indole-building-block | - Page 105 of 1434

Indrigo, Eugenio et al. published their research in Chemical Communications (Cambridge, United Kingdom) in 2016 | CAS: 754214-56-7

7-Azaindole-5-boronic Acid Pinacol Ester (cas: 754214-56-7) 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. 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 754214-56-7

Palladium-mediated in situ synthesis of an anticancer agent was written by Indrigo, Eugenio;Clavadetscher, Jessica;Chankeshwara, Sunay V.;Lilienkampf, Annamaria;Bradley, Mark. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2016.Product Details of 754214-56-7 This article mentions the following:

As a novel prodrug activation strategy Pd(0) nanoparticles, entrapped within a modular polymeric support, were used in cell culture, to synthesize the anticancer agent PP-121 from two non-toxic precursors, thereby inducing cell death in the first example of in situ mediated drug synthesis. In the experiment, the researchers used many compounds, for example, 7-Azaindole-5-boronic Acid Pinacol Ester (cas: 754214-56-7Product Details of 754214-56-7).

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Yilmaz, Ayse Didem et al. published their research in Journal of Enzyme Inhibition and Medicinal Chemistry in 2012 | 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. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Product Details of 827-01-0

Synthesis and antioxidant activity evaluations of melatonin-based analogue indole-hydrazide/hydrazone derivatives was written by Yilmaz, Ayse Didem;Coban, Tulay;Suzen, Sibel. And the article was included in Journal of Enzyme Inhibition and Medicinal Chemistry in 2012.Product Details of 827-01-0 This article mentions the following:

Melatonin (MLT) is a hormone synthesized from the pineal gland. It is a direct scavenger of free radicals, which is related to its ability to defend cells from oxidative stress. Recently MLT-related compounds are under investigation to establish which ones exhibit the maximum activity with the lowest side effects. In this study, 5-chloroindole hydrazide/hydrazone derivatives were synthesized from 5-chloroindole-3-carboxaldehyde and phenylhydrazine derivatives All the compounds were characterized and in vitro antioxidant activity was investigated against MLT and BHT. Most of the compounds showed strong inhibitory effect on the superoxide radical scavenging assay at 1 mM concentration (79 to 95%). Almost all the tested compounds possessed strong scavenging activity against the DPPH radical scavenging activity with IC₅₀ values (2 to 60 μM). Lastly, compound (E)-I revealed stronger inhibitory activity against MLT in the LP inhibitory assay at 0.1mM concentration (51%) while the rest of the compounds showed moderate inhibition. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Product Details of 827-01-0).

Liang, Yuwang et al. published their research in New Journal of Chemistry in 2022 | 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.Synthetic Route of C8H6N2O2

In situ preparation of a ferric polymeric aluminum chloride-silica gel nanocatalyst by mechanical grinding and its solid-phase catalytic behavior in organic synthesis was written by Liang, Yuwang;Wang, Gang;Li, Xiang;Zhang, Qiuping;Zhan, Haijuan;Bi, Shuxian;Wu, Zhiqiang;Liu, Wanyi. And the article was included in New Journal of Chemistry in 2022.Synthetic Route of C8H6N2O2 This article mentions the following:

In recent years, clean and sustainable mechanochem. solvent-free reactions have emerged as a viable alternative to solution chem. In order to completely solve the problem of environmental pollution caused by solvents and surfactants in LASC and LASSC systems, a green method for the in situ preparation of environmentally friendly inorganic polymeric Lewis acids and silica gel as nanocatalysts (PLASC) under solvent-free mech. grinding conditions was designed and realized by mechanochem. means, which is simple to operate and the process generates no other waste. Subsequently, 3-alkylindole derivatives (35-75%), β-amino alc. derivatives (90%), benzimidazole derivatives (85-90%) and quinoxaline derivatives (93-99%) were synthesized by a one-pot cooking method under continuous grinding conditions. The mechanism of in situ self-assembly of PAFC and silica gel on the silica gel surface under mech. forces and the new catalytically active species-Si-O-Al(Fe) polynuclear metal complexes resulting from chem. reforming were discovered and confirmed by SEM, HR-TEM, FT-IR, XRD and XPS tests as well as by solution morphol. studies. The true active center -O-Fe-O-Si-O-/-O-Si-O-Al-O- chem. bonding unit was revealed and found to be a nanoscale fibrous structure that is highly stable and can be reused at least 10 times without deactivation. The PLASC catalyst has remarkable green chem. properties such as easy recycling and a very low E factor, making it a new type of cheap, efficient and green catalyst. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4Synthetic Route of C8H6N2O2).

Guo, Jincheng et al. published their research in Journal of Agricultural and Food Chemistry in 2019 | CAS: 90271-86-6

5-Bromo-3-cyanoindole (cas: 90271-86-6) belongs to indole derivatives. Indole produced by Proteus, Pseudomonas, Escherichia and other species was shown to be a growth promoting factor in Arabidopsis thaliana. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Computed Properties of C9H5BrN2

Optimization, Structure-Activity Relationship, and Mode of Action of Nortopsentin Analogues Containing Thiazole and Oxazole Moieties was written by Guo, Jincheng;Hao, Yanan;Ji, Xiaofei;Wang, Ziwen;Liu, Yuxiu;Ma, Dejun;Li, Yongqiang;Pang, Huailin;Ni, Jueping;Wang, Qingmin. And the article was included in Journal of Agricultural and Food Chemistry in 2019.Computed Properties of C9H5BrN2 This article mentions the following:

Plant diseases seriously endanger plant health, and it is very difficult to control them. A series of nortopsentin analogs were designed, synthesized, and evaluated for their antiviral activities and fungicidal activities. Most of these compounds displayed higher antiviral activities than ribavirin. Compounds (CAS 224434-76-8, 265110-91-6, 272104-33-3), with excellent antiviral activities, emerged as novel antiviral lead compounds, among which compound (CAS 265110-91-6) was selected for further antiviral mechanism research. The mechanism research results indicated that these compounds may play an antiviral role by aggregating viral particles to prevent their movement in plants. Further fungicidal activity tests revealed that nortopsentin analogs displayed broad-spectrum fungicidal activities. Compounds (CAS 2376842-39-4 and 2376840-03-6) displayed higher antifungal activities against Alternaria solani than the com. fungicides carbendazim and chlorothalonil. Current research has laid a foundation for the application of nortopsentin analogs in plant protection. In the experiment, the researchers used many compounds, for example, 5-Bromo-3-cyanoindole (cas: 90271-86-6Computed Properties of C9H5BrN2).

Ji, Li et al. published their research in Organic Letters in 2015 | CAS: 150560-58-0

5-Isopropylindoline-2,3-dione (cas: 150560-58-0) 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. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Recommanded Product: 5-Isopropylindoline-2,3-dione

Palladium-Catalyzed Glycosylation: Novel Synthetic Approach to Diverse N-Heterocyclic Glycosides was written by Ji, Li;Xiang, Shao-Hua;Leng, Wei-Lin;Le Mai Hoang, Kim;Liu, Xue-Wei. And the article was included in Organic Letters in 2015.Recommanded Product: 5-Isopropylindoline-2,3-dione This article mentions the following:

An efficient and highly stereoselective method for the construction of N-heterocyclic glycosides is reported. This method is based on a palladium-catalyzed allylation which proceeded to provide N-heterocyclic glycosyl compounds in good-to-excellent yields with β- or α-selectivity. Various N-nucleophiles were examined for this reaction and selected N-glycosyl isatin substrates were further elaborated to bis-indole sugars which have potential as antiproliferative drugs. In the experiment, the researchers used many compounds, for example, 5-Isopropylindoline-2,3-dione (cas: 150560-58-0Recommanded Product: 5-Isopropylindoline-2,3-dione).

Liu, Ruixing et al. published their research in Chemical Communications (Cambridge, United Kingdom) in 2018 | 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.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.SDS of cas: 4769-96-4

Synthesis of indolizine derivatives containing eight-membered rings via a gold-catalyzed two-fold hydroarylation of diynes was written by Liu, Ruixing;Wang, Qiang;Wei, Yin;Shi, Min. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2018.SDS of cas: 4769-96-4 This article mentions the following:

A gold-catalyzed method for the construction of indolizines with eight-membered rings has been developed. The reaction proceeded through a two-fold hydroarylation with indole or pyrrole derivatives containing a 1,6-diyne using a tri(1-adamantyl)phosphine gold complex as the catalyst, affording 1,8-disubstituted indolizines in moderate to good yields in DCE at 80°. The potential usefulness of these indolizines as blue or green OLEDs has been also disclosed. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4SDS of cas: 4769-96-4).

Ding, Ying et al. published their research in Molecules in 2021 | CAS: 112656-95-8

7-Nitroindoline-2,3-dione (cas: 112656-95-8) belongs to indole derivatives. Indole produced by Proteus, Pseudomonas, Escherichia and other species was shown to be a growth promoting factor in Arabidopsis thaliana. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.HPLC of Formula: 112656-95-8

Synthesis and antiproliferatory activities evaluation of multi-substituted isatin derivatives was written by Ding, Ying;Zhao, Lianbo;Fu, Ying;Hao, Lei;Fu, Yupeng;Yuan, Yuan;Yu, Peng;Teng, Yuou. And the article was included in Molecules in 2021.HPLC of Formula: 112656-95-8 This article mentions the following:

A series of multi-substituted isatin derivatives I (R¹ = H, F, Cl, Br, OMe; R² = F, Cl, Me, etc.) were synthesized using the powerful Sandmeyer reaction. Inhibition of proliferation activities of these derivatives against human leukemia cells (K562), human hepatocellular carcinoma cells (HepG2) and human colon carcinoma cells (HT-29) were evaluated in vitro using the MTT assay. Among the series, compound I (R¹ = F; R² = Br) exhibited strong antiproliferatory activities against K562, HepG2 and HT-29 cells with IC₅₀ values of 1.75, 3.20, and 4.17μM, resp. The morphol., growth inhibitory and apoptosic effects of compound I (R¹ = F; R² = Br) in K562 cells, wound healing effect in HepG2 cells, and tube formatting effect in matrix gel of HUVEC cells were evaluated consequently. All results indicated that compound I (R¹ = F; R² = Br) could be used as a potential antitumor agent in further investigations. In the experiment, the researchers used many compounds, for example, 7-Nitroindoline-2,3-dione (cas: 112656-95-8HPLC of Formula: 112656-95-8).

Brandukova, N. E. et al. published their research in Izvestiya Akademii Nauk, Seriya Khimicheskaya in 1996 | CAS: 5388-42-1

2-Phenylisoindolin-1-one (cas: 5388-42-1) 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 was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Category: indole-building-block

Reactions of imides with samarium(II) iodide was written by Brandukova, N. E.;Vygodskii, Ya. S.;Komarova, L. I.;Strelkova, T. V.. And the article was included in Izvestiya Akademii Nauk, Seriya Khimicheskaya in 1996.Category: indole-building-block This article mentions the following:

One of the carbonyl groups of N-phenylphthalimide is reduced by SmI₂ to a CHOH or CH₂ group at ∼20°. The reaction pathway depends mainly on the reactant ratio and the sequence of reactant addition to the reaction mixture Under similar conditions, both CO groups of N-acetylcaprolactam are reduced by SmI₂, whereas the CO group of ε-caprolactam is not reduced. In the experiment, the researchers used many compounds, for example, 2-Phenylisoindolin-1-one (cas: 5388-42-1Category: indole-building-block).

La Regina, Giuseppe et al. published their research in Journal of Medicinal Chemistry in 2009 | CAS: 210345-56-5

Methyl 5-bromo-1H-indole-2-carboxylate (cas: 210345-56-5) 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. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.HPLC of Formula: 210345-56-5

New Arylthioindoles and Related Bioisosteres at the Sulfur Bridging Group. 4. Synthesis, Tubulin Polymerization, Cell Growth Inhibition, and Molecular Modeling Studies was written by La Regina, Giuseppe;Sarkar, Taradas;Bai, Ruoli;Edler, Michael C.;Saletti, Roberto;Coluccia, Antonio;Piscitelli, Francesco;Minelli, Lara;Gatti, Valerio;Mazzoccoli, Carmela;Palermo, Vanessa;Mazzoni, Cristina;Falcone, Claudio;Scovassi, Anna Ivana;Giansanti, Vincenzo;Campiglia, Pietro;Porta, Amalia;Maresca, Bruno;Hamel, Ernest;Brancale, Andrea;Novellino, Ettore;Silvestri, Romano. And the article was included in Journal of Medicinal Chemistry in 2009.HPLC of Formula: 210345-56-5 This article mentions the following:

A series of arylthioindoles, e.g., I (X = S, R¹ = H, CO₂Me, CO₂Et, R² = H, Cl, Br, OMe), the corresponding ketones I (X = CO) and diarylmethanes I (X = CH₂), as well as pyrrole II (Y = CH₂, CO, Z = CH, R³ = CO₂Et, R⁴ = R⁵ = H; etc.) and imidazole analogs II (Y = CO, Z = N, R³ = R⁵ = H, R⁴ = CO₂Et; etc.) were synthesized and their activity as tubulin polymerization and cancer cell growth inhibitors assessed. As growth inhibitors of MCF-7 cells, sulfur derivatives were superior or sometimes equivalent to the ketones, while methylene derivatives were substantially less effective. Indoles I (X = S, R¹ = H, R² = Br; X = S, CO, CH₂, R¹ = CO₂Me, R² = Br, OMe) showed ∼50% of inhibition on human HeLa and HCT116/chr3 cells at 0.5 μM, and these compounds inhibited the growth of HEK, M14, and U937 cells with IC₅₀‘s in the 78-220 nM range. While murine macrophage J744.1 cell growth was significantly less affected (20% at higher concentrations), four other non-transformed cell lines remained sensitive to these indoles. The effect of drug treatment on cell morphol. was examined by time-lapse microscopy. In a protocol set up to evaluate toxicity on the Saccharomyces cerevisiae BY4741 wild type strain, compounds I (X = S, R¹ = H, R² = Br) and II (Y = CH₂, Z = CH, R³ = CO₂H, R⁴ = R⁵ = H) strongly reduced cell growth, and I (X = CH₂, R¹ = CO₂Me, R² = Br; X = S, CO, R¹ = CO₂Me, R² = OMe) also showed significant inhibition. In the experiment, the researchers used many compounds, for example, Methyl 5-bromo-1H-indole-2-carboxylate (cas: 210345-56-5HPLC of Formula: 210345-56-5).

Liu, Huan et al. published their research in Chinese Chemical Letters in 2022 | CAS: 4769-96-4

6-Nitro-1H-indole (cas: 4769-96-4) 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.Formula: C8H6N2O2

Access to 3-alkylselenindoles by multicomponent reaction of indoles, selenium powder and unactivated alkyl halides under transition-metal-free conditions was written by Liu, Huan;Cai, Zhong-Jian;Ji, Shun-Jun. And the article was included in Chinese Chemical Letters in 2022.Formula: C8H6N2O2 This article mentions the following:

Herein, a convenient and efficient multicomponent reaction of indoles, selenium powder and unactivated alkyl halides is reported. This protocol provides a practical, and facile approach for the synthesis of 3-alkylselenindole derivatives The advantages of this strategy include mild and transition-metal-free conditions, broad functional group tolerance, the use of simple and easily accessible selenium powder and alkyl halides as coupling partners. More importantly, the reaction proceeded smoothly with a large scale (> 10 g, > 90% yield), which further highlighted the potential application of this selenation strategy. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4Formula: C8H6N2O2).