Day: October 21, 2022

Application of 120-72-9In 2020 ,《Role of indole scaffolds as pharmacophores in the development of anti-lung cancer agents》 appeared in Molecules. The author of the article were Dhuguru, Jyothi; Skouta, Rachid. The article conveys some information:

A review. Lung cancer is the leading cause of death in men and women worldwide, affecting millions of people. Between the two types of lung cancers, non-small cell lung cancer (NSCLC) is more common than small cell lung cancer (SCLC). Besides surgery and radiotherapy, chemotherapy is the most important method of treatment for lung cancer. Indole scaffold is considered one of the most privileged scaffolds in heterocyclic chem. Indole may serve as an effective probe for the development of new drug candidates against challenging diseases, including lung cancer. In this review, we will focus on discussing the existing indole based pharmacophores in the clin. and pre-clin. stages of development against lung cancer, along with the synthesis of some of the selected anti-lung cancer drugs. Moreover, the basic mechanism of action underlying indole based anti-lung cancer treatment, such as protein kinase inhibition, histone deacetylase inhibition, DNA topoisomerase inhibition, and tubulin inhibition will also be discussed. The results came from multiple reactions, including the reaction of 1H-Indole(cas: 120-72-9Application of 120-72-9)

1H-Indole(cas: 120-72-9) belongs to indole. 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. 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.Application of 120-72-9

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

《Copper-Catalyzed Aerobic Oxidative Amination of Indole Derivatives via Single-Electron Transfer》 was written by Zhao, Peizheng; Wang, Ke; Yue, Yuanyuan; Chao, Junli; Ye, Yaqing; Tang, Qinghu; Liu, Jianming. Related Products of 399-52-0 And the article was included in ChemCatChem in 2020. The article conveys some information:

An efficient and clean approach for the oxidative amination of indole derivatives with phenothiazines is developed under copper-catalyzed aerobic conditions. The reaction is carried out via the cross-coupling of indole radical cation and phenothiazine radical in air. This approach offers a new perspective in the application of phenothiazine as a nitrogen group source for C-N bond formation reactions. The experimental process involved the reaction of 5-Fluoro-1H-indole(cas: 399-52-0Related Products of 399-52-0)

5-Fluoro-1H-indole(cas: 399-52-0) is a member of aromaticfluorinated building blocks. Fluorine-containing aromatics have been incorporated into crop-protection chemicals (herbicides, insecticides, fungicides). Liquid crystals, positron emission tomography, and imaging systems represent new areas where fluoroaromatics and fluoroheterocyclics have gained attention.Related Products of 399-52-0

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

Shaikh, Iqbal N.; Rahim, Abdul; Faazil, Shaikh; Adil, Syed Farooq; Assal, Mohamed E.; Hatshan, Mohammad Rafe published an article in 2021. The article was titled 《BF3-OEt2 catalyzed C3-alkylation of indole: synthesis of indolylsuccinimides and their cytotoxicity studies》, and you may find the article in Molecules.Recommanded Product: 5-Fluoro-1H-indole The information in the text is summarized as follows:

A simple and efficient BF3-OEt2 promoted C3-alkylation of indole has been developed to obtain 3-indolylsuccinimides I (R1 = H, OMe, F, Br, CN, NO2; R2 = H, Me, Bn; R3 = Me, Ph, Bn) from com. available indoles II and maleimides III, with excellent yields under mild reaction conditions. Furthermore, anti-proliferative activity of these conjugates was evaluated against HT-29 (Colorectal), Hepg2 (Liver) and A549 (Lung) human cancer cell lines. One of the compounds, I (R1 = H, R2 = R3 = Me), having N,N-Dimethylatedindolylsuccinimide is a potent congener amongst the series with IC50 value 0.02μM and 0.8μM against HT-29 and Hepg2 cell lines, resp., and compound I (R1 = R2 = H, R3 = Bn) was most active amongst the series with IC50 value 1.5μM against A549 cells. Mol. docking study and mechanism of reaction have briefly been discussed. This method is better than previous reports in view of yield and substrate scope including electron deficient indoles. After reading the article, we found that the author used 5-Fluoro-1H-indole(cas: 399-52-0Recommanded Product: 5-Fluoro-1H-indole)

5-Fluoro-1H-indole(cas: 399-52-0) is a member of aromaticfluorinated building blocks. Fluorine-containing aromatics have been incorporated into crop-protection chemicals (herbicides, insecticides, fungicides). Liquid crystals, positron emission tomography, and imaging systems represent new areas where fluoroaromatics and fluoroheterocyclics have gained attention.Recommanded Product: 5-Fluoro-1H-indole

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

Reference of 1H-IndoleIn 2019 ,《C2/C4 Regioselective Heteroarylation of Indoles by Tuning C-H Metalation Modes》 appeared in ACS Catalysis. The author of the article were Chen, Shuyou; Zhang, Min; Su, Rongchuan; Chen, Xingyu; Feng, Boya; Yang, Yudong; You, Jingsong. The article conveys some information:

The development of a rational strategy to achieve the complete regioselectivity and the capability to switch regioselectivity is an appealing, yet challenging, puzzle in transition-metal-catalyzed oxidative Ar-H/Ar-H cross-coupling. Disclosed herein is an iridium-catalyzed C2/C4 regioselective C-H heteroarylation of indoles with the help of a pivaloyl group at the C3 position. The judicious choice of the catalytic systems allows the C2-heteroarylation of indole via a concerted metalation-deprotonation (CMD) process and the C4-heteroarylation via a trimol. electrophilic substitution (SE3) pathway. The oxidants Cu(OAc)2·H2O and Ag2O are demonstrated to play a vital role in the C2/C4 regioselectivity. In this Article, a heteroaryl-Ir(III)-heteroaryl complex prior to reductive elimination is successfully isolated and characterized, which represents the first example of capturing the bis(hetero)aryl metallic intermediate in oxidative Ar-H/Ar-H cross-coupling. The regiodivergent heteroarylation of indoles developed herein provides an opportunity to rapidly assemble diverse C4- and C2-heteroarylated indoles. The experimental part of the paper was very detailed, including the reaction process of 1H-Indole(cas: 120-72-9Reference of 1H-Indole)

1H-Indole(cas: 120-72-9) belongs to indole. 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. 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.Reference of 1H-Indole

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

Kelly, R. J.; Moser, B. C. published their research in HortScience on December 31 ,1983. The article was titled 《Influence of temperature and auxin on root regeneration by seedlings of Liriodendron tulipifera L》.Name: Potassium 4-(1H-indol-3-yl)butanoate The article contains the following contents:

Root regeneration and shoot growth of seedlings of L. tulipifera (tulip tree) increased as temperature of either the soil or aerial growing environment increased from 10° to 21°. IBA K salt  [60096-23-3] applied to the tap roots at 1000 mg/L, increased root regeneration and shoot growth when both air and soil temperatures were at 15.5° or 21°. When air temperature was maintained at 21° and soil temperature was varied from 10° to 21°, root regeneration and shoot growth increased as soil temperature increased. IBA increased root regeneration only when soil temperature was 21°. In the experiment, the researchers used Potassium 4-(1H-indol-3-yl)butanoate(cas: 60096-23-3Name: Potassium 4-(1H-indol-3-yl)butanoate)

Potassium 4-(1H-indol-3-yl)butanoate(cas: 60096-23-3) is auxin-family plant hormone, and is thought to be a precursor of indole-3-acetic acid (IAA) the most abundant and the basic auxin natively occurring and functioning in plants. IAA generates the majority of auxin effects in intact plants, and is the most potent native auxin.Name: Potassium 4-(1H-indol-3-yl)butanoate

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

The author of 《Switchable Skeletal Rearrangement of Dihydroisobenzofuran Acetals with Indoles》 were Li, Guofeng; Yao, Ying; Wang, Zheng; Zhao, Man; Xu, Jiecheng; Huang, Liwu; Zhu, Gongming; Bao, Guangjun; Sun, Wangsheng; Hong, Liang; Wang, Rui. And the article was published in Organic Letters in 2019. Computed Properties of C8H6FN The author mentioned the following in the article:

The switchable skeletal rearrangement for the construction of amino indanones and tetrahydroisoquinolones frameworks had been developed. In the presence of a chiral phosphoric acid catalyst, the reaction gave the amino indanones in high yields and good to excellent ee (85-98%), while the methoxyl substituent at the 5-position of dihydroisobenzofuran acetal selectively gave isoquinolinones products in good to excellent ee (46-98%). Furthermore, DFT calculations were performed to explain the regioselectivity of the switchable transformation pathways. The experimental process involved the reaction of 5-Fluoro-1H-indole(cas: 399-52-0Computed Properties of C8H6FN)

5-Fluoro-1H-indole(cas: 399-52-0) is a member of aromaticfluorinated building blocks. Fluorine-containing aromatics have been incorporated into crop-protection chemicals (herbicides, insecticides, fungicides). Liquid crystals, positron emission tomography, and imaging systems represent new areas where fluoroaromatics and fluoroheterocyclics have gained attention.Computed Properties of C8H6FN

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

The author of 《Halogen Bond-Catalyzed Friedel-Crafts Reactions of Aldehydes and Ketones Using a Bidentate Halogen Bond Donor Catalyst: Synthesis of Symmetrical Bis(indolyl)methanes》 were Liu, Xuelei; Ma, Shuang; Toy, Patrick H.. And the article was published in Organic Letters in 2019. SDS of cas: 120-72-9 The author mentioned the following in the article:

The use of a halogen bond donor to catalyze Friedel-Crafts reactions of indoles with a range of aldehydes and ketones to directly produce bis(indolyl)methanes, including the natural products arsindoline A, arundine, trisindoline, and vibrindole A, is reported. The bidentate catalyst used in these reactions proved to be more effective than a monondentate analog, a thiourea commonly used as an organocatalyst, and even a trityl cation that has been used previously in the synthesis of bis(indolyl)methanes.1H-Indole(cas: 120-72-9SDS of cas: 120-72-9) was used in this study.

1H-Indole(cas: 120-72-9) belongs to indole. 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. 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.SDS of cas: 120-72-9

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

《Intestinal microbiota-derived tryptophan metabolites are predictive of Ah receptor activity》 was written by Dong, Fangcong; Hao, Fuhua; Murray, Iain A.; Smith, Philip B.; Koo, Imhoi; Tindall, Alyssa M.; Kris-Etherton, Penny M.; Gowda, Krishne; Amin, Shantu G.; Patterson, Andrew D.; Perdew, Gary H.. Application In Synthesis of 1H-Indole And the article was included in Gut Microbes in 2020. The article conveys some information:

Commensal microbiota-dependent tryptophan catabolism within the gastrointestinal tract is known to exert profound effects upon host physiol., including the maintenance of epithelial barrier and immune function. Using GC/MS and LC/MS platforms, quantification of these novel AHR activators, along with previously established AHR-activating tryptophan metabolites, was achieved, providing a relative order of abundance. Using physiol. relevant concentrations and quant. gene expression analyses, the relative efficacy of these tryptophan metabolites with regard to mouse or human AHR activation potential is examined These data reveal indole, 2-oxindole, indole-3-acetic acid and kynurenic acid as the dominant AHR activators in mouse cecal contents and human stool from participants on a controlled diet. Here we provide the first documentation of the relative abundance and AHR activation potential of a panel of microbiota-derived tryptophan metabolites. Furthermore, these data reveal the human AHR to be more sensitive, at physiol. relevant concentrations, to tryptophan metabolite activation than mouse AHR. Addnl., correlation analyses indicate a relationship linking major tryptophan metabolite abundance with AHR activity, suggesting these cecal/fecal metabolites represent biomarkers of intestinal AHR activity.1H-Indole(cas: 120-72-9Application In Synthesis of 1H-Indole) was used in this study.

1H-Indole(cas: 120-72-9) belongs to indole. 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. 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.Application In Synthesis of 1H-Indole

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

Application of 399-52-0In 2021 ,《Protein-observed 19F NMR of LecA from Pseudomonas aeruginosa》 appeared in Glycobiology. The author of the article were Shanina, Elena; Siebs, Eike; Zhang, Hengxi; Silva, Daniel Varon; Joachim, Ines; Titz, Alexander; Rademacher, Christoph. The article conveys some information:

The carbohydrate-binding protein LecA (PA-IL) from Pseudomonas aeruginosa plays an important role in the formation of biofilms in chronic infections. Development of inhibitors to disrupt LecA-mediated biofilms is desired but it is limited to carbohydrate-based ligands. Moreover, discovery of drug-like ligands for LecA is challenging because of its weak affinities. Therefore, we established a protein-observed 19F (PrOF) NMR (NMR) to probe ligand binding to LecA. LecA was labeled with 5-fluoroindole to incorporate 5-fluorotryptophanes and the resonances were assigned by site-directed mutagenesis. This incorporation did not disrupt LecA preference for natural ligands, Ca2+ and D-galactose (D-Gal). Following NMR perturbation of W42, which is located in the carbohydrate-binding region of LecA, allowed to monitor binding of low-affinity ligands such as N-acetyl D-galactosamine (D-GalNAc, Kd = 780 ± 97 μM). Moreover, PrOF NMR titration with glycomimetic of LecA p-nitrophenyl β-D-galactoside (pNPGal, Kd = 54 ± 6 μM) demonstrated a 6-fold improved binding of D-Gal proving this approach to be valuable for ligand design in future drug discovery campaigns that aim to generate inhibitors of LecA.5-Fluoro-1H-indole(cas: 399-52-0Application of 399-52-0) was used in this study.

5-Fluoro-1H-indole(cas: 399-52-0) is a member of aromaticfluorinated building blocks. Depending on which substituents are present, fluoroaromatic intermediates can be converted into fluorinated or fluorine-free commercial end products.Fluorine-containing aromatics have been incorporated into drugs (hypnotics, tranquilizers, antiinflammatory agents, analgesics, antibacterials).Application of 399-52-0

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

Application In Synthesis of 5-Fluoro-1H-indoleIn 2021 ,《Palladium-Catalyzed Direct and Specific C-7 Acylation of Indolines with 1,2-Diketones》 appeared in Organic Letters. The author of the article were Xie, Guilin; Zhao, Yuhan; Cai, Changqun; Deng, Guo-Jun; Gong, Hang. The article conveys some information:

Herein, a palladium-catalyzed direct and specific C-7 acylation of indolines in the presence of an easily removed directing group was developed. This strategy usually considered as a practical strategy for the preparation of acylated indoles because indoline can be easily converted to indole under oxidation conditions. In particular, these strategy greatly improved the alkacylation yield of indolines for which only an unsatisfactory yield could be achieved in the previous studies. Furthermore, the reaction can be scaled up to gram level in the standard reaction conditions with a much lower palladium loading (1 mol %). The experimental process involved the reaction of 5-Fluoro-1H-indole(cas: 399-52-0Application In Synthesis of 5-Fluoro-1H-indole)

5-Fluoro-1H-indole(cas: 399-52-0) is a member of aromaticfluorinated building blocks. Depending on which substituents are present, fluoroaromatic intermediates can be converted into fluorinated or fluorine-free commercial end products.Fluorine-containing aromatics have been incorporated into drugs (hypnotics, tranquilizers, antiinflammatory agents, analgesics, antibacterials).Application In Synthesis of 5-Fluoro-1H-indole

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