Staahl, Marianne et al. published their research in Journal of the American Chemical Society in 1991 | CAS: 2382-80-1

Ethyl acetyl-L-tryptophanate (cas: 2382-80-1) 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.Application of 2382-80-1

Induced stereo- and substrate selectivity of bioimprinted 伪-chymotrypsin in anhydrous organic media was written by Staahl, Marianne;Jeppsson-Wistrand, Ulla;Maansson, Mats Olle;Mosbach, Klaus. And the article was included in Journal of the American Chemical Society in 1991.Application of 2382-80-1 This article mentions the following:

Chymotrypsin bioimprinted with N-acetyl-D-tryptophan was shown to also accept N-acetyl-D-tryptophan as a substrate for Et ester formation in anhydrous organic media, probably by obtaining a new conformation. Small additions of water however, perturbed the new conformation of the enzyme, returning the enzyme to a structure with more native-like properties, i.e., L specificity. Chymotrypsin bioimprinted with the N-acetyl derivatives of the aromatic amino acids, tryptophan, tyrosine, and phenylalanine, expressed, in the same synthetic reaction, leading to the corresponding Et esters, high specificity for the resp. amino acid used during bioimprinting. In the experiment, the researchers used many compounds, for example, Ethyl acetyl-L-tryptophanate (cas: 2382-80-1Application of 2382-80-1).

Ethyl acetyl-L-tryptophanate (cas: 2382-80-1) 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.Application of 2382-80-1

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

Lawson, William B. et al. published their research in Journal of Organic Chemistry in 1961 | CAS: 2971-31-5

2-(2-Oxoindolin-3-yl)acetic acid (cas: 2971-31-5) belongs to indole derivatives. Indole produced by Proteus, Pseudomonas, Escherichia and other species was shown to be a growth promoting factor in Arabidopsis thaliana.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Application of 2971-31-5

Simple method for the preparation of oxindole acetic and propionic acids from the parent indoles was written by Lawson, William B.;Witkop, Bernhard. And the article was included in Journal of Organic Chemistry in 1961.Application of 2971-31-5 This article mentions the following:

The smooth hydrogenolysis of 5-bromodioxindole-3-propionic acid lactone (I) to oxindole-3-propionic acid, C6H4.NH.CO.CH(CH2)nCO2H (II) (n = 2) (III), was adapted to provide a simple method of direct conversion of indoles to oxindoles. Indole-3-propionic acid (3.0 g.) in 100 ml. ice-cold 50% AcOH swirled 5 min. with gradual addition of 5.65 g. (H2CCO)2NBr, the mixture kept 15 min. at 20掳, hydrogenated 18 hrs. with 1 g. 10% Pd-C, the filtered solution evaporated, and the residue crystallized from H2O (C) yielded 49% III, m. 165-7掳, identical with a sample prepared by hydrogenolysis of I. Indole-3-acetic acid (1.0 g.) in 50 ml. ice-cold 50% AcOH kept 1 hr. at 20掳 with 4.85 ml. AcOH containing 1.83 g. Br, the mixture hydrogenated 17 hrs. with 0.5 g. 10% Pd-C, the residue on evaporation of the filtered solution diluted with 15 ml. H2O, extracted with EtOAc, the dried extract (Na2SO4) evaporated, and the residue crystallized from Et2O-petr. ether (b. 50-60掳) gave 686 mg. material, m. 100-40掳, recrystallized from Me2CO-C6H6 and dried 45 min. in vacuo at 55掳 to yield 49% II (n = 1), m. 140-2掳, characterized by smooth acid-catalyzed conversion to 3,4-dihydro-2(1H)-quinolone-4-carboxylic acid, m. 210-14掳. In the experiment, the researchers used many compounds, for example, 2-(2-Oxoindolin-3-yl)acetic acid (cas: 2971-31-5Application of 2971-31-5).

2-(2-Oxoindolin-3-yl)acetic acid (cas: 2971-31-5) belongs to indole derivatives. Indole produced by Proteus, Pseudomonas, Escherichia and other species was shown to be a growth promoting factor in Arabidopsis thaliana.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Application of 2971-31-5

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

Wen, Zhonghang et al. published their research in European Journal of Medicinal Chemistry in 2017 | CAS: 10601-19-1

5-Methoxy-1H-indole-3-carbaldehyde (cas: 10601-19-1) 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. In addition to indole, the strain-release chemistry worked for numerous substrates including amines, alcohols, thiols, carboxylic acids, imidazoles, and pyrazoles.Quality Control of 5-Methoxy-1H-indole-3-carbaldehyde

Novel 3′,5′-diprenylated chalcones inhibited the proliferation of cancer cells in vitro by inducing cell apoptosis and arresting cell cycle phase was written by Wen, Zhonghang;Zhang, Yongqiang;Wang, Xinghui;Zeng, Xiaoping;Hu, Zhanxing;Liu, Yi;Xie, Yuxin;Liang, Guangyi;Zhu, Jianguo;Luo, Heng;Xu, Bixue. And the article was included in European Journal of Medicinal Chemistry in 2017.Quality Control of 5-Methoxy-1H-indole-3-carbaldehyde This article mentions the following:

A double Claisen rearrangements synthetic strategy was established for the total synthesis of 4,4′-dimethyl medicagenin (I, compound 6c). A series of its analogs also were prepared, including two novel 3′,5′-diprenylated chalcones, in which ring B was replaced by azaheterocycle. The structures of the twenty-two newly synthesized compounds were confirmed by 1H NMR, 13C NMR and ESI-MS. In vitro, the cytotoxicity of the target compounds was evaluated using cancer cells. Noticeably, compound 10 (II) exhibited broad-spectrum cytotoxicity on PC3 prostate cancer cells, MDA-MB-231 breast cancer cells (MDA), HEL and K562 erythroleukemia cells with IC50 values of 2.92, 3.14, 1.85 and 2.64 渭M, resp. Further studies indicated that compound 10 induced apoptosis and arrested the cell cycle phase of the above mentioned four cancer cell lines. By contrast, compound 6g (III) selectively displayed potent inhibitory activity against the proliferation of HEL cells with an IC50 value of 4.35 渭M. Compound 6g slightly induced apoptosis and arrested cell cycle phase of HEL cells. Preliminary structure-activity relationship studies indicated that, in all cancer cell lines evaluated, the 3-pyridinyl group was essential for cytotoxicity. In the experiment, the researchers used many compounds, for example, 5-Methoxy-1H-indole-3-carbaldehyde (cas: 10601-19-1Quality Control of 5-Methoxy-1H-indole-3-carbaldehyde).

5-Methoxy-1H-indole-3-carbaldehyde (cas: 10601-19-1) 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. In addition to indole, the strain-release chemistry worked for numerous substrates including amines, alcohols, thiols, carboxylic acids, imidazoles, and pyrazoles.Quality Control of 5-Methoxy-1H-indole-3-carbaldehyde

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

Merkt, Franziska K. et al. published their research in Chemistry – A European Journal in 2021 | CAS: 2521-13-3

5-Methoxy-1-methyl-1H-indole (cas: 2521-13-3) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Related Products of 2521-13-3

Fluorescent Indolo[3,2-a]phenazines against Toxoplasma gondii: Concise Synthesis by Gold-Catalyzed Cycloisomerization with 1,2-Silyl Migration and ipso-Iodination Suzuki Sequence was written by Merkt, Franziska K.;Mazzone, Flaminia;Sazzadeh, Shabnam Shaneh;Bonda, Lorand;Hinz, Larissa K. E.;Gruber, Irina;Buchholz, Karin;Janiak, Christoph;Pfeffer, Klaus;Mueller, Thomas J. J.. And the article was included in Chemistry – A European Journal in 2021.Related Products of 2521-13-3 This article mentions the following:

A gold-catalyzed cycloisomerization of 2-indolyl-3-[(trimethylsilyl)ethynyl)]quinoxalines with concomitant 1,2-silyl shift forms 6-(trimethylsilyl)indolo[3,2-a]phenazines in moderate to excellent yield. These silylated heterocycles are readily transformed into 6-aryl-indolo[3,2-a]phenazines in moderate to good yield by one-pot ipso-iodination Suzuki coupling. The title compounds represent a novel type of tunable luminophore. Structure-property relationships for 6-aryl-indolo[3,2-a]phenazines obtained from Hammett correlations with 蟽p+ substituent parameters indicate that emission maxima, Stokes shifts, and fluorescence quantum yields can be fine-tuned by the remote para-aryl substituent. Furthermore, indolo[3,2-a]phenazines were found to exhibit interesting activities against medically relevant pathogens such as the Apicomplexa parasite Toxoplasma gondii with an IC50 of up to 0.67卤0.13渭M. Thus, these compounds are promising candidates for novel anti-parasitic therapies. In the experiment, the researchers used many compounds, for example, 5-Methoxy-1-methyl-1H-indole (cas: 2521-13-3Related Products of 2521-13-3).

5-Methoxy-1-methyl-1H-indole (cas: 2521-13-3) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Related Products of 2521-13-3

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

Karar, Monaj et al. published their research in Journal of Molecular Liquids in 2021 | CAS: 442-51-3

7-Methoxy-1-methyl-9H-pyrido[3,4-b]indole (cas: 442-51-3) belongs to indole derivatives. Indole produced by Proteus, Pseudomonas, Escherichia and other species was shown to be a growth promoting factor in Arabidopsis thaliana. 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.Product Details of 442-51-3

Dual macrocyclic chemical input based highly protective molecular keypad lock using fluorescence in solution phase: A new type approach was written by Karar, Monaj;Paul, Provakar;Mistri, Rajib;Majumdar, Tapas;Mallick, Arabinda. And the article was included in Journal of Molecular Liquids in 2021.Product Details of 442-51-3 This article mentions the following:

Generally, the non-bonding interactions provide the stability to the host-guest complexes without affecting the mol. identity of macrocyclic host and guest (probe) mols. As a result, macrocyclic-based systems are far more deserving candidates over the ionic systems, as the chance of chem. bleaching is suitably dodged due to the weaker non-bonding interaction. The present article intends to highlight an unconventional and completely innovative designing strategy to validate the operation of a highly protective opto-chem. keypad lock driven by the macrocyclics. Herein, we have utilized the reversible photoswitching phenomenon between two prototropic forms (cationic and neutral) of Harmine (HM) regulated by the dual macrocyclic components, CTAB and 尾-CD. Most interestingly, methodol. provides the choice of the selection of emission detector one at a time between two available emission channels (416 and 365 nm), which have been considered as the “optical inputs”. Substantial emission intensities of the probe at the resp. emission channels have been treated as the “optical outputs”. On the basis of a cautious literature survey, we anticipate that, this kind of designing for a highly protective opto-chem. security device driven by the macrocyclic “chem. inputs” has never explored yet. In the experiment, the researchers used many compounds, for example, 7-Methoxy-1-methyl-9H-pyrido[3,4-b]indole (cas: 442-51-3Product Details of 442-51-3).

7-Methoxy-1-methyl-9H-pyrido[3,4-b]indole (cas: 442-51-3) belongs to indole derivatives. Indole produced by Proteus, Pseudomonas, Escherichia and other species was shown to be a growth promoting factor in Arabidopsis thaliana. 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.Product Details of 442-51-3

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

Merour, Jean Yves et al. published their research in Tetrahedron Letters in 1992 | CAS: 16800-68-3

1-Acetylindolin-3-one (cas: 16800-68-3) 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. 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.Electric Literature of C10H9NO2

Arylation of 3-oxo-2,3-dihydroindoles with aryllead triacetates was written by Merour, Jean Yves;Chichereau, Lucien;Finet, Jean Pierre. And the article was included in Tetrahedron Letters in 1992.Electric Literature of C10H9NO2 This article mentions the following:

Arylation of 2-alkoxycarbonyl-3-oxo-2,3-dihydroindoles I (R = H, Me, COMe; R1 = CO2Me, CO2Et; R2 = H) with aryllead (IV) triacetates II (R3 = H, OMe) leads selectively to 2-alkoxycarbonyl-2-aryl-3-oxo-2,3-dihydroindoles III. Direct selective C-arylation of 1-substituted-3-oxo-2,3-dihydroindoles I (R = COMe, SO2Ph; R1 = H, Me, Ph; R2 = H, Me, OMe) with II (R3 = OMe) affords the corresponding 1-substituted-2-aryl-3-oxo-2,3-dihydroindoles III. In the experiment, the researchers used many compounds, for example, 1-Acetylindolin-3-one (cas: 16800-68-3Electric Literature of C10H9NO2).

1-Acetylindolin-3-one (cas: 16800-68-3) 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. 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.Electric Literature of C10H9NO2

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

Chapkin, Robert S. et al. published their research in Molecular Nutrition & Food Research in 2021 | CAS: 244-63-3

9H-Pyrido[3,4-b]indole (cas: 244-63-3) 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.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Related Products of 244-63-3

Role of the Aryl Hydrocarbon Receptor (AhR) in Mediating the Effects of Coffee in the Colon was written by Chapkin, Robert S.;Davidson, Laurie A.;Park, Hyejin;Jin, Un-Ho;Fan, Yang-Yi;Cheng, Yating;Hensel, Martha E.;Landrock, Kerstin K.;Allred, Clinton;Menon, Rani;Klemashevich, Cory;Jayaraman, Arul;Safe, Stephen. And the article was included in Molecular Nutrition & Food Research in 2021.Related Products of 244-63-3 This article mentions the following:

This study investigates the mechanism of action and functional effects of coffee extracts in colonic cells, on intestinal stem cell growth, and inhibition of dextran sodium sulfate (DSS)-induced intestinal barrier damage in mice. Aqueous coffee extracts induced Ah receptor (AhR) -responsive CYP1A1, CYP1B1, and UGT1A1 gene expression in colon-derived Caco2 and YAMC cells. Tissue-specific AhR knockout (AhRf/f x Lgr5-GFP-CreERT2 x Villin-Cre), wild-type (Lgr5-CreERT2 x Villin-Cre) mice are sources of stem cell enriched organoids and both coffee extracts and norharman, an AhR-active component of these extracts inhibited stem cell growth. Coffee extracts also inhibit DSS-induced damage to intestinal barrier function and DSS-induced mucosal inflammatory genes such as IL-6 and TGF-尾1 in wild-type (AhR+/+) but not AhR-/- mice. In contrast, coffee does not exhibit protective effects in intestinal-specific AhR knockout mice. Coffee extracts also enhanced overall formation of AhR-active microbial metabolites. In colon-derived cells and in the mouse intestine, coffee induced several AhR-dependent responses including gene expression, inhibition of intestinal stem cell-enriched organoid growth, and inhibition of DSS-induced intestinal barrier damage. We conclude that the anti-inflammatory effects of coffee in the intestine are due, in part, to activation of AhR signaling. In the experiment, the researchers used many compounds, for example, 9H-Pyrido[3,4-b]indole (cas: 244-63-3Related Products of 244-63-3).

9H-Pyrido[3,4-b]indole (cas: 244-63-3) 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.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Related Products of 244-63-3

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

Kapish, Kapoor et al. published their research in World Journal of Pharmaceutical Research in 2020 | CAS: 160970-54-7

(-)-1-(3-Hydroxypropyl)-5-[(2R)-2-[[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl]amino]propyl]-2,3-di-hydro-1H-indole-7-carboxamide (cas: 160970-54-7) 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.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Application In Synthesis of (-)-1-(3-Hydroxypropyl)-5-[(2R)-2-[[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl]amino]propyl]-2,3-di-hydro-1H-indole-7-carboxamide

Molecular docking study on approved drugs against treatment of SARS-CoV-2 pandemic: a drug repurposing study was written by Kapish, Kapoor;Aman, Mourya;Yuvraj, Patidar;Shoyab, Khan Md.;Nayan, Shroff;Aayushi, Kavishwar. And the article was included in World Journal of Pharmaceutical Research in 2020.Application In Synthesis of (-)-1-(3-Hydroxypropyl)-5-[(2R)-2-[[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl]amino]propyl]-2,3-di-hydro-1H-indole-7-carboxamide This article mentions the following:

COVID-19(corona virus disease -19) is a viral flu which is caused by SARS-CoV-2(severe acute respiratory syndrome corona virus 2) has affected more than 1.5 million people around the world. Currently there are 19 different ways to tackle this pandemic approved by USFDA, one of it is drug repurposing or positioning of current existing drugs. In this study more than 1800 mols. approved by the USFDA were chosen for the mol. docking studies. These mols. were docked on PDB code; 6LU7 (The crystal structure of COVID-19 main protease in complex with an inhibitor N3) using Molegro virtual docker version 6.0.1 . The study helped in identifying HITS and further in vitro and in-vivo studies of the selected HITS can be studied for their therapeutic potential in treating COVID-19. In the experiment, the researchers used many compounds, for example, (-)-1-(3-Hydroxypropyl)-5-[(2R)-2-[[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl]amino]propyl]-2,3-di-hydro-1H-indole-7-carboxamide (cas: 160970-54-7Application In Synthesis of (-)-1-(3-Hydroxypropyl)-5-[(2R)-2-[[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl]amino]propyl]-2,3-di-hydro-1H-indole-7-carboxamide).

(-)-1-(3-Hydroxypropyl)-5-[(2R)-2-[[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl]amino]propyl]-2,3-di-hydro-1H-indole-7-carboxamide (cas: 160970-54-7) 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.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Application In Synthesis of (-)-1-(3-Hydroxypropyl)-5-[(2R)-2-[[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl]amino]propyl]-2,3-di-hydro-1H-indole-7-carboxamide

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

Matheson, Christopher J. et al. published their research in ACS Chemical Biology in 2016 | CAS: 34387-89-8

N-(tert-Butoxycarbonylamino)phthalimide (cas: 34387-89-8) 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. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Safety of N-(tert-Butoxycarbonylamino)phthalimide

A WEE1 Inhibitor Analog of AZD1775 Maintains Synergy with Cisplatin and Demonstrates Reduced Single-Agent Cytotoxicity in Medulloblastoma Cells was written by Matheson, Christopher J.;Venkataraman, Sujatha;Amani, Vladimir;Harris, Peter S.;Backos, Donald S.;Donson, Andrew M.;Wempe, Michael F.;Foreman, Nicholas K.;Vibhakar, Rajeev;Reigan, Philip. And the article was included in ACS Chemical Biology in 2016.Safety of N-(tert-Butoxycarbonylamino)phthalimide This article mentions the following:

The current treatment for medulloblastoma includes surgical resection, radiation, and cytotoxic chemotherapy. Although this approach has improved survival rates, the high doses of chemotherapy required for clin. efficacy often result in lasting neurocognitive defects and other adverse events. Therefore, the development of chemosensitizing agents that allow dose reductions of cytotoxic agents, limiting their adverse effects but maintaining their clin. efficacy, would be an attractive approach to treat medulloblastoma. We previously identified WEE1 kinase as a new mol. target for medulloblastoma from an integrated genomic anal. of gene expression and a kinome-wide siRNA screen of medulloblastoma cells and tissue. In addition, we demonstrated that WEE1 prevents DNA damage-induced cell death by cisplatin and that the WEE1 inhibitor AZD1775 displays synergistic activity with cisplatin. AZD1775 was developed as a WEE1 inhibitor from an initial hit from a high-throughput screen. However, given the lack of structure-activity data for AZD1775, we developed a small series of analogs to determine the requirements for WEE1 inhibition and further examine the effects of WEE1 inhibition in medulloblastoma. Interestingly, the compounds that inhibited WEE1 in the same nanomolar range as AZD1775 had significantly reduced single-agent cytotoxicity compared with AZD1775 and displayed synergistic activity with cisplatin in medulloblastoma cells. The potent cytotoxicity of AZD1775, unrelated to WEE1 inhibition, may result in dose-limiting toxicities and exacerbate adverse effects; therefore, WEE1 inhibitors that demonstrate low cytotoxicity could be dosed at higher concentrations to chemosensitize the tumor and potentiate the effect of DNA-damaging agents such as cisplatin. In the experiment, the researchers used many compounds, for example, N-(tert-Butoxycarbonylamino)phthalimide (cas: 34387-89-8Safety of N-(tert-Butoxycarbonylamino)phthalimide).

N-(tert-Butoxycarbonylamino)phthalimide (cas: 34387-89-8) 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. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Safety of N-(tert-Butoxycarbonylamino)phthalimide

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

Ding, Mei et al. published their research in ACS Chemical Biology in 2019 | CAS: 280744-09-4

3-(2,4-Dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione (cas: 280744-09-4) 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. 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). COA of Formula: C19H12Cl2N2O2

A phenotypic screening approach using human Treg cells identified regulators of Forkhead Box p3 expression was written by Ding, Mei;Brengdahl, Johan;Lindqvist, Madelene;Gehrmann, Ulf;Ericson, Elke;von Berg, Stefan;Ripa, Lena;Malhotra, Rajneesh. And the article was included in ACS Chemical Biology in 2019.COA of Formula: C19H12Cl2N2O2 This article mentions the following:

Regulatory T (Treg) cells, expressing the transcription factor forkhead box p3 (FOXP3), are the key cells regulating peripheral autoreactive T lymphocytes by suppressing effector T cells. FOXP3+ Treg cells play essential roles controlling immune responses in autoimmune diseases and cancer. Several clin. approaches (e.g., polyclonal expansion of Treg cells with anti-CD3 and anti-CD28 coated beads in the presence of drugs) are under evaluation. However, expression of FOXP3, recognized as the master regulator of Treg cells, in induced Treg cells have been shown to be instable, and mol. targets involved in regulating FOXP3 expression and Treg cell function have not been well-defined. Thus, new targets directly regulating FOXP3 expression and the expression of its downstream genes (e.g., cytotoxic T-lymphocyte-associated protein 4 (CTLA4)) have the potential to stabilize the Treg cell phenotype and function. This report describes the development of an automated medium-throughput 384-well plate flow cytometry phenotypic assay measuring the protein expression of FOXP3 and CTLA4 in human Treg cells. Screening a library of 4213 structurally diverse compounds allowed us to identify a variety of compounds regulating FOXP3 and CTLA4 expression. Further evaluation of these and related small mols., followed by confirmation using siRNA-mediated gene knockdown, revealed three targets: euchromatic histone-lysine N-methyltransferase (EHMT2) and glycogen synthase kinase 3 alpha/beta (GSK3伪/尾) as potent pos. regulators of FOXP3 expression, and bromodomain and extra-terminal domain (BET) inhibitors as neg. regulators of FOXP3 and CTLA4 expression. These targets have potential implications for establishing novel therapies for autoimmune diseases and cancer. In the experiment, the researchers used many compounds, for example, 3-(2,4-Dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione (cas: 280744-09-4COA of Formula: C19H12Cl2N2O2).

3-(2,4-Dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione (cas: 280744-09-4) 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. 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). COA of Formula: C19H12Cl2N2O2

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