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Devi, N. Saritha et al. published their research in Journal of Pharmaceutical Sciences and Research in 2019 | CAS: 112656-95-8

7-Nitroindoline-2,3-dione (cas: 112656-95-8) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. In addition to indole, the strain-release chemistry worked for numerous substrates including amines, alcohols, thiols, carboxylic acids, imidazoles, and pyrazoles.Formula: C8H4N2O4

Synthesis and screening of 3-[N-substituted phenylamino-2-phenyl-4-thiazolidinon-5-ylidene]-1,3-dihydro-indol-2-ones for in vivo anti-inflammatory activity was written by Devi, N. Saritha;Srinivas, B.;Sarangapani, Manda. And the article was included in Journal of Pharmaceutical Sciences and Research in 2019.Formula: C8H4N2O4 This article mentions the following:

A novel 3-[N-substituted phenylamino-2-phenyl-4-thiazolidinon-5-ylidene]-1,3-dihydro-indol-2-ones I (R = H, 5-F, 7-Me) was synthesized by condensation of isatins II with 2-phenyl-3-(phenylamino)-1,3-thiazolidin-4-one. The compounds I (5-Cl, 7-Cl, 5-F, 5-Br, 5,6-Cl₂, 5-OH) evaluated for in vivo anti-inflammatory activity. The compound I (R = 5,6-Cl₂) showed more in vivo anti-inflammatory activity with 72.5% of inhibition among test compounds The compounds I (R = 5-F, 5Cl, 5-Br, 7-Cl,5-OH) were next in the order of exhibiting in vivo anti-inflammatory activity with 65.75, 63.0, 61.25, 52.5 and 51.25% resp., when compared to standard drug Indomethacin with 73.7% of inhibition. In the experiment, the researchers used many compounds, for example, 7-Nitroindoline-2,3-dione (cas: 112656-95-8Formula: C8H4N2O4).

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

Gortner, Willis A. et al. published their research in Botanical Gazette (Chicago) in 1969 | CAS: 6639-06-1

3-(1H-Indol-1-yl)propanoic acid (cas: 6639-06-1) 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. 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: C11H11NO2

Relation of chemical structure to plant growth-regulator activity in the pineapple plant. V. Post-harvest delay of senescence of pineapple fruit was written by Gortner, Willis A.;Leeper, Robert W.. And the article was included in Botanical Gazette (Chicago) in 1969.Formula: C11H11NO2 This article mentions the following:

The effects of 369 compounds, including 94 phenoxyacetic acids, 43 other phenoxy acids, 23 phenylacetic acids, 15 hydrocinnamic acids, 9 benzoic acids, 7 salicylic acids, 48 naphthalene derivatives, 22 indole acids, 5 hydrazine derivatives, and 8 cinnamic acids, for postharvest delay of senescence of pineapple fruit (Ananas comosus) were determined Seventy-six of the compounds were active, and 27 were highly active in delaying senescence. In the phenoxyacetic acid series, high activity was obtained from some halogen-substituted acids but not generally from Me-substituted acids. In the phenoxy-α-propionic acid series, high activity was not observed for a number of halogen- and Me-substituted acids. None of the substituted phenoxy acids other than HOAc and α- propionic showed even moderate activity. An appreciable number of Cl-substituted phenylacetic acids and several benzoic acids showed activity. None of the phenylalkylcarboxylic acids other than HOAc showed even moderate activity. None of the salicylic acid, phthalic acids, or phthalamic acids showed any activity. All hydrazine derivatives were inactive. In the experiment, the researchers used many compounds, for example, 3-(1H-Indol-1-yl)propanoic acid (cas: 6639-06-1Formula: C11H11NO2).

Abbott, Jason R. et al. published their research in Journal of Medicinal Chemistry in 2018 | CAS: 827-01-0

5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Safety of 5-Chloroindole-3-carboxaldehyde

Discovery of Aminopiperidine Indoles That Activate the Guanine Nucleotide Exchange Factor SOS1 and Modulate RAS Signaling was written by Abbott, Jason R.;Hodges, Timothy R.;Daniels, R. Nathan;Patel, Pratiq A.;Kennedy, J. Phillip;Howes, Jennifer E.;Akan, Denis T.;Burns, Michael C.;Sai, Jiqing;Sobolik, Tammy;Beesetty, Yugandhar;Lee, Taekyu;Rossanese, Olivia W.;Phan, Jason;Waterson, Alex G.;Fesik, Stephen W.. And the article was included in Journal of Medicinal Chemistry in 2018.Safety of 5-Chloroindole-3-carboxaldehyde This article mentions the following:

Indole-substituted tryptophan amides such as I were prepared through optimization of aminopiperidine-substituted indoles as activators of the guanine nucleotide exchange factor (GEF) son of sevenless homolog 1 (SOS1) for use in modulating RAS signaling and thus as potential antitumor agents. Substitution patterns on the indole nucleus, the pendant amino acid moiety, and the linker unit connecting these two fragments were modified to determine structure-activity relations for the SOS1-mediated activation of nucleotide exchange. Effective compounds such as I activated the nucleotide exchange process at sub-micromolar concentrations in vitro (IC₅₀ for I = 0.8 ± 0.36 μM), increased levels of active RAS-GTP in HeLa cells, and elicited signaling changes in the mitogen-activated protein kinase/extracellular regulated kinase (MAPK/ERK) pathway, resulting in a decrease in pERK1/2^T202/Y204 protein levels at higher compound concentrations The structures of selected compounds bound to the ternary complex of RAS, SOS1, and RAS were determined by X-ray crystallog. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Safety of 5-Chloroindole-3-carboxaldehyde).

Raj, I. Victor Paul et al. published their research in Acta Chimica Slovenica in 2010 | CAS: 150560-58-0

5-Isopropylindoline-2,3-dione (cas: 150560-58-0) 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. In addition to indole, the strain-release chemistry worked for numerous substrates including amines, alcohols, thiols, carboxylic acids, imidazoles, and pyrazoles.Recommanded Product: 150560-58-0

H-β zeolite, an efficient reusable catalyst for one-pot synthesis of isatins from anilines was written by Raj, I. Victor Paul;Shaikh, Tanveer Mahamadali;Sudalai, Arumugam. And the article was included in Acta Chimica Slovenica in 2010.Recommanded Product: 150560-58-0 This article mentions the following:

The authors described a simple and highly efficient procedure for the single-step preparation of isatins from the com. available anilines using H-β zeolite as a truly heterogeneous catalyst. H-β zeolite is readily separated from the reaction mixture by simple filtration and was reused several times without considerable loss of activity. In the experiment, the researchers used many compounds, for example, 5-Isopropylindoline-2,3-dione (cas: 150560-58-0Recommanded Product: 150560-58-0).

See, Cheng Shang et al. published their research in European Journal of Medicinal Chemistry in 2018 | CAS: 827-01-0

5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) 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.Electric Literature of C9H6ClNO

Discovery of the cancer cell selective dual acting anti-cancer agent (Z)-2-(1H-indol-3-yl)-3-(isoquinolin-5-yl)acrylonitrile (A131) was written by See, Cheng Shang;Kitagawa, Mayumi;Liao, Pei-Ju;Lee, Kyung Hee;Wong, Jasmine;Lee, Sang Hyun;Dymock, Brian W.. And the article was included in European Journal of Medicinal Chemistry in 2018.Electric Literature of C9H6ClNO This article mentions the following:

Selective targeting of cancer cells over normal cells is a key objective of targeted therapy. However few approaches achieve true mechanistic selectivity resulting in debilitating side effects and dose limitation. In this work we describe the discovery of A131 (4a), a new agent with an unprecedented dual mechanism of action targeting both mitosis and autophagy. Compound 4a was first identified in a phenotypic screen in which HeLa cells treated with 4a manifested mitotic arrest along with formation of multiple vesicles. Further investigations showed that 4a causes an increase in mitotic marker pH3 and autophagy marker LC3. Importantly 4a induces cell death in cancer cells while sparing normal cells which regrow after 4a is removed. Dual activities against pH3 and LC3 markers are required for cancer cell selectivity. An extensive SAR investigation confirmed 4a as the optimal dual inhibitor with potency against a panel of 30 cancer cell lines (average antiproliferative GI₅₀ 1.5μM). In a mouse model of paclitaxel-resistant colon cancer, 4a showed 74% tumor growth inhibition when administered at a dose of 20mg/kg IP twice a day. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Electric Literature of C9H6ClNO).

Alexander, Juliana R. et al. published their research in Organic Letters in 2021 | CAS: 3484-23-9

2-Methyl-6-nitro-1H-indole (cas: 3484-23-9) 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.Safety of 2-Methyl-6-nitro-1H-indole

Silver Mediated Banert Cascade with Carbon Nucleophiles was written by Alexander, Juliana R.;Kevorkian, Paul V.;Topczewski, Joseph J.. And the article was included in Organic Letters in 2021.Safety of 2-Methyl-6-nitro-1H-indole This article mentions the following:

The Banert cascade of propargylic azides was promoted by simple silver salts and the triazafulvene intermediate can be intercepted by carbon nucleophiles. Various indoles (>25 examples, up to 92% yield) and electron-rich heterocycles were effective. The Mayr nucleophilicity parameter (N) was found to correlate to the reaction efficiency, which enabled the formation of Csp³-Csp² and Csp³-Csp³ bonds under otherwise identical conditions from structurally dissimilar nucleophiles. In the experiment, the researchers used many compounds, for example, 2-Methyl-6-nitro-1H-indole (cas: 3484-23-9Safety of 2-Methyl-6-nitro-1H-indole).

Nosova, E. V. et al. published their research in Russian Chemical Bulletin in 2011 | CAS: 774-47-0

5,6-Difluoroindoline-2,3-dione (cas: 774-47-0) 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.Recommanded Product: 774-47-0

Fluorine-containing quinoline and quinoxaline styryl derivatives: synthesis and photophysical properties was written by Nosova, E. V.;Trashakhova, T. V.;Ustyugov, V. S.;Mochul’skaya, N. N.;Valova, M. S.;Lipunova, G. N.;Charushin, V. N.. And the article was included in Russian Chemical Bulletin in 2011.Recommanded Product: 774-47-0 This article mentions the following:

(E)-2-Styryl-substituted 6,7-difluoroquinolines, e.g., I, and quinoxalines, e.g., II, were synthesized by the condensation of the corresponding 2-methylbenzazines with aromatic aldehydes. Photoluminescence of the synthesized 6,7-difluoro-2-styrylbenzazines was studied. In the experiment, the researchers used many compounds, for example, 5,6-Difluoroindoline-2,3-dione (cas: 774-47-0Recommanded Product: 774-47-0).

Lin, Dian-Zhao et al. published their research in Organic Letters in 2019 | CAS: 827-01-0

5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) 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.Application In Synthesis of 5-Chloroindole-3-carboxaldehyde

Synthesis of 3-Formylindoles via Electrochemical Decarboxylation of Glyoxylic Acid with an Amine as a Dual Function Organocatalyst was written by Lin, Dian-Zhao;Huang, Jing-Mei. And the article was included in Organic Letters in 2019.Application In Synthesis of 5-Chloroindole-3-carboxaldehyde This article mentions the following:

A method for 3-formylation of indoles has been developed through electrochem. decarboxylation of glyoxylic acid with the amine as a dual function organocatalyst. The amine facilitated both the electrochem. decarboxylation and the nucleophilic reaction efficiently, whose loading can be as low as 1 mol %. This protocol has a broad range of functional group tolerance under ambient conditions. The gram-scale experiment has shown great potential in the synthetic application of this strategy. 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).

Xiang, Jiachen et al. published their research in Organic & Biomolecular Chemistry in 2015 | 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. 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.Safety of 6-Nitro-1H-indole

One-pot total synthesis of streptindole, arsindoline B and their congeners through tandem decarboxylative deaminative dual-coupling reaction of amino acids with indoles was written by Xiang, Jiachen;Wang, Jungang;Wang, Miao;Meng, Xianggao;Wu, Anxin. And the article was included in Organic & Biomolecular Chemistry in 2015.Safety of 6-Nitro-1H-indole This article mentions the following:

This paper described a decarboxylative deaminative dual-coupling reaction of amino acids with indoles to afford BIM (bis(indolyl)methane) scaffolds and its further application to the one-pot total synthesis of natural products. This method featured a stimulating example of activating amino acids in one pot as multi-carbon building blocks for transformation into final targets which are equipped with amino acid side chain backbones. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4Safety of 6-Nitro-1H-indole).

Mahajan, Y. R. et al. published their research in Science of Synthesis in 2005 | CAS: 150560-58-0

5-Isopropylindoline-2,3-dione (cas: 150560-58-0) 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. 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

Introduction [Synthesis of amides] was written by Mahajan, Y. R.;Weinreb, S. M.. And the article was included in Science of Synthesis in 2005.Category: indole-building-block This article mentions the following:

A review which constitutes an overview of a whole volume which covers the synthesis of compounds containing an amide moiety, including peptides and lactams. These compounds were divided into groups depending on the type of amide and nature of the substituents around the amide functionality. In the experiment, the researchers used many compounds, for example, 5-Isopropylindoline-2,3-dione (cas: 150560-58-0Category: indole-building-block).