Tag: M.W=100-150

An article Phosphine-Catalyzed Remote 1,7-Addition for Synthesis of Diene Carboxylates WOS:000526394500004 published article about GAMMA-SUBSTITUTED ALLENOATES; UMPOLUNG ADDITION-REACTION; CROSS-COUPLING REACTION; MORITA-BAYLIS-HILLMAN; DIASTEREOSELECTIVE SYNTHESIS; SEQUENTIAL ANNULATION; BOND FORMATION; 3+2 CYCLOADDITION; MICHAEL ADDITION; DOMINO REACTION in [Feng, Jiaxu; Huang, You] Nankai Univ, Coll Chem, State Key Lab, Tianjin 300071, Peoples R China; [Feng, Jiaxu; Huang, You] Nankai Univ, Coll Chem, Inst Elementoorgan Chem, Tianjin 300071, Peoples R China in 2020.0, Cited 105.0. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3. Product Details of 59-48-3

A phosphine-catalyzed remote 1,7-addition of vinyl allenoates has been developed, providing a series of 1,3-dienes derivatives in high yields (up to 99%) and with good chemo-, regio-, and stereoselectivity. This reaction demonstrated that the introduction of vinyl in allenoates effectively extended reaction types of phosphine-catalyzed nucleophilic addition of allenoates, leading to concise synthesis of diene carboxylates. Notably, the enantioselective variant of this 1,7-addition can also be performed by chiral phosphine catalyst.

Bye, fridends, I hope you can learn more about C8H7NO, If you have any questions, you can browse other blog as well. See you lster.. Product Details of 59-48-3

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

Name: Indolin-2-one. Lee, J; Vinh, NB; Drinkwater, N; Yang, W; Sivaraman, KK; Schembri, LS; Gazdik, M; Grin, PM; Butler, GS; Overall, CM; Charman, SA; McGowan, S; Scammells, PJ 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 published Novel Human Aminopeptidase N Inhibitors: Discovery and Optimization of Subsite Binding Interactions in 2019, Cited 80. 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.

Name: Indolin-2-one. Welcome to talk about 59-48-3, If you have any questions, you can contact Lee, J; Vinh, NB; Drinkwater, N; Yang, W; Sivaraman, KK; Schembri, LS; Gazdik, M; Grin, PM; Butler, GS; Overall, CM; Charman, SA; McGowan, S; Scammells, PJ or send Email.

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

Formula: C8H7NO. Wei, CL; Zhao, L; Sun, ZR; Hu, DY; Song, BA 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 published Discovery of novel indole derivatives containing dithioacetal as potential antiviral agents for plants in 2020.0, Cited 33.0. 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.

Formula: C8H7NO. 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

HPLC of Formula: C8H7NO. Recently I am researching about SPHINGOLIPID METABOLISM; CELLULAR-RESPONSES; GAUCHER-DISEASE; SPHINGOSINE-1-PHOSPHATE; POTENT; GLUCOSYLSPHINGOSINE; GLUCOSYLCERAMIDE; ACCUMULATION; PURIFICATION; DEFICIENCY, Saw an article supported by the . Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Di Martino, S; Tardia, P; Cilibrasi, V; Caputo, S; Mazzonna, M; Russo, D; Penna, I; Realini, N; Margaroli, N; Migliore, M; Pizzirani, D; Ottonello, G; Bertozzi, SM; Armirotti, A; Nguyen, D; Sun, Y; Bongarzone, ER; Lansbury, P; Liu, M; Skerlj, R; Scarpelli, R. The CAS is 59-48-3. Through research, I have a further understanding and discovery of Indolin-2-one

Sphingolipids (SphLs) are a diverse class of molecules that are regulated by a complex network of enzymatic pathways. A disturbance in these pathways leads to lipid accumulation and initiation of several SphL-related disorders. Acid ceramidase is one of the key enzymes that regulate the metabolism of ceramides and glycosphingolipids, which are important members of the SphL family. Herein, we describe the lead optimization studies of benzoxazolone carboxamides resulting in piperidine 22m, where we demonstrated target engagement in two animal models of neuropathic lysosomal storage diseases (LSDs), Gaucher’s and Krabbe’s diseases. After daily intraperitoneal administration at 90 mg kg(-1), 22m significantly reduced the brain levels of the toxic lipids glucosylsphingosine (GluSph) in 4L;C* mice and galactosylsphingosine (GalSph) in Twitcher mice. We believe that 22m is a lead molecule that can be further developed for the correction of severe neurological LSDs where GluSph or GalSph play a significant role in disease pathogenesis.

HPLC of Formula: C8H7NO. Welcome to talk about 59-48-3, If you have any questions, you can contact Di Martino, S; Tardia, P; Cilibrasi, V; Caputo, S; Mazzonna, M; Russo, D; Penna, I; Realini, N; Margaroli, N; Migliore, M; Pizzirani, D; Ottonello, G; Bertozzi, SM; Armirotti, A; Nguyen, D; Sun, Y; Bongarzone, ER; Lansbury, P; Liu, M; Skerlj, R; Scarpelli, R or send Email.

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

Hendrikse, ER; Liew, LP; Bower, RL; Bonnet, M; Jamaluddin, MA; Prodan, N; Richards, KD; Walker, CS; Pairaudeau, G; Smith, DM; Rujan, RM; Sudra, R; Reynolds, CA; Booe, JM; Pioszak, AA; Flanagan, JU; Hay, MP; Hay, DL in [Hendrikse, Erica R.; Bower, Rebekah L.; Jamaluddin, Muhammad A.; Prodan, Nicole; Richards, Keith D.; Walker, Christopher S.; Hay, Debbie L.] Univ Auckland, Sch Biol Sci, Auckland 1010, New Zealand; [Hendrikse, Erica R.; Bower, Rebekah L.; Jamaluddin, Muhammad A.; Walker, Christopher S.; Flanagan, Jack U.; Hay, Michael P.; Hay, Debbie L.] Univ Auckland, Maurice Wilkins Ctr Mol Biodiscovery, Auckland 1010, New Zealand; [Liew, Lydia P.; Bonnet, Muriel; Flanagan, Jack U.; Hay, Michael P.] Univ Auckland, Auckland Canc Soc Res Ctr, Auckland 1023, New Zealand; [Pairaudeau, Garry] AstraZeneca, Hit Discovery, Discovery Sci, R&D, Cambridge CB2 0SL, England; [Smith, David M.] AstraZeneca, Emerging Innovat, R&D, Discovery Sci, Cambridge CB2 0SL, England; [Rujan, Roxana-Maria; Sudra, Risha; Reynolds, Christopher A.] Univ Essex, Sch Life Sci, Colchester CO4 3SQ, Essex, England; [Booe, Jason M.; Pioszak, Augen A.] Univ Oklahoma, Dept Biochem & Mol Biol, Hlth Sci Ctr, Oklahoma City, OK 73104 USA published Identification of Small-Molecule Positive Modulators of Calcitonin-like Receptor-Based Receptors in 2020, Cited 67. Name: Indolin-2-one. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3.

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.

Name: Indolin-2-one. Welcome to talk about 59-48-3, If you have any questions, you can contact Hendrikse, ER; Liew, LP; Bower, RL; Bonnet, M; Jamaluddin, MA; Prodan, N; Richards, KD; Walker, CS; Pairaudeau, G; Smith, DM; Rujan, RM; Sudra, R; Reynolds, CA; Booe, JM; Pioszak, AA; Flanagan, JU; Hay, MP; Hay, DL or send Email.

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

An article Lead Optimization of Benzoxazolone Carboxamides as Orally Bioavailable and CNS Penetrant Acid Ceramidase Inhibitors WOS:000526405300016 published article about SPHINGOLIPID METABOLISM; CELLULAR-RESPONSES; GAUCHER-DISEASE; SPHINGOSINE-1-PHOSPHATE; POTENT; GLUCOSYLSPHINGOSINE; GLUCOSYLCERAMIDE; ACCUMULATION; PURIFICATION; DEFICIENCY in [Lansbury, Peter; Liu, Min; Skerlj, Renato] Lysosomal Therapeut Inc, Cambridge, MA 02139 USA; [Di Martino, Simona; Tardia, Piero; Cilibrasi, Vincenzo; Caputo, Samantha; Mazzonna, Marco; Realini, Natalia; Margaroli, Natasha; Migliore, Marco; Pizzirani, Daniela; Scarpelli, Rita] Fdn Ist Italiano Tecnol, Drug Discovery & Dev D3 Validat, I-16163 Genoa, Italy; [Russo, Debora; Penna, Ilaria] Fdn Ist Italiano Tecnol, D3 Pharma Chem, I-16163 Genoa, Italy; [Ottonello, Giuliana; Bertozzi, Sine Mandrup; Armirotti, Andrea] Fdn Ist Italiano Tecnol, Analyt Chem Lab, I-16163 Genoa, Italy; [Duc Nguyen; Bongarzone, Ernesto R.] Univ Illinois, Coll Med, Dept Anat & Cell Biol, Myelin Regenerat Grp, Chicago, IL 60612 USA; [Sun, Ying] Univ Cincinnati, Coll Med, Cincinnati Childrens Hosp Med Ctr, Dept Pediat,Div Human Genet, Cincinnati, OH 45229 USA in 2020.0, Cited 58.0. Name: Indolin-2-one. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3

Sphingolipids (SphLs) are a diverse class of molecules that are regulated by a complex network of enzymatic pathways. A disturbance in these pathways leads to lipid accumulation and initiation of several SphL-related disorders. Acid ceramidase is one of the key enzymes that regulate the metabolism of ceramides and glycosphingolipids, which are important members of the SphL family. Herein, we describe the lead optimization studies of benzoxazolone carboxamides resulting in piperidine 22m, where we demonstrated target engagement in two animal models of neuropathic lysosomal storage diseases (LSDs), Gaucher’s and Krabbe’s diseases. After daily intraperitoneal administration at 90 mg kg(-1), 22m significantly reduced the brain levels of the toxic lipids glucosylsphingosine (GluSph) in 4L;C* mice and galactosylsphingosine (GalSph) in Twitcher mice. We believe that 22m is a lead molecule that can be further developed for the correction of severe neurological LSDs where GluSph or GalSph play a significant role in disease pathogenesis.

Bye, fridends, I hope you can learn more about C8H7NO, If you have any questions, you can browse other blog as well. See you lster.. Name: Indolin-2-one

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

In 2020.0 J FLUORESC published article about SENSOR; FE3+; PROBE; CR3+; GLYCOCLUSTER; CATIONS; AL3+ in [Sadak, Ali Enis; Karakus, Erman] TUBITAK UME Sci & Technol Res Council Turkey, Organ Chem Lab, Natl Metrol Inst, Chem Grp, TR-41470 Kocaeli, Turkey in 2020.0, Cited 36.0. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3. Formula: C8H7NO

We investigated the ability of a novel triazatruxene-rhodamine-based (TAT-ROD) chemosensor to detect the trivalent metal ions aluminium (Al3+), iron (Fe3+) and chromium (Cr3+). Operating via the through-bond energy transfer (TBET) pathway, the chemosensor exhibited low detection limits of 23.0, 25.0 and 170.0 nM for Al3+, Fe3+ and Cr3+, respectively, along with high sensitivity and selectivity during a brief period (<15 s). The binding ratio of the chemosensor and trivalent metal ions achieved by Job's method was 3:1, and when we added ethylenediaminetetraacetic acid (EDTA), the sensing process reversed. Altogether, our TAT-ROD chemosensor marks the first triazatruxene-based colorimetric and fluorometric metal ion sensor reported in the literature. Formula: C8H7NO. Welcome to talk about 59-48-3, If you have any questions, you can contact Sadak, AE; Karakus, E or send Email.

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

In 2020 J CHEM INF MODEL published article about MEDICINAL CHEMISTRY; PROTEIN-KINASES; DRUG DISCOVERY; DESIGN; POWERFUL; DATABASE; MUTANT; KLIFS in [Sydow, Dominique; Schmiel, Paula; Volkamer, Andrea] Charite, Inst Physiol, Silico Toxicol & Struct Bioinformat, D-10117 Berlin, Germany; [Mortier, Jeremie] Bayer AG, Digital Technol Computat Mol Design, D-13342 Berlin, Germany in 2020, Cited 49. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3. Formula: C8H7NO

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.

Formula: C8H7NO. Bye, fridends, I hope you can learn more about C8H7NO, If you have any questions, you can browse other blog as well. See you lster.

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

An article Triazatruxene-Rhodamine-Based Ratiometric Fluorescent Chemosensor for the Sensitive, Rapid Detection of Trivalent Metal Ions: Aluminium (III), Iron (III) and Chromium (III) WOS:000519286200024 published article about SENSOR; FE3+; PROBE; CR3+; GLYCOCLUSTER; CATIONS; AL3+ in [Sadak, Ali Enis; Karakus, Erman] TUBITAK UME Sci & Technol Res Council Turkey, Organ Chem Lab, Natl Metrol Inst, Chem Grp, TR-41470 Kocaeli, Turkey in 2020.0, Cited 36.0. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3. Formula: C8H7NO

We investigated the ability of a novel triazatruxene-rhodamine-based (TAT-ROD) chemosensor to detect the trivalent metal ions aluminium (Al3+), iron (Fe3+) and chromium (Cr3+). Operating via the through-bond energy transfer (TBET) pathway, the chemosensor exhibited low detection limits of 23.0, 25.0 and 170.0 nM for Al3+, Fe3+ and Cr3+, respectively, along with high sensitivity and selectivity during a brief period (<15 s). The binding ratio of the chemosensor and trivalent metal ions achieved by Job's method was 3:1, and when we added ethylenediaminetetraacetic acid (EDTA), the sensing process reversed. Altogether, our TAT-ROD chemosensor marks the first triazatruxene-based colorimetric and fluorometric metal ion sensor reported in the literature. Welcome to talk about 59-48-3, If you have any questions, you can contact Sadak, AE; Karakus, E or send Email.. Formula: C8H7NO

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

An article Macrocyclic Modalities Combining Peptide Epitopes and Natural Product Fragments WOS:000526392200048 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. Quality Control of Indolin-2-one

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.

Quality Control of Indolin-2-one. Welcome to talk about 59-48-3, If you have any questions, you can contact Gueret, SM; Thavam, S; Carbajo, RJ; Potowski, M; Larsson, N; Dahl, G; Dellsen, A; Grossmann, TN; Plowright, AT; Valeur, E; Lemurell, M; Waldmann, H or send Email.

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