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Liu, Yue et al. published their research in Advanced Synthesis & Catalysis in 2020 | CAS: 112656-95-8

7-Nitroindoline-2,3-dione (cas: 112656-95-8) 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.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Reference of 112656-95-8

Palladium-Catalyzed Cascade Hydrosilylation and Amino-Methylation of Isatin Derivatives was written by Liu, Yue;Xia, Yun-Tao;Cui, Su-Hang;Ji, Yi-Gang;Wu, Lei. And the article was included in Advanced Synthesis & Catalysis in 2020.Reference of 112656-95-8 This article mentions the following:

3-Aminomethyl-3-silyloxy-2-indolones I (R₃ = Et₃, ^tBuMe₂, Bu₃; R¹ = Me, R¹₂ = CH₂CH₂OCH₂CH₂; R² = Me, MeO, halo, CO₂Me) were prepared by palladium acetate-catalyzed tandem hydrosilylative coupling of isatins with hydrosilanes HSiR₃ and formamides R¹₂NCHO. We demonstrate that using palladium acetate as a catalyst for reduction of DMF and isatin derivatives by hydrosilanes, a cascade hydrosilylation and amino-methylation reaction can be realized. With DMF as a reactant and a solvent, the in-situ generated siloxymethylamine intermediate, an adduct of DMF and hydrosilanes, smoothly participates in the successive stages, providing a serials of Si, N-functionalized indolin-2-ones in moderate to good yields. This strategy exhibits high chemoselectivity toward carbonyl moieties reduction among the substrates. In the experiment, the researchers used many compounds, for example, 7-Nitroindoline-2,3-dione (cas: 112656-95-8Reference of 112656-95-8).

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

Cao, Yun-yun et al. published their research in Zhongguo Yaowu Huaxue Zazhi in 2013 | 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.Related Products of 774-47-0

Synthesis and antitumor activity of novel 6-substituted methylenehydrazinyl-2,4-bismorpholino-pyrimidine and 1,3,5-triazine derivatives was written by Cao, Yun-yun;Zhu, Wu-fu;Zhu, Yan;Guo, Fei;Lu, Xiang-ran;Gong, Ping. And the article was included in Zhongguo Yaowu Huaxue Zazhi in 2013.Related Products of 774-47-0 This article mentions the following:

A series of 6-substituted methylenehydrazinyl-2,4-bismorpholino-pyrimidine and 1,3,5-triazine derivatives were synthesized and their chem. structures were confirmed by ¹H-NMR and MS spectra. As the raw materials, 2,4,6-trichloropyrimidine or cyanuric chloride, aniline, benzimidazole and pyrrole were used to obtain the title compounds by multi-step reactions including substitution, cyclization, N-alkylation and Vilsmeier reaction. All the synthesized compounds were evaluated for their antitumor activities against three cancer cell lines (H460, A549 and H226) by the MTT method and BMCL-200908069-1 as the pos. control. Most of the prepared compounds exhibited moderate cytotoxic activities and high selectivity against H460 cancer cell line and A549 compared with the pos. control compound The pharmacol. data indicated that the introduction of substituted aryl methylene group was favorable for increasing the antitumor activity. The most promising compound 6a showed a strong antitumor activity against H460, A549 and H226 cell lines with IC₅₀ values of 3.4濠电偞鎸鹃幐绱€l闁荤姾娅ｉ弸?sup>-1, 0.75濠电偞鎸鹃幐绱€l闁荤姾娅ｉ弸?sup>-1 and 0.86濠电偞鎸鹃幐绱€l闁荤姾娅ｉ弸?sup>-1, which were 2.8 to 16.8 times more active than the pos. control (9.52濠电偞鎸鹃幐绱€l闁荤姾娅ｉ弸?sup>-1, 29.24濠电偞鎸鹃幐绱€l闁荤姾娅ｉ弸?sup>-1, 36.21濠电偞鎸鹃幐绱€l闁荤姾娅ｉ弸?sup>-1), resp. Further studies are currently underway and will be reported in the future. In the experiment, the researchers used many compounds, for example, 5,6-Difluoroindoline-2,3-dione (cas: 774-47-0Related Products of 774-47-0).

Alvarez, Estela et al. published their research in Chemistry – A European Journal 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. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Recommanded Product: 6-Nitro-1H-indole

Bronsted Acid-Catalyzed Cascade Reactions Involving 1,2-Indole Migration was written by Alvarez, Estela;Nieto Faza, Olalla;Silva Lopez, Carlos;Fernandez-Rodriguez, Manuel A.;Sanz, Roberto. And the article was included in Chemistry – A European Journal in 2015.Recommanded Product: 6-Nitro-1H-indole This article mentions the following:

A cascade reaction of indoles with propargylic diols involving an unprecedented metal-free 1,2-indole migration onto an alkyne was carried out. DFT calculations support a mechanism consisting of a concerted nucleophilic attack of the indole nucleus with loss of water, followed by the 1,2-migration and subsequent Nazarov cyclization. This Bronsted acid-catalyzed protocol affords indole-functionalized benzofulvene derivatives in high yields. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4Recommanded Product: 6-Nitro-1H-indole).

Li, Dingzhong et al. published their research in Catalysis Communications in 2022 | 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.Synthetic Route of C8H6N2O2

Industrial Cunninghamia lanceolata carbon supported FeO(OH) nanoparticles-catalyzed hydrogenation of nitroarenes was written by Li, Dingzhong;Lu, Hao;Yang, Tianbao;Xing, Chen;Sun, Tulai;Fu, Lihua;Qiu, Renhua. And the article was included in Catalysis Communications in 2022.Synthetic Route of C8H6N2O2 This article mentions the following:

An industrial Cunninghamia lanceolata carbon supported FeO(OH) nanoparticles process for the synthesis of aryl amines with good yields via hydrogenation of nitroarenes was reported. Nine key anti-cancer drug intermediates were successfully achieved with protocol. And Osimertinib intermediate could be smoothly synthesized at a 2.67 kg-scale with >99.5% HPLC purity. This protocol featured cheap carbon source, highly catalytic activity, simple operation, kilogram-scalable and recyclable catalysts (eight times without observable losing activity). In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4Synthetic Route of C8H6N2O2).

Lu, Lin 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. Indole, first isolated in 1866, and it is commonly synthesized from phenylhydrazine and pyruvic acid, although several other procedures have been discovered. 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). Safety of 5-Chloroindole-3-carboxaldehyde

Access to Polycyclic Sulfonyl Indolines via Fe(II)-Catalyzed or UV-Driven Formal [2 + 2 + 1] Cyclization Reactions of N-((1H-indol-3-yl)methyl)propiolamides with NaHSO₃ was written by Lu, Lin;Luo, Chenguang;Peng, Hui;Jiang, Huanfeng;Lei, Ming;Yin, Biaolin. And the article was included in Organic Letters in 2019.Safety of 5-Chloroindole-3-carboxaldehyde This article mentions the following:

A variety of structurally novel polycyclic sulfonyl indolines were synthesized via FeCl₂-catalyzed or UV-driven intramol. formal [2 + 2 + 1] dearomatizing cyclization reactions of N-(1H-indol-3-yl)methylpropiolamides with NaHSO₃ in an aqueous medium. The reactions involve the formation of one C-C bond and two C-S bonds in a single step. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Safety of 5-Chloroindole-3-carboxaldehyde).

Kaila, Neelu et al. published their research in Journal of Medicinal Chemistry in 2007 | 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. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Application of 150560-58-0

Synthesis and biological evaluation of quinoline salicylic acids as P-selectin antagonists was written by Kaila, Neelu;Janz, Kristin;DeBernardo, Silvano;Bedard, Patricia W.;Camphausen, Raymond T.;Tam, Steve;Tsao, Desiree H. H.;Keith, James C. Jr.;Nickerson-Nutter, Cheryl;Shilling, Adam;Young-Sciame, Ruth;Wang, Qin. And the article was included in Journal of Medicinal Chemistry in 2007.Application of 150560-58-0 This article mentions the following:

Leukocyte recruitment of sites of inflammation and tissue injury involves leukocyte rolling along the endothelial wall, followed by firm adherence of the leukocyte, and finally transmigration of the leukocyte across cell junctions into the underlying tissue. The initial rolling step is mediated by the interaction of leukocyte glycoproteins containing active moieties such as sialyl Lewis^x (sLe^x) with P-selectin expressed on endothelial cells. Consequently, inhibition of this interaction by means of a small mol. P-selectin antagonist is an attractive strategy for the treatment of inflammatory diseases such as arthritis. High-throughput screening of the Wyeth chem. library identified the quinoline salicylic acid class of compounds as antagonists of P-selectin, with potency in in vitro and cell-based assays far superior to that of sLe^x. Through iterative medicinal chem., it was identified analogs with improved P-selectin activity, decreased inhibition of dihydrooratate dehydrogenase, and acceptable CYP profiles. Lead compound , I, was efficacious in the rat AIA model of rheumatoid arthritis. In the experiment, the researchers used many compounds, for example, 5-Isopropylindoline-2,3-dione (cas: 150560-58-0Application of 150560-58-0).

Li, Shunian et al. published their research in Organic Chemistry Frontiers in 2021 | CAS: 774-47-0

5,6-Difluoroindoline-2,3-dione (cas: 774-47-0) 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. 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: C8H3F2NO2

Ni-Catalyzed asymmetric hetero-Diels-Alder reactions of conjugated vinyl azides: Synthesis of chiral azido polycycles was written by Li, Shunian;Lu, Haifeng;Xu, Zhenghu;Wei, Fang. And the article was included in Organic Chemistry Frontiers in 2021.COA of Formula: C8H3F2NO2 This article mentions the following:

The authors describe an efficient Ni(II)/Feng ligand-catalyzed asym. hetero-Diels-Alder reaction between conjugated vinyl azides RC(:CH₂)N₃ [R = 1-cyclohexenyl, 1-cyclopentenyl, C₆H₅CH:CH, C₆H₅C(:CH₂)] and carbonyl groups in compounds such as isatins I (R¹ = H, 5,6-F₂, 7-Br, 5-Me, etc.) and R²C(O)C(O)OR³ (R² = H, Ph, 4-MeOC₆H₄, 4-FC₆H₄, 4-MeC₆H₄, R³ = Me, Et). This method provides a platform for the synthesis of complicated chiral azido polycycles II (R⁴ = H, 10,11-F₂, 9-Br, 11-OCF₃, 11-Me, etc.) and III in high yields and excellent enantioselectivities. In the experiment, the researchers used many compounds, for example, 5,6-Difluoroindoline-2,3-dione (cas: 774-47-0COA of Formula: C8H3F2NO2).

Liu, Ruixing et al. published their research in Organic Letters in 2019 | CAS: 4769-96-4

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

Activation Relay on Rhodium-Catalyzed C-H Aminomethylation in Cooperation with Photoredox Catalysis was written by Liu, Ruixing;Liu, Jiaxin;Wei, Yin;Shi, Min. And the article was included in Organic Letters in 2019.Name: 6-Nitro-1H-indole This article mentions the following:

A site selective C-H aminomethylation at indole’s C3 position was achieved by merging rhodium(III)-catalyzed C-H activation and photoredox catalysis in a one-pot manner. A study of the mechanistic insights rationalized the essence of the activation relay and the combination mode. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4Name: 6-Nitro-1H-indole).

Ma, Liang et al. published their research in Applied Microbiology and Biotechnology in 2017 | CAS: 827-01-0

5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) 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.Recommanded Product: 5-Chloroindole-3-carboxaldehyde

Identification and characterization of a biosynthetic gene cluster for tryptophan dimers in deep sea-derived Streptomyces sp. SCSIO 03032 was written by Ma, Liang;Zhang, Wenjun;Zhu, Yiguang;Zhang, Guangtao;Zhang, Haibo;Zhang, Qingbo;Zhang, Liping;Yuan, Chengshan;Zhang, Changsheng. And the article was included in Applied Microbiology and Biotechnology in 2017.Recommanded Product: 5-Chloroindole-3-carboxaldehyde This article mentions the following:

Tryptophan dimers (TDs) are an important class of natural products with diverse bioactivities and share conserved biosynthetic pathways. We report the identification of a partial gene cluster (spm) responsible for the biosynthesis of a class of unusual TDs with non-planar skeletons including spiroindimicins (SPMs), indimicins (IDMs), and lynamicins (LNMs) from the deep-sea derived Streptomyces sp.SCSIO 03032. Bioinformatics anal., targeted gene disruptions, and heterologous expression studies confirmed the involvement of the spm gene cluster in the biosynthesis of SPM/IDM/LNMs, and revealed the indispensable roles for the halogenase/reductase pair SpmHF, the amino acid oxidase SpmO, and the chromopyrrolic acid (CPA) synthase SpmD, as well as the pos. regulator SpmR and the putative transporter SpmA. However, the spm gene cluster was unable to confer a heterologous host the ability to produce SPM/IDM/LNMs. In addition, the P 450 enzyme SpmP and the monooxygenase SpmX2 were found to be non-relevant to the biosynthesis of SPM/IDM/LNMs. Sequence alignment and structure modeling suggested the lack of key conserved amino acid residues in the substrate-binding pocket of SpmP. Furthermore, feeding experiments in the non-producing 闂佸墽绮锕憁O mutant revealed several biosynthetic precursors en route to SPMs, indicating that key enzymes responsible for the biosynthesis of SPMs should be encoded by genes outside of the identified spm gene cluster. Finally, the biosynthetic pathways of SPM/IDM/LNMs are proposed to lay a basis for further insights into their intriguing biosynthetic machinery. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Recommanded Product: 5-Chloroindole-3-carboxaldehyde).

Karadayi, Fikriye Zengin et al. published their research in New Journal of Chemistry in 2021 | 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.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Name: 5-Chloroindole-3-carboxaldehyde

Design, synthesis, anticancer activity, molecular docking and ADME studies of novel methylsulfonyl indole-benzimidazoles in comparison with ethylsulfonyl counterparts was written by Karadayi, Fikriye Zengin;Yaman, Murat;Kisla, Mehmet Murat;Konu, Ozlen;Ates-Alagoz, Zeynep. And the article was included in New Journal of Chemistry in 2021.Name: 5-Chloroindole-3-carboxaldehyde This article mentions the following:

In this study, novel methylsulfonyl indole-benzimidazole derivatives I (R¹ = Me, cyclohexyl, (3,4-dichlorophenyl)methyl, etc.; R² = H, OMe, Cl, Br) have been synthesized upon substitution of resp. first (R¹) and fifth (R²) positions of benzimidazole and indole groups. Structure and activity relationships were then studied via ¹H NMR, ¹³C NMR, mass spectral and in silico docking analyses, as well as cell viability measurements. The compounds I that exhibited substantial affinity levels towards ER alpha (ER婵? were found. In addition, the correlation anal. of cytotoxicity profiles between ethyl- and methyl-sulfonyl indole-benzimidazoles revealed a collection of effective and consistent R¹ and R² substitutions. However, for some candidate derivatives, I distinctive cytotoxicity levels and varying viability vs. ER婵?affinity correlations were observable across the studies, suggesting that the sulfonyl side chain modifications themselves can also influence the ER婵?binding levels. These results demonstrated that novel methylsulfonyl indole-benzimidazole derivatives, I similar to their ethylsulfonyl counterparts, exhibit anticancer effects with potential estrogen receptor modulatory actions. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Name: 5-Chloroindole-3-carboxaldehyde).