Tag: M.W=100-150

Authors 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 AMER CHEMICAL SOC 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. Safety of Indolin-2-one. 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

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. Formula: C8H7NO

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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Indoline – Wikipedia,
,Indoline | C8H9N – PubChem

An article KinFragLib: Exploring the Kinase Inhibitor Space Using Subpocket-Focused Fragmentation and Recombination WOS:000608875100049 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. Formula: C8H7NO. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3

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.

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Indoline – Wikipedia,
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I found the field of Chemistry very interesting. Saw the article Models for Understanding Divergent Reactivity in Lewis Acid-Catalyzed Transformations of Carbonyls and Olefins published in 2020.0. Product Details of 59-48-3, Reprint Addresses Reid, JP (corresponding author), Univ Utah, Dept Chem, Salt Lake City, UT 84112 USA.; Schindler, CS (corresponding author), Univ Michigan, Willard Henry Dow Lab, Dept Chem, Ann Arbor, MI 48109 USA.. The CAS is 59-48-3. Through research, I have a further understanding and discovery of Indolin-2-one

Carbonyl-ene, Prins, and carbonyl-olefin metathesis reactions represent powerful strategies for carbon-carbon bond formation relying on Lewis acid catalysts. Although common Lewis acids are able to provide efficient activation, the reactions often proceed with low regio- or chemoselectivity, while high selectivity frequently requires the use of well-designed metal-ligand complexes. Here we demonstrate that simple Lewis acids including Me2AlCl, FeCl3, and SnCl4 can show remarkable selectivity in differentiating between distinct transformations of carbonyl and olefin functional groups, resulting in either carbonyl-ene or carbonyl-olefin metathesis products. Specifically, we report the development of predictive multivariate linear regression models that rely on kinetic and thermodynamic information obtained in DFT calculations to gain important insights into the complex potential energy surfaces (PES) of these competing reaction paths. The presented results further our understanding of Lewis acid reactivity and suggest that even simple Lewis acids have the potential to function as highly selective catalysts.

Product Details of 59-48-3. 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.

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Indoline – Wikipedia,
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Computed Properties of C8H7NO. In 2020.0 ANGEW CHEM INT EDIT published article about CROSS-COUPLING REACTIONS; FUNCTIONALIZATION; DERIVATIVES; OXINDOLES; ETHERS; BONDS; PHOTOSENSITIZERS; HYDROCARBONS; ACTIVATION; ANNULATION in [Hu, Ren-Ming; Han, Dong-Yang; Li, Ning; Huang, Jie; Feng, Yu; Xu, Da-Zhen] Nankai Univ, State Key Lab, Coll Chem, Natl Engn Res Ctr Pesticide Tianjin, Tianjin 300071, Peoples R China; [Hu, Ren-Ming; Han, Dong-Yang; Li, Ning; Huang, Jie; Feng, Yu; Xu, Da-Zhen] Nankai Univ, Inst Elementoorgan Chem, Coll Chem, Tianjin 300071, Peoples R China in 2020.0, Cited 61.0. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3.

Presented herein is the first direct alkylation and hydroxylation reaction between two different C(sp(3))-H bonds, indolin-2-ones and alkyl-substituted N-heteroarenes, through an oxidative cross-coupling reaction. The reaction is catalyzed by a simple iron salt under mild ligand-free and base-free conditions. The reaction is environmentally benign, employs air (molecular oxygen) as the terminal oxidant and oxygen source for the synthesis of O-containing compounds, and produces only water as the byproduct.

Computed Properties of 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

Product Details of 59-48-3. 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. 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.

Product Details of 59-48-3. 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

Quality Control of Indolin-2-one. 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.

Quality Control of Indolin-2-one. Welcome to talk about 59-48-3, If you have any questions, you can contact Vaidya, GN; Nagpure, M; Kumar, D or send Email.

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

HPLC of Formula: C8H7NO. Recently I am researching about CROSS-COUPLING REACTIONS; FUNCTIONALIZATION; DERIVATIVES; OXINDOLES; ETHERS; BONDS; PHOTOSENSITIZERS; HYDROCARBONS; ACTIVATION; ANNULATION, Saw an article supported by the National Natural Science Foundation of China (NSFC)National Natural Science Foundation of China (NSFC) [21302101]; National Training Programs of Innovation and Entrepreneurship for Undergraduates [201810055095, 201910055087]; Chemistry College of Nankai University. Published in WILEY-V C H VERLAG GMBH in WEINHEIM ,Authors: Hu, RM; Han, DY; Li, N; Huang, J; Feng, Y; Xu, DZ. The CAS is 59-48-3. Through research, I have a further understanding and discovery of Indolin-2-one

Presented herein is the first direct alkylation and hydroxylation reaction between two different C(sp(3))-H bonds, indolin-2-ones and alkyl-substituted N-heteroarenes, through an oxidative cross-coupling reaction. The reaction is catalyzed by a simple iron salt under mild ligand-free and base-free conditions. The reaction is environmentally benign, employs air (molecular oxygen) as the terminal oxidant and oxygen source for the synthesis of O-containing compounds, and produces only water as the byproduct.

Welcome to talk about 59-48-3, If you have any questions, you can contact Hu, RM; Han, DY; Li, N; Huang, J; Feng, Y; Xu, DZ or send Email.. HPLC of Formula: C8H7NO

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

An article Desymmetrization of Prochiral Cyclopentenes Enabled by Enantioselective Palladium-Catalyzed Oxidative Heck Reaction WOS:000506088700066 published article about ASYMMETRIC HECK; MATSUDA ARYLATIONS; ACYCLIC ALKENES; LIGANDS; OLEFINS; COMPLEXES in [Chen, Guihua; Cao, Jian; Wang, Qian; Zhu, Jieping] Ecole Polytech Fed Lausanne, Lab Synth & Nat Prod, Inst Chem Sci & Engn, SB,ISIC,LSPN, BCH 5304, CH-1015 Lausanne, Switzerland; [Chen, Guihua] Southwest Univ, Sch Chem & Chem Engn, Key Lab Appl Chem Chongqing Municipal, Chongqing 400715, Peoples R China; [Cao, Jian] Hangzhou Normal Univ, Key Lab Organosilicon Chem & Mat Technol, Minist Educ, Hangzhou 311121, Peoples R China in 2020.0, Cited 46.0. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3. Computed Properties of C8H7NO

In the presence of a catalytic amount of Pd(TFA)(2) and a chiral Pyox ligand under oxygen atmosphere, oxidative Heck reaction between arylboronic acids and 4-substituted or 4,4-disubstituted cyclopent-1-enes afforded the chiral arylated products with concurrent creation of two stereocenters in good yields with excellent diastereo- and enantioselectivities.

Computed Properties of 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.

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Indoline – Wikipedia,
,Indoline | C8H9N – PubChem

HPLC of Formula: C8H7NO. In 2020.0 CHINESE J CATAL published article about ENANTIOSELECTIVE CONSTRUCTION; AMIDES; NITRILES; ALCOHOLS; ESTERS; ACTIVATION; HYDRATION; VERSATILE; ISATIN in [Rashed, Md Nurnobi; Touchy, Abeda Sultana; Jeon, Jaewan; Siddiki, S. M. A. Hakim; Toyao, Takashi; Shimizu, Ken-ichi] Hokkaido Univ, Inst Catalysis, N-21,W-10, Sapporo, Hokkaido 0010021, Japan; [Chaudhari, Chandan] Nagoya Univ, Grad Sch Engn, Dept Chem Syst Engn, Nagoya, Aichi 4648603, Japan; [Toyao, Takashi; Shimizu, Ken-ichi] Kyoto Univ, Elements Strategy Initiat Catalysts & Batteries, Kyoto 6158520, Japan in 2020.0, Cited 39.0. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3.

We report herein that a commercially available CeO2 is an active and reusable catalyst for the C3-selective alkenylation of oxindole with aldehydes under solvent-free conditions. This. catalytic method is generally applicable to different aromatic and aliphatic aldehydes, giving 3-alkyledene-oxindoles in high yields (87%-99%) and high stereoselectivities (79%-93% to E-isomers). This is the first example of the catalytic synthesis of 3-alkenyl-oxindoles from oxindole and various aliphatic aldehydes. The Lewis acid-base interaction between Lewis acid sites on CeO2 and benzaldehyde was studied by in situ IR. The structure-activity relationship study using CeO2 catalysts with different sizes suggests that defect-free CeO2 surface is the active site for this reaction. (C) 2020, Dalian Institute of Chemical Physics, Chinese Academy of Sciences. Published by Elsevier B.V. All rights reserved.

Welcome to talk about 59-48-3, If you have any questions, you can contact Rashed, MN; Touchy, AS; Chaudhari, C; Jeon, J; Siddiki, SMAH; Toyao, T; Shimizu, K or send Email.. HPLC of Formula: C8H7NO

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