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An article Selective C3-alkenylation of oxindole with aldehydes using heterogeneous CeO2 catalyst WOS:000531430200008 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. Category: indolines-derivatives

An article Selective C3-alkenylation of oxindole with aldehydes using heterogeneous CeO2 catalyst WOS:000531430200008 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. Category: indolines-derivatives

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.

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

Properties and Exciting Facts About Indolin-2-one

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. Name: Indolin-2-one. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3.

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. Name: 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.

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

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Application In Synthesis 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

Application In Synthesis 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.

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

Final Thoughts on Chemistry for Indolin-2-one

I found the field of Pharmacology & Pharmacy very interesting. Saw the article Novel Human Aminopeptidase N Inhibitors: Discovery and Optimization of Subsite Binding Interactions published in 2019. Quality Control of Indolin-2-one, Reprint Addresses Scammells, PJ (corresponding author), Monash Univ, Monash Inst Pharmaceut Sci, Med Chem, Parkville Campus, Parkville, Vic 3052, Australia.; McGowan, S (corresponding author), Monash Univ, Infect & Immun Program, Biomed Discovery Inst, Clayton Campus, Clayton, Vic 3800, Australia.; McGowan, S (corresponding author), Monash Univ, Dept Microbiol, Clayton Campus, Clayton, Vic 3800, Australia.. The CAS is 59-48-3. Through research, I have a further understanding and discovery of Indolin-2-one

I found the field of Pharmacology & Pharmacy very interesting. Saw the article Novel Human Aminopeptidase N Inhibitors: Discovery and Optimization of Subsite Binding Interactions published in 2019. Quality Control of Indolin-2-one, Reprint Addresses Scammells, PJ (corresponding author), Monash Univ, Monash Inst Pharmaceut Sci, Med Chem, Parkville Campus, Parkville, Vic 3052, Australia.; McGowan, S (corresponding author), Monash Univ, Infect & Immun Program, Biomed Discovery Inst, Clayton Campus, Clayton, Vic 3800, Australia.; McGowan, S (corresponding author), Monash Univ, Dept Microbiol, Clayton Campus, Clayton, Vic 3800, Australia.. The CAS is 59-48-3. Through research, I have a further understanding and discovery of Indolin-2-one

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

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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. SDS of cas: 59-48-3

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. SDS of cas: 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

What kind of challenge would you like to see in a future of compound:Indolin-2-one

Sydow, D; Schmiel, P; Mortier, J; Volkamer, A 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 published KinFragLib: Exploring the Kinase Inhibitor Space Using Subpocket-Focused Fragmentation and Recombination in 2020, Cited 49. HPLC of Formula: C8H7NO. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3.

Sydow, D; Schmiel, P; Mortier, J; Volkamer, A 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 published KinFragLib: Exploring the Kinase Inhibitor Space Using Subpocket-Focused Fragmentation and Recombination in 2020, Cited 49. HPLC of 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.

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.. HPLC of Formula: C8H7NO

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

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An article Direct Access to Alkylideneoxindoles via Axially Enantioselective Knoevenagel Condensation WOS:000467320000011 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. Computed Properties of C8H7NO. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3

An article Direct Access to Alkylideneoxindoles via Axially Enantioselective Knoevenagel Condensation WOS:000467320000011 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. Computed Properties of C8H7NO. 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.

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Reference:
Indoline – Wikipedia,
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Recommanded Product: 59-48-3. 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.

Recommanded Product: 59-48-3. 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.

Recommanded Product: 59-48-3. Welcome to talk about 59-48-3, If you have any questions, you can contact Liu, CY; Li, ZY; Weng, ZY; Fang, XY; Zhao, F; Tang, KH; Chen, JY; Ma, WB or send Email.

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

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Recently I am researching about TOBACCO-MOSAIC-VIRUS; LULICONAZOLE; BIOACTIVITY; MECHANISMS; DESIGN, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [21867002]. Published in ACADEMIC PRESS INC ELSEVIER SCIENCE in SAN DIEGO ,Authors: Wei, CL; Zhao, L; Sun, ZR; Hu, DY; Song, BA. The CAS is 59-48-3. Through research, I have a further understanding and discovery of Indolin-2-one. Application In Synthesis of Indolin-2-one

Recently I am researching about TOBACCO-MOSAIC-VIRUS; LULICONAZOLE; BIOACTIVITY; MECHANISMS; DESIGN, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [21867002]. Published in ACADEMIC PRESS INC ELSEVIER SCIENCE in SAN DIEGO ,Authors: Wei, CL; Zhao, L; Sun, ZR; Hu, DY; Song, BA. The CAS is 59-48-3. Through research, I have a further understanding and discovery of Indolin-2-one. Application In Synthesis of Indolin-2-one

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.

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

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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. Recommanded Product: Indolin-2-one. The Name is Indolin-2-one. Through research, I have a further understanding and discovery 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. Recommanded Product: 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.

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