100-200 | - Page 4 of 93 - Indole Building Blocks

Lavrenov, Sergey N. et al. published their research in Pharmaceuticals in 2020 | CAS: 6639-06-1

3-(1H-Indol-1-yl)propanoic acid (cas: 6639-06-1) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Reference of 6639-06-1

N-(Hydroxyalkyl) derivatives of tris(1H-indol-3-yl)methylium salts as promising antibacterial agents: synthesis and biological evaluation was written by Lavrenov, Sergey N.;Isakova, Elena B.;Panov, Alexey A.;Simonov, Alexander Y.;Tatarskiy, Viktor V.;Trenin, Alexey S.. And the article was included in Pharmaceuticals in 2020.Reference of 6639-06-1 This article mentions the following:

The main objective of the study was to prepare and elucidate the effect of substitutions in tris(1H-indol-3-yl)methylium derivatives I [n = 1,2,3,4,5] on their antibacterial activity and toxicity to human cells. Antibacterial activity of compounds I was performed in vitro on 12 bacterial strains, including drug resistant strains, that were clin. isolates or collection strains. The cytotoxic effect of the compounds was determined using an test with HPF-hTERT (human postnatal fibroblasts, immortalized with hTERT) cells. The min. inhibitory concentration (MIC) of the most active compound I [n = 5] on Gram-pos. bacteria, including MRSA, was 0.5濠电偞鎸鹃幐?mL. Compounds I [n = 4,5] also revealed high activity against Staphylococcus epidermidis (1.0 and 0.5濠电偞鎸鹃幐?mL, resp.) and moderate activity against Gram-neg. bacteria Escherichia coli (8濠电偞鎸鹃幐?mL) and Klebsiella pneumonia (2 and 8濠电偞鎸鹃幐?mL, resp.). However, they had no activity against Salmonella cholerasuis and Pseudomonas aeruginosa. The most active compounds I [n = 4,5] revealed higher antibacterial activity on MRSA than the reference drug levofloxacin, and their ratio between antibacterial and cytotoxic activity exceeded 10 times. In the experiment, the researchers used many compounds, for example, 3-(1H-Indol-1-yl)propanoic acid (cas: 6639-06-1Reference of 6639-06-1).

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

Sashidhara, Koneni V. et al. published their research in European Journal of Medicinal Chemistry in 2014 | CAS: 827-01-0

5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) 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. Indole plays a fundamental role for QS in E. coli, being one of the signal molecules responsible for the transcription of a variety of genes (gabT, and tnaB ASTD). Application In Synthesis of 5-Chloroindole-3-carboxaldehyde

Design and synthesis of novel indole-chalcone fibrates as lipid lowering agents was written by Sashidhara, Koneni V.;Dodda, Ranga Prasad;Sonkar, Ravi;Palnati, Gopala Reddy;Bhatia, Gitika. And the article was included in European Journal of Medicinal Chemistry in 2014.Application In Synthesis of 5-Chloroindole-3-carboxaldehyde This article mentions the following:

A series of novel indole-chalcone fibrates were synthesized and their hypolipidemic activity was evaluated in triton WR-1339 induced hyperlipidemic rat model. Preliminary studies indicated that three hybrids, e.g., I, exhibited potent in vitro antioxidant and significant in vivo antidyslipidemic effects. The results results suggest that these new hybrid scaffolds may serve as promising leads for the development of next generation lipid lowering agents. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Application In Synthesis of 5-Chloroindole-3-carboxaldehyde).

Rodrigues, Tiago et al. published their research in Angewandte Chemie, International Edition in 2015 | CAS: 827-01-0

5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Application of 827-01-0

Multidimensional De Novo Design Reveals 5-HT_2B Receptor-Selective Ligands was written by Rodrigues, Tiago;Hauser, Nadine;Reker, Daniel;Reutlinger, Michael;Wunderlin, Tiffany;Hamon, Jacques;Koch, Guido;Schneider, Gisbert. And the article was included in Angewandte Chemie, International Edition in 2015.Application of 827-01-0 This article mentions the following:

The authors report a multi-objective de novo design study driven by synthetic tractability and aimed at the prioritization of computer-generated 5-HT_2B receptor ligands with accurately predicted target-binding affinities. Relying on quant. bioactivity models the authors designed and synthesized structurally novel, selective, nanomolar, and ligand-efficient 5-HT_2B modulators with sustained cell-based effects. The authors’ results suggest that seamless amalgamation of computational activity prediction and mol. design with microfluidics-assisted synthesis enables the swift generation of small mols. with the desired polypharmacol. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Application of 827-01-0).

Wu, Zhiqiang et al. published their research in Synthetic Communications in 2021 | CAS: 4769-96-4

6-Nitro-1H-indole (cas: 4769-96-4) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Related Products of 4769-96-4

Solvent-free multi-component synthesis of unsymmetrical bis(indolyl)alkanes with Lewis acid-surfactant-SiO₂ as nanocatalyst was written by Wu, Zhiqiang;Wang, Gang;Li, Zhenliang;Feng, Enke;Liang, Yanping;Zhan, Haijuan;Liu, Wanyi. And the article was included in Synthetic Communications in 2021.Related Products of 4769-96-4 This article mentions the following:

Herein, the multicomponent synthesis of the bis(indolyl)methane derivatives in a ball mill were reported. The reaction was carried out under solvent-free conditions using only the Lewis acid-surfactant-SiO₂ composite nanocatalyst (LASSC) prepared in situ. The unsym. bis(indolyl) methane derivatives containing nitro or fluorine substitution with a yield of 72%-92% were obtained in a short reaction time. Under the action of the verified combined catalyst of AlCl₃闁?H₂O + SDS + SiO₂, the method of preparing unsym. bis(indolyl)methane by mech. grinding without solvent was obvious advantages. Finally, the catalysis system was used eight times without a significant decrease in activity were inspected. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4Related Products of 4769-96-4).

Zhang, Shunji et al. published their research in Youji Huaxue in 2020 | CAS: 4769-96-4

6-Nitro-1H-indole (cas: 4769-96-4) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure. Indole plays a fundamental role for QS in E. coli, being one of the signal molecules responsible for the transcription of a variety of genes (gabT, and tnaB ASTD). Recommanded Product: 6-Nitro-1H-indole

Sulfuric acid catalyzed rapid nucleophilic substitution of propargyl alcohols was written by Zhang, Shunji;Liu, Huili. And the article was included in Youji Huaxue in 2020.Recommanded Product: 6-Nitro-1H-indole This article mentions the following:

Sulfuric acid efficiently catalyzes the direct substitution of the hydroxyl group of propargylic alcs. R¹C(OH)CCR² (R¹ = 3,4-dimethoxyphenyl, 4-(benzyloxy)phenyl, 3-(trifluoromethyl)phenyl, etc.; R² = pentyl, Ph, 4-methoxyphenyl) with a variety of C- and O-based nucleophiles such as isopropanol, phenol, furan, etc. to aid C-C and C-O bond formation. The reactions can be performed in an undried solvent under air atm. to obtain the desired products R¹C(R³)CCR² (R³ = OMe, furan-2-yl, 4-hydroxyphenyl, etc.) in good yields. In most cases, the reaction proceeds to completion in 1 min at room temperature In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4Recommanded Product: 6-Nitro-1H-indole).

Lai, Mei-Jung et al. published their research in European Journal of Medicinal Chemistry in 2019 | CAS: 4769-96-4

6-Nitro-1H-indole (cas: 4769-96-4) 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. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.COA of Formula: C8H6N2O2

1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase was written by Lai, Mei-Jung;Ojha, Ritu;Lin, Mei-Hsiang;Liu, Yi-Min;Lee, Hsueh-Yun;Lin, Tony Eight;Hsu, Kai-Cheng;Chang, Chi-Yen;Chen, Mei-Chuan;Nepali, Kunal;Chang, Jang-Yang;Liou, Jing-Ping. And the article was included in European Journal of Medicinal Chemistry in 2019.COA of Formula: C8H6N2O2 This article mentions the following:

We report structure-activity relationships of 1-arylsulfonyl indoline based benzamides. The benzamide (9) exhibits striking tubulin inhibition with an IC₅₀ value of 1.1 濠电偞鎸鹃幏? better than that of combretastain A-4 (3), and substantial antiproliferative activity against a variety of cancer cells, including MDR-pos. cell lines with an IC₅₀ value of 49 nM (KB), 79 nM (A549), 63 nM (MKN45), 64 nM (KB-VIN10), 43 nM (KB-S15), and 46 nM (KB-7D). Dual inhibitory potential of compound 9 was found as it demonstrated significant inhibitory potential against HDAC1, 2 and 6 in comparison to MS-275 (6). Some key interactions of 9 with the amino acid residues of the active site of tubulin and with amino acid residues of HDAC 1 isoform have been figured out by mol. modeling. Compound 9 also demonstrated significant in vivo efficacy in the human non-small cell lung cancer A549 xenograft model as well as B-cell lymphoma BJAB xenograft tumor model. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4COA of Formula: C8H6N2O2).

Hegedus, Louis S. et al. published their research in Journal of Organic Chemistry in 1981 | CAS: 6639-06-1

3-(1H-Indol-1-yl)propanoic acid (cas: 6639-06-1) belongs to indole derivatives. Indole produced by Proteus, Pseudomonas, Escherichia and other species was shown to be a growth promoting factor in Arabidopsis thaliana. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Product Details of 6639-06-1

Palladium-assisted N-alkylation of indoles: attempted application to polycyclization was written by Hegedus, Louis S.;Winton, Peter M.;Varaprath, Sudarsanan. And the article was included in Journal of Organic Chemistry in 1981.Product Details of 6639-06-1 This article mentions the following:

The palladium(II) complexes of the olefins ethene, propene, and 1-hexene reacted with 1-lithioindole to produce N-alkylated indoles exclusively. Attempts to perform this N-alkylation intramol. (to form tricyclic material from 2-allylskatole) failed. Anilines with dienic side chains in the 2-position were subjected to Pd(II)-assisted cyclization conditions in attempts to induce polycyclization. However, only monocyclization was observed In the experiment, the researchers used many compounds, for example, 3-(1H-Indol-1-yl)propanoic acid (cas: 6639-06-1Product Details of 6639-06-1).

Islam, Mohammad Shahidul et al. published their research in ACS Omega in 2021 | CAS: 827-01-0

5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) 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. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Recommanded Product: 827-01-0

Construction of Spirooxindole Analogues Engrafted with Indole and Pyrazole Scaffolds as Acetylcholinesterase Inhibitors was written by Islam, Mohammad Shahidul;Al-Majid, Abdullah Mohammed;Azam, Mohammad;Verma, Ved Prakash;Barakat, Assem;Haukka, Matti;Elgazar, Abdullah A.;Mira, Amira;Badria, Farid A.. And the article was included in ACS Omega in 2021.Recommanded Product: 827-01-0 This article mentions the following:

Twenty-five new hits of spirooxindole analogs engrafted with indole and pyrazole scaffolds were designed and constructed via a [3+2]cycloaddition (32CA) reaction starting from three components: new chalcone-based indole and pyrazole scaffolds, substituted isatins, and secondary amines. The potency of the compounds were assessed in modulating cholinesterase (AChE) activity using Ellman’s method. Two compounds showed the strongest acetylcholine esterase inhibition (AChEI) with IC₅₀ values of 24.1 and 27.8濠电偞鎸鹃幏? resp. Mol. docking was used to study their interaction with the active site of hAChE. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Recommanded Product: 827-01-0).

Javid, Muhammad Tariq et al. published their research in Bioorganic Chemistry in 2018 | CAS: 150560-58-0

5-Isopropylindoline-2,3-dione (cas: 150560-58-0) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.HPLC of Formula: 150560-58-0

Synthesis, SAR elucidations and molecular docking study of newly designed isatin based oxadiazole analogs as potent inhibitors of thymidine phosphorylase was written by Javid, Muhammad Tariq;Rahim, Fazal;Taha, Muhammad;Nawaz, Mohsan;Wadood, Abdul;Ali, Muhammad;Mosaddik, Ashik;Shah, Syed Adnan Ali;Farooq, Rai Khalid. And the article was included in Bioorganic Chemistry in 2018.HPLC of Formula: 150560-58-0 This article mentions the following:

Thymidine phosphorylase is an enzyme involved in pyrimidine salvage pathway that is identical to platelet-derived endothelial cell growth factor (PD-ECGF) and gliostatin. It is enormously up regulated in a variety of solid tumors. Furthermore, surpassing of TP level protects tumor cells from apoptosis and helps cell survival. Thus TP is identified as a prime target for developing novel anticancer therapies. A new class of exceptionally potent isatin based oxadiazole (1-30) has been synthesized and evaluated for thymidine phosphorylase inhibitory potential. All analogs showed potent thymidine phosphorylase inhibition when compared with standard 7-Deazaxanthine, 7DX (IC₅₀=38.68闂?.12濠电偞鎸鹃幏?. Mol. docking study was performed in order to determine the binding interaction of these newly synthesized compounds, which revealed that these synthesized compounds established stronger hydrogen bonding network with active site of residues as compare to the standard compound 7DX. In the experiment, the researchers used many compounds, for example, 5-Isopropylindoline-2,3-dione (cas: 150560-58-0HPLC of Formula: 150560-58-0).

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).