline – Wikipedia,
,Indoline | C8H9N – PubChem

Quality Control of Indolin-2-one. In 2020.0 ASIAN J ORG CHEM published article about S BOND FORMATION; CATALYZED C-S; SULFONYL CHLORIDES; SULFENYLATION; SULFUR; ENAMINONES; FUNCTIONALIZATION; THIOPHENOLS; SULFIDES; INDOLES in [Liu, Changying; Li, Zheyu; Weng, Zhengyun; Fang, Xinyue; Zhao, Fei; Tang, Kehui; Ma, Wenbo] Chengdu Univ, Sichuan Ind Inst Antibiot, Antibiot Res & Reevaluat Key Lab Sichuan Prov, Huaguan Rd 168, Chengdu 610052, Peoples R China; [Chen, Jianyang] Chongqing Univ Arts & Sci, Coll Chem & Environm Engn, 319 Honghe Ave, Chongqing, Peoples R China in 2020.0, Cited 60.0. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3.

A synthetic method for the preparation of unsymmetrical 2-arylthioacetamides though direct C(sp(3))-H thiolation of arylacetamides with readily available substituted thiols, sulfenylchlorides and disulfides have been developed. Our strategy features a green reaction medium with ample substrate scope, affording the mono-thiolated aryl acetic acid derivatives in moderate to good yields in the presence of weak bases without any transition-metal catalyst.

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Reference:
Indoline – Wikipedia,
,Indoline | C8H9N – PubChem