indole-building-block | - Page 83 of 1434

Banjare, Shyam Kumar et al. published their research in Journal of Organic Chemistry in 2020 | CAS: 4769-96-4

6-Nitro-1H-indole (cas: 4769-96-4) belongs to indole derivatives. The indole subunit is an almost ubiquitous component of biologically active natural products, and its study has been the focus of research for decades. In addition to indole, the strain-release chemistry worked for numerous substrates including amines, alcohols, thiols, carboxylic acids, imidazoles, and pyrazoles.Category: indole-building-block

Cobalt-Catalyzed One-Step Access to Pyroquilon and C-7 Alkenylation of Indoline with Activated Alkenes Using Weakly Coordinating Functional Groups was written by Banjare, Shyam Kumar;Biswal, Pragati;Ravikumar, Ponneri Chandrababu. And the article was included in Journal of Organic Chemistry in 2020.Category: indole-building-block This article mentions the following:

A new strategy for the C(7)-H functionalization of indoline derivatives using first-row transition-metal cobalt was demonstrated wherein the pivaloyl group acts as a weakly coordinating directing group. Biol. important pyroquilon(tetrahydropyroquinolinone) derivatives were synthesized in a one-pot manner through selective C(7)-H functionalization and concomitant cyclization. In this process, aromatic C-H and amidic C-N bonds were cleaved and new C-C and C-N bonds were formed in a step-economical fashion. Further, selective C(7)-H alkenylation of indoline derivatives was also accomplished using activated alkenes by varying the reaction conditions. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4Category: indole-building-block).

Referemce:
Indole alkaloid derivatives as building blocks of natural products from闂佽壈浜崹淇沜illus thuringiensis闂佽壈浜粋鍧闂佽壈浜崹淇沜illus velezensis闂佽壈浜粋鍧 their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Apsel, Beth et al. published their research in Nature Chemical Biology in 2008 | CAS: 754214-56-7

7-Azaindole-5-boronic Acid Pinacol Ester (cas: 754214-56-7) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.SDS of cas: 754214-56-7

Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases was written by Apsel, Beth;Blair, Jimmy A.;Gonzalez, Beatriz;Nazif, Tamim M.;Feldman, Morri E.;Aizenstein, Brian;Hoffman, Randy;Williams, Roger L.;Shokat, Kevan M.;Knight, Zachary A.. And the article was included in Nature Chemical Biology in 2008.SDS of cas: 754214-56-7 This article mentions the following:

The clin. success of multitargeted kinase inhibitors has stimulated efforts to identify promiscuous drugs with optimal selectivity profiles. It remains unclear to what extent such drugs can be rationally designed, particularly for combinations of targets that are structurally divergent. Here we report the systematic discovery of mols. that potently inhibit both tyrosine kinases and phosphatidylinositol-3-OH kinases, two protein families that are among the most intensely pursued cancer drug targets. Through iterative chem. synthesis, X-ray crystallog. and kinome-level biochem. profiling, we identified compounds that inhibit a spectrum of new target combinations in these two families. Crystal structures revealed that the dual selectivity of these mols. is controlled by a hydrophobic pocket conserved in both enzyme classes and accessible through a rotatable bond in the drug skeleton. We show that compound I blocks the proliferation of tumor cells by direct inhibition of oncogenic tyrosine kinases and phosphatidylinositol-3-OH kinases. These mols. demonstrate the feasibility of accessing a chem. space that intersects two families of oncogenes. In the experiment, the researchers used many compounds, for example, 7-Azaindole-5-boronic Acid Pinacol Ester (cas: 754214-56-7SDS of cas: 754214-56-7).

Abu Khalaf, Reema et al. published their research in Molecular Diversity in 2022 | CAS: 167631-84-7

Methyl 5-fluoro-1H-indole-2-carboxylate (cas: 167631-84-7) belongs to indole derivatives. Indole produced by Proteus, Pseudomonas, Escherichia and other species was shown to be a growth promoting factor in Arabidopsis thaliana. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Application In Synthesis of Methyl 5-fluoro-1H-indole-2-carboxylate

Discovery, synthesis and in combo studies of Schiff闂備胶鍋ㄩ崕鎶芥倶?bases as promising dipeptidyl peptidase-IV inhibitors was written by Abu Khalaf, Reema;Awad, Maha;Al-Essa, Luay;Mefleh, Sara;Sabbah, Dima;Al-Shalabi, Eveen;Shabeeb, Ihsan. And the article was included in Molecular Diversity in 2022.Application In Synthesis of Methyl 5-fluoro-1H-indole-2-carboxylate This article mentions the following:

Diabetes mellitus is a main global health apprehension. Macrovascular illnesses, neuropathy, retinopathy, and nephropathy are considered some of its severe hitches. Gliptins are a group of hypoglycemic agents that inhibit dipeptidyl peptidase-IV (DPP-IV) enzyme and support blood glucose-lowering effect of incretins. In the current research, synthesis, characterization, docking, and biol. evaluation of fourteen Schiff闂備胶鍋ㄩ崕鎶芥倶?bases 5a-f and 9a-h were carried out. Compound 9f revealed the best in vitro anti-DPP-IV activity of 35.7% inhibition at a concentration of 100 濠电偞鎸鹃幏? Compounds 9c and 9f with the highest in vitro DPP-IV inhibition were subjected to the in vivo glucose-lowering test using vildagliptin as a pos. inhibitor. Vildagliptin, 9c, and 9f showed significant reduction in the blood glucose levels of the treated mice after 30 min of glucose administration. Moreover, induced fit docking showed that these derivatives accommodated the enzyme binding site with comparable docking scores. Schiff闂備胶鍋ㄩ崕鎶芥倶?bases can serve as promising lead for the development of new DPP-IV inhibitors. In the experiment, the researchers used many compounds, for example, Methyl 5-fluoro-1H-indole-2-carboxylate (cas: 167631-84-7Application In Synthesis of Methyl 5-fluoro-1H-indole-2-carboxylate).

Kryshchyshyn-Dylevych, Anna et al. published their research in Synthetic Communications in 2020 | CAS: 167631-84-7

Methyl 5-fluoro-1H-indole-2-carboxylate (cas: 167631-84-7) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Recommanded Product: 167631-84-7

Synthesis and anticancer activity evaluation of 3-(4-oxo-2-thioxothiazolidin-5-yl)-1H-indole-carboxylic acids derivatives was written by Kryshchyshyn-Dylevych, Anna;Garazd, Myroslav;Karkhut, Andrew;Polovkovych, Sviatoslav;Lesyk, Roman. And the article was included in Synthetic Communications in 2020.Recommanded Product: 167631-84-7 This article mentions the following:

A mild and efficient method for the synthesis of 1-oxo-9H-thiopyrano[3,4-b]indole-3-carboxylic acids I (R = F, H, OMe) and dimerized 3-(4-carboxy-1H-3-indolyl)-2-propenoic acids II (R¹ = Me, Et) via alk. hydrolysis of 3-(rhodanin-5-yl)-1H-indole-2-carboxylic acids derivatives III (R² = H, methoxycarbonyl; R³ = H, methoxycarbonyl, carboxy; R⁴ = H, Me, Et) was elaborated. Anticancer activity screening in NCI60-cell lines assay allowed identification of III (R = F; R² = R⁴ = H; R³ = methoxycarbonyl) with significant antimitotic activity at micromolar and submicromolar concentrations In the experiment, the researchers used many compounds, for example, Methyl 5-fluoro-1H-indole-2-carboxylate (cas: 167631-84-7Recommanded Product: 167631-84-7).

Jones, Hilton Ira et al. published their research in Journal of the American Chemical Society in 1918 | CAS: 24407-32-7

4,5,6,7-Tetrabromoisoindoline-1,3-dione (cas: 24407-32-7) belongs to indole derivatives. Indole produced by Proteus, Pseudomonas, Escherichia and other species was shown to be a growth promoting factor in Arabidopsis thaliana. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Name: 4,5,6,7-Tetrabromoisoindoline-1,3-dione

Preparation of methylamine was written by Jones, Hilton Ira;Wheatley, Roth. And the article was included in Journal of the American Chemical Society in 1918.Name: 4,5,6,7-Tetrabromoisoindoline-1,3-dione This article mentions the following:

A study of the equations given by Werner to explain the mechanism of the reaction between HCHO and NH₄Cl shows that if the temperature should be kept down and the decomposition of the HCO₂H as It formed should be hastened MeNH₂ should be almost the sole product, a deduction which has been verified by experiment Of 4 experiments, one was a duplication of W.’s, the 2nd was a slow distillation like the first but under 20 mm., in the 3rd the material was refluxed 8 hrs. under atm. pressure before the distillation (also under atm. pressure). while in the 4th the refluxing (4.5 hrs.) and distillation were carried out under 20 mm. Working with 150 g. NH₄Cl and 300 g. of 40% HCHO, the following results were obtained in the 4 experiments, resp.: unchanged NH₄Cl, 46.47, 79.9, 33.5, 27.18; MeNH₂Cl, 70.67, 44.83, 67.60, 82.50; Me₂NH₂Cl, 12.40, 9.66, 17.35, 7.90; non-crystallizing residue, 45.53, 23.53, 64-73, 54.43 g. The sp. gr. and rotations of the distillates and the approx. amounts of HCO₂Me and HCO₂H present were also determined The results all accord with W.’s theory. In the experiment, the researchers used many compounds, for example, 4,5,6,7-Tetrabromoisoindoline-1,3-dione (cas: 24407-32-7Name: 4,5,6,7-Tetrabromoisoindoline-1,3-dione).

Obara, Tetsujiro et al. published their research in Nippon Shokuhin Kogyo Gakkaishi in 1963 | CAS: 1912-45-4

2-(5-Chloro-1H-indol-3-yl)acetic acid (cas: 1912-45-4) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Recommanded Product: 1912-45-4

Manufacture of foods. I. Influence of growth regulators on germination of barley and rye. 1. Amylase activity was written by Obara, Tetsujiro;Ogasawara, Yasokichi;Kimura, Tsugie. And the article was included in Nippon Shokuhin Kogyo Gakkaishi in 1963.Recommanded Product: 1912-45-4 This article mentions the following:

Influences of 婵?naphthaleneacetic acid and gibberellin were tested on amylase activities and growth of germinating barley and rye. Both barley and rye germinated best on a medium containing 0.1-1.0 ppm. gibberellin. Gibberellin increased the formation of amylase 60-100% at 1 ppm., while 婵?naphthaleneacetic acid had no effect. The highest amylase activity was produced after 80 hrs. of incubation in the presence of 1 ppm. gibberellin. In the experiment, the researchers used many compounds, for example, 2-(5-Chloro-1H-indol-3-yl)acetic acid (cas: 1912-45-4Recommanded Product: 1912-45-4).

Ekhtiari, Zeinab et al. published their research in Zeitschrift fuer Naturforschung, B: A Journal of Chemical Sciences in 2016 | CAS: 24407-32-7

4,5,6,7-Tetrabromoisoindoline-1,3-dione (cas: 24407-32-7) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.SDS of cas: 24407-32-7

An expedient and convenient approach for one-pot synthesis of 1H-isoindole-1,3(2H)-diones was written by Ekhtiari, Zeinab;Havasi, Forugh;Nikpour, Farzad. And the article was included in Zeitschrift fuer Naturforschung, B: A Journal of Chemical Sciences in 2016.SDS of cas: 24407-32-7 This article mentions the following:

An easy and expedient method for the one-pot synthesis of 1H-isoindole-1,3(2H)-diones, e.g., 3-hydroxy-2,3-dihydro-1H-isoindol-1-one has been developed by the reaction of corresponding cyclic anhydrides, e.g., 3-hydroxy-1,3-dihydro-2-benzofuran-1-one with guanidinium chloride as a nitrogen source in the presence of FeCl₃ as a catalyst under mild reaction conditions. In the experiment, the researchers used many compounds, for example, 4,5,6,7-Tetrabromoisoindoline-1,3-dione (cas: 24407-32-7SDS of cas: 24407-32-7).

Luo, Guanglin et al. published their research in Journal of Medicinal Chemistry in 2019 | CAS: 898746-35-5

1H-Pyrrolo[2,3-b]pyridine-6-carboxylic acid (cas: 898746-35-5) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Category: indole-building-block

Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective Na_V1.7 Inhibitors for the Treatment of Pain was written by Luo, Guanglin;Chen, Ling;Easton, Amy;Newton, Amy;Bourin, Clotilde;Shields, Eric;Mosure, Kathy;Soars, Matthew G.;Knox, Ronald J.;Matchett, Michele;Pieschl, Rick L.;Post-Munson, Debra J.;Wang, Shuya;Herrington, James;Graef, John;Newberry, Kimberly;Sivarao, Digavalli V.;Senapati, Arun;Bristow, Linda J.;Meanwell, Nicholas A.;Thompson, Lorin A.;Dzierba, Carolyn. And the article was included in Journal of Medicinal Chemistry in 2019.Category: indole-building-block This article mentions the following:

3-Aryl-indole and 3-aryl-indazole derivatives were identified as potent and selective Na_v1.7 inhibitors. Compound I was shown to be efficacious in the mouse formalin assay and also reduced complete Freund’s adjuvant (CFA)-induced thermal hyperalgesia and chronic constriction injury (CCI) induced cold allodynia and models of inflammatory and neuropathic pain, resp., following i.p. (IP) doses of 30 mg/kg. The observed efficacy could be correlated with the mouse dorsal root ganglion exposure and Na_V1.7 potency associated with I. In the experiment, the researchers used many compounds, for example, 1H-Pyrrolo[2,3-b]pyridine-6-carboxylic acid (cas: 898746-35-5Category: indole-building-block).

Xu, Hang et al. published their research in European Journal of Organic Chemistry in 2022 | CAS: 4583-55-5

5-Bromo-2,3-dimethyl-1H-indole (cas: 4583-55-5) belongs to indole derivatives. Indole, first isolated in 1866, and it is commonly synthesized from phenylhydrazine and pyruvic acid, although several other procedures have been discovered. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Application of 4583-55-5

Green Oxidation of Indoles Using Molecular Oxygen over a Copper Nitride Nanocube Catalyst was written by Xu, Hang;Yamaguchi, Sho;Mitsudome, Takato;Mizugaki, Tomoo. And the article was included in European Journal of Organic Chemistry in 2022.Application of 4583-55-5 This article mentions the following:

Oxidative transformation of indoles is a promising approach for synthesizing valuable nitrogen-containing compounds; however, conventional methods use toxic oxidants and additives. Herein, authors report for the first time the catalytic oxidative trimerization and the oxygenative cleavage (Witkop oxidation) of indoles using mol. oxygen under additive-free conditions accomplished by a copper nitride nanocube (Cu₃N NC) catalyst. The Cu₃N NC catalyst exhibits excellent activity to produce various indolin-3-ones and 2-ketoanilides with high functional group tolerance. Owing to this excellent catalytic performance, the Cu₃N NC catalyst is distinguished from the conventional copper catalysts, demonstrating the high catalytic potential of metal nitride in organic synthesis. In the experiment, the researchers used many compounds, for example, 5-Bromo-2,3-dimethyl-1H-indole (cas: 4583-55-5Application of 4583-55-5).

Zhao, Yun-Long et al. published their research in Angewandte Chemie, International Edition in 2017 | CAS: 320734-35-8

7-Bromooxindole (cas: 320734-35-8) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Computed Properties of C8H6BrNO

Organocatalytic Friedel-Crafts Alkylation/Lactonization Reaction of Naphthols with 3-Trifluoroethylidene Oxindoles: The Asymmetric Synthesis of Dihydrocoumarins was written by Zhao, Yun-Long;Lou, Qin-Xin;Wang, Long-Sheng;Hu, Wen-Hui;Zhao, Jun-Ling. And the article was included in Angewandte Chemie, International Edition in 2017.Computed Properties of C8H6BrNO This article mentions the following:

Naphthols and 3-trifluoroethylidene oxindoles were found to undergo an asym. Friedel-Crafts alkylation/lactonization reaction, catalyzed by only 2.5 mol % of a quinine-derived squaramide catalyst, to afford the corresponding 婵?aryl-闁?trifluoromethyl dihydrocoumarin derivatives I (R¹ = H, 5-Me, 5-Cl, 5-Br, 7-F, 7-Br; R² = H, 6-MeO, 6-OBn, 6-Ph, etc.) in high yields (up to 99 %) with excellent enantio- and diastereoselectivities (up to 98 % ee, >20:1 d.r.). Importantly, the lactonization proceeded by nucleophilic attack of the naphthol hydroxy group at the amide motif of the oxindoles under mild reaction conditions. This protocol represents a new strategy for the formation of dihydrocoumarins by an efficient intramol. amide C-N bond-cleavage and esterification process. In the experiment, the researchers used many compounds, for example, 7-Bromooxindole (cas: 320734-35-8Computed Properties of C8H6BrNO).