Month: October 2021

An article Transition-Metal-Free Selective C(sp(3))-H Thiolation of Arylacetamides with Substituted Benzenethiols, Aryl Sulfenylchlorides and Diaryl Disulfides WOS:000524357500028 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. Formula: C8H7NO

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.

Formula: C8H7NO. About Indolin-2-one, 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 concate me.

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. HPLC of Formula: 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.

HPLC of Formula: C8H7NO. About Indolin-2-one, 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 concate me.

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

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. 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.

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.

Quality Control of Indolin-2-one. About Indolin-2-one, 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 concate me.

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

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. Safety 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.

About Indolin-2-one, 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 concate me.. Safety of Indolin-2-one

Reference:
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. About Indolin-2-one, If you have any questions, you can contact Sydow, D; Schmiel, P; Mortier, J; Volkamer, A or concate me.

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

HPLC of Formula: C8H7NO. 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.

HPLC of Formula: C8H7NO. About Indolin-2-one, 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 concate me.

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

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. Recommanded Product: Indolin-2-one. 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.

Recommanded Product: Indolin-2-one. About Indolin-2-one, If you have any questions, you can contact Vaidya, GN; Nagpure, M; Kumar, D or concate me.

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

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. SDS of cas: 59-48-3. About Indolin-2-one, If you have any questions, you can contact Sadak, AE; Karakus, E or concate me.

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

HPLC of Formula: C8H7NO. Recently I am researching about AGOUTI-RELATED PROTEIN; STRUCTURAL BASIS; CYCLIC-PEPTIDES; DISCOVERY; DESIGN; POTENT; TARGETS; SPSB2; RECOGNITION; CYCLIZATION, Saw an article supported by the . Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Gueret, SM; Thavam, S; Carbajo, RJ; Potowski, M; Larsson, N; Dahl, G; Dellsen, A; Grossmann, TN; Plowright, AT; Valeur, E; Lemurell, M; Waldmann, H. The CAS is 59-48-3. Through research, I have a further understanding and discovery 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.

HPLC of Formula: C8H7NO. About Indolin-2-one, 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 concate me.

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

An article Harnessing Applied Potential: Selective beta-Hydrocarboxylation of Substituted Olefins WOS:000510531900023 published article about ELECTROINITIATED POLYMERIZATION; CARBON-DIOXIDE; VISIBLE-LIGHT; ELECTROCHEMICAL DICARBOXYLATION; STYRENE; CO2; ALKENES; ELECTROCARBOXYLATION; CARBOXYLATION; KINETICS in [Alkayal, Anas; Tabas, Volodymyr; Montanaro, Stephanie; Wright, Iain A.; Malkov, Andrei V.; Buckley, Benjamin R.] Loughborough Univ, Sch Sci, Dept Chem, Loughborough LE11 3TU, Leics, England in 2020, Cited 31. HPLC of Formula: C8H7NO. The Name is Indolin-2-one. Through research, I have a further understanding and discovery of 59-48-3

The construction of carboxylic acid compounds in a selective fashion from low value materials such as alkenes remains a long-standing challenge to synthetic chemists. In particular, beta-addition to styrenes is underdeveloped. Herein we report a new electrosynthetic approach to the selective hydrocarboxylation of alkenes that overcomes the limitations of current transition metal and photochemical approaches. The reported method allows unprecedented direct access to carboxylic acids derived from beta,beta-trisubstituted alkenes, in a highly regioselective manner.

About Indolin-2-one, If you have any questions, you can contact Alkayal, A; Tabas, V; Montanaro, S; Wright, IA; Malkov, AV; Buckley, BR or concate me.. HPLC of Formula: C8H7NO

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