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Tan, Wei et al. published their research in RSC Advances in 2013 | CAS: 774-47-0

5,6-Difluoroindoline-2,3-dione (cas: 774-47-0) belongs to indole derivatives. Indole produced by Proteus, Pseudomonas, Escherichia and other species was shown to be a growth promoting factor in Arabidopsis thaliana. 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 of 774-47-0

Diversity-oriented synthesis of spiro-oxindole-based 2,5-dihydropyrroles via three-component cycloadditions and evaluation on their cytotoxicity was written by Tan, Wei;Zhu, Xiao-Tong;Zhang, Shu;Xing, Gui-Juan;Zhu, Ren-Yi;Shi, Feng. And the article was included in RSC Advances in 2013.Application of 774-47-0 This article mentions the following:

The construction of a spiro-oxindole-based 2,5-dihydropyrrole scaffold I (R = H, Me, Ph, etc.; R¹ = H, 4-Cl, 5-OMe, etc.; R² = Me, Et) with potential bioactivity has been established via an efficient three-component reaction of isatin, amino-ester and alkyne. This protocol represents the first 1,3-dipolar cycloaddition of electron-deficient alkynes with isatin-derived azomethine ylides, providing an easy access to spiro-oxindole-based 2,5-dihydropyrroles with structural diversity in high yields (up to 99%). In addition, the bioscreen of these new spiro-dihydropyrroles has led to the finding of sixteen compounds with promising cytotoxicity to MCF-7 cells. In the experiment, the researchers used many compounds, for example, 5,6-Difluoroindoline-2,3-dione (cas: 774-47-0Application of 774-47-0).

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

Heda, L. C. et al. published their research in E-Journal of Chemistry in 2009 | 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. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Category: indole-building-block

Synthesis and antimicrobial activity of some derivatives of 5-substituted indole dihydropyrimidines was written by Heda, L. C.;Sharma, Rashmi;Pareek, C.;Chaudhari, P. B.. And the article was included in E-Journal of Chemistry in 2009.Category: indole-building-block This article mentions the following:

Haloindole substituted dihydropyrimidines I (R = H, Br, Cl, I; X = O or S) have been prepared via Bignelli reaction of haloformylindoles with urea (or thiourea) and ethylacetoacetate. I were evaluated for their antibacterial and antifungal activity with the min. inhibitory concentration (MIC) determined by micro dilution technique in Mueller-Hinton broth. The MICs were recorded after 24 h of incubation at 37闂? These results are promising, showing these compounds are biol. active. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Category: indole-building-block).

Song, Zhuang et al. published their research in European Journal of Medicinal Chemistry in 2016 | CAS: 150560-58-0

5-Isopropylindoline-2,3-dione (cas: 150560-58-0) belongs to indole derivatives. Indole produced by Proteus, Pseudomonas, Escherichia and other species was shown to be a growth promoting factor in Arabidopsis thaliana. 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: 5-Isopropylindoline-2,3-dione

Design, synthesis, and biological evaluation of (2E)-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)acetate derivatives as anti-proliferative agents through ROS-induced cell apoptosis was written by Song, Zhuang;Chen, Cai-Ping;Liu, Jun;Wen, Xiaoan;Sun, Hongbin;Yuan, Haoliang. And the article was included in European Journal of Medicinal Chemistry in 2016.Recommanded Product: 5-Isopropylindoline-2,3-dione This article mentions the following:

A novel class of (2E)-(2-oxo-1, 2-dihydro-3H-indol-3-ylidene)acetate derivatives I [R = H, Me, Bn; R¹ = OMe, NMe, OC₆H₅, etc.; R² = H, 5-Me, 5-Cl, etc.] and (2-oxo-1,2-dihydro-3H-indol-3-yl)acetate derivatives II [R = H, Me; R¹ = Me, t-Bu] were designed and synthesized. Their in vitro anti-proliferative activity was evaluated against different cancer cell lines, including SK-BR-3, MDA-MB-231, HCT-116, SW480, Ovcar-3, HL-60, Saos-2 and HepG2. The results showed that, compound I [R = H; R¹ = Ot-Bu; R² = H] (IC₅₀ = 2.45 濠电偞鎸鹃幏?, I [R = Me; R¹ = Ot-Bu; R² = H] (IC₅₀ = 2.76 濠电偞鎸鹃幏? and I [R = H; R¹ = Ot-Bu; R² = 5-Cl] (IC₅₀ = 3.16 濠电偞鎸鹃幏? were the most potent ones against HL-60. Further biol. assays showed that HL-60, HCT116 and MDA-MB-231 were the most sensitive cell lines for compound I [R = H; R¹ = Ot-Bu; R² = H] and I [R = H; R¹ = Ot-Bu; R² = 5-Cl]. Mechanistic study revealed that compound I [R = H; R¹ = Ot-Bu; R² = H] enhanced reactive oxygen species level by inhibiting TrxR and then induced apoptosis by activating apoptosis proteins, bax and cleaved-caspase-3 in HCT116 cells. SAR anal. showed that the double bond in this series of compounds was very important for their cytostatic activity, indicating that the Michael-acceptor structure might contribute greatly to the anti-proliferative activity. 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).

Semenya, Dorothy et al. published their research in ACS Medicinal Chemistry Letters in 2022 | 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. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Computed Properties of C9H6ClNO

Structural Rigidification of N-Aryl-pyrroles into Indoles Active against Intracellular and Drug-Resistant Mycobacteria was written by Semenya, Dorothy;Touitou, Meir;Ribeiro, Camila Maringolo;Pavan, Fernando Rogerio;Pisano, Luca;Singh, Vinayak;Chibale, Kelly;Bano, Georg;Toscani, Anita;Manetti, Fabrizio;Gianibbi, Beatrice;Castagnolo, Daniele. And the article was included in ACS Medicinal Chemistry Letters in 2022.Computed Properties of C9H6ClNO This article mentions the following:

A series of indolyl-3-methyleneamines incorporating lipophilic side chains were designed through a structural rigidification approach and synthesized for investigation as new chem. entities against Mycobacterium tuberculosis (Mtb). The screening led to the identification of a 6-chloroindole analog 7j (I) bearing an N-octyl chain and a cycloheptyl moiety, which displayed potent in vitro activity against laboratory and clin. Mtb strains, including a pre-extensively drug-resistant (pre-XDR) isolate. 7j also demonstrated a marked ability to restrict the intracellular growth of Mtb in murine macrophages. Further assays geared toward mechanism of action elucidation have thus far ruled out the involvement of various known promiscuous targets, thereby suggesting that the new indole 7j may inhibit Mtb via a unique mechanism. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Computed Properties of C9H6ClNO).

O’Sullivan, D. G. et al. published their research in Journal of the Chemical Society in 1957 | 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. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Category: indole-building-block

Influence of ortho substituents on the stretching frequencies of side-chain carbonyl groups in substituted benzenes was written by O’Sullivan, D. G.;Sadler, P. W.. And the article was included in Journal of the Chemical Society in 1957.Category: indole-building-block This article mentions the following:

Carbonyl frequencies for ortho-substituted benzoic acids, acetanilides, hydroxyimino acetanilides, anthranilic acids, and 4- and 7-substituted isatins are tabulated for NH₂, Me, H, F, I, Br, Cl, CF₃, and NO₂ as substituents. The frequencies increase with para-闂?(Hammett’s) values, with acidity of the correspondingly substituted pyridinium ions, with Taft’s 闂?sup>+-values (C.A. 46, 10793f; 48, 11287e) and are well correlated among each other. In the experiment, the researchers used many compounds, for example, 7-Nitroindoline-2,3-dione (cas: 112656-95-8Category: indole-building-block).

Ravi, Ch. et al. published their research in Nucleosides, Nucleotides & Nucleic Acids in 2019 | CAS: 827-01-0

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

Synthesis, spectral studies, DNA binding, photocleavage, antimicrobial and anticancer activities of isoindol Ru(II) polypyridyl complexes was written by Ravi, Ch.;Vuradi, Ravi Kumar;Avudoddi, Srishailam;Yata, Praveen Kumar;Putta, Venkat Reddy;Srinivas, G.;Merugu, Ramchander;Satyanarayana, S.. And the article was included in Nucleosides, Nucleotides & Nucleic Acids in 2019.Application of 827-01-0 This article mentions the following:

Three new Ru(II) polypyridyl complexes [Ru(phen)₂CIIP]²⁺ (1) {CIIP = 2-(5-Chloro-3aH-Isoindol-3-yl)-1H-Imidazo[4,5-f][1,10]phenanthroline} (phen = 1,10-phenanthroline), [Ru(bpy)₂CIIP]²⁺ (2) (bpy = 2,2′-bipyridine) and [Ru(dmb)₂CIIP]²⁺ (3) (dmb = 4,4′-dimethyl-2,2′-bipyridine) were synthesized and characterized by different spectral methods. The DNA-binding behavior of these complexes was studied by absorption, emission spectroscopic titration and viscosity measurements, indicating that these three complexes bind to CT-DNA in an intercalative mode, but binding affinities of these complexes were different. The DNA-binding constants K_b of 1–3 were calculated in the order of 10⁶. All three complexes cleave pBR322 DNA in photoactivated cleavage studies and exhibit good antimicrobial activity. Anticancer activity of these Ru(II) complexes was evaluated in MCF7 cells. Cytotoxicity by MTT assay showed growth inhibition in a dose dependent manner. Cell cycle anal. by flow cytometry data showed an increase in Sub G1 population. Annexin V FITC/PI staining confirms that these complexes cause cell death by the induction of apoptosis. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Application of 827-01-0).

Henkel, Michael et al. published their research in Synthesis in 2020 | 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. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.SDS of cas: 4769-96-4

Annulation of Indoles with 1,n-Dibromoalkanes by a Pd(II)-Catalyzed and Norbornene-Mediated Reaction Cascade was written by Henkel, Michael;Bach, Thorsten. And the article was included in Synthesis in 2020.SDS of cas: 4769-96-4 This article mentions the following:

By employing 1,3-dibromopropane, 1,4-dibromobutane, and 1,5-dibromopentane as biselectrophiles, the annulation of indoles I (R = H, 5-Br, 4-CN, 5-t-BuO₂C, etc.) was probed in the presence of PdCl₂(CH₃CN)₂ as a catalyst and norbornene as a transpositional ligand. Ring formation to a five-membered ring was observed at positions C2 and N, while annulation of a six-membered ring occurred at positions C2 and C3. The latter cascade process was successfully applied to the direct synthesis of 1,2,3,4-tetrahydrocarbazoles II from indoles I (11 examples, 31-68% yields). Seven-membered-ring annulation was feasible by an initial coupling at position C2 followed by alkylation at C3. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4SDS of cas: 4769-96-4).

Zhang, Ming-Zhi et al. published their research in Tetrahedron in 2021 | 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.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: 827-01-0

First discovery of pimprinine derivatives and analogs as novel potential herbicidal, insecticidal and nematicidal agents was written by Zhang, Ming-Zhi;Mulholland, Nick;Seville, Anne;Hough, Gemma;Smith, Nicholas;Dong, Hong-Qiang;Zhang, Wei-Hua;Gu, Yu-Cheng. And the article was included in Tetrahedron in 2021.SDS of cas: 827-01-0 This article mentions the following:

Pimprinine and streptochlorin are indole natural products produced by many species of organisms, and they are reported to possess a wide range of biol. activities, such as anticancer, antiviral, antifungal activity and so on. In this study, three series of pimprinine derivatives or analogs were efficiently synthesized under the optimized methods. Biol. assays conducted at Syngenta firstly indicated the pimprinine derivatives or analogs possessed potential herbicidal and insecticidal activity, and this is highlighted by several compounds that possessed significant biol. activity as well as broad spectrum. Meanwhile, compounds with benzothiophene-oxazole core showed effective nematicidal activity in primary screening. Compounds 5-(benzofuran-3-yl)oxazole and 5-(benzodioxol-5-yl)oxazole were identified as the most promising lead structures for further study. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0SDS of 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.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: 827-01-0

Tilley, Jefferson W. et al. published their research in Journal of Medicinal Chemistry in 1980 | CAS: 150560-58-0

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

Pyrido[2,1-b]quinazolinecarboxylic acids as orally active antiallergy agents was written by Tilley, Jefferson W.;LeMahieu, Ronald A.;Carson, Mathew;Kierstead, Richard W.;Baruth, Herman W.;Yaremko, Bohdan. And the article was included in Journal of Medicinal Chemistry in 1980.Product Details of 150560-58-0 This article mentions the following:

Eight title compounds I (R = CO₂H, H, Me, or CHMe₂; R¹ = H, Me, CHMe₂, Ac, N(:CMe)OMe, or CO₂H) were synthesized by the Ni carbonyl mediated carboxylation of the corresponding bromides. Comparable antiallergy activities were observed for both the 2-alkyl-8-carboxy and the corresponding 8-alkyl-2-carboxy analogs. I; R = CO₂H, R¹ = CHMe₂ [68700-95-8] was one of the most active substances administered orally in the rat passive cutaneous anaphylasis test. In the experiment, the researchers used many compounds, for example, 5-Isopropylindoline-2,3-dione (cas: 150560-58-0Product Details of 150560-58-0).

Harrison, William T. A. et al. published their research in Acta Crystallographica, Section E: Structure Reports Online in 2006 | CAS: 167631-84-7

Methyl 5-fluoro-1H-indole-2-carboxylate (cas: 167631-84-7) 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. In addition to indole, the strain-release chemistry worked for numerous substrates including amines, alcohols, thiols, carboxylic acids, imidazoles, and pyrazoles.Related Products of 167631-84-7

5-Fluoro-1H-indole-2-carbohydrazide was written by Harrison, William T. A.;Yathirajan, H. S.;Ashalatha, B. V.;Raj, K. K. Vijaya;Narayana, B.. And the article was included in Acta Crystallographica, Section E: Structure Reports Online in 2006.Related Products of 167631-84-7 This article mentions the following:

The geometric parameters for the essentially planar mol. of the title compound, C₉H₈FN₃O, are normal. A network of N-H…O and N-H…N H-bonds helps to establish the crystal packing. Crystal data: orthorhombic, space group Pbca, a 10.0451(3), b 9.4978(2), c 18.5293(6) 闂? Z = 8, d = 1.452 g/cm, 1497 observed reflections with I > 2(I), 140 refined parameters, R[F² > 2闂?F²)] = 0.032, wR(F²) = 0.089. In the experiment, the researchers used many compounds, for example, Methyl 5-fluoro-1H-indole-2-carboxylate (cas: 167631-84-7Related Products of 167631-84-7).