Tag: 100-200

Catalyst-Free Chemoselective Reduction of Nitroarenes Using Thiourea as a Hydrogen Source was written by Lv, Mei-fang;Lu, Guo-ping;Cai, Chun. And the article was included in Asian Journal of Organic Chemistry in 2015.COA of Formula: C8H6N2O2 This article mentions the following:

A newly developed protocol for the reduction of nitroarenes using thiourea as the hydrogen source was described. The method was simple, inexpensive and easily applicable to the preparation of a variety of substituted anilines with high yields and selectivity. In contrast to traditional hydrogenation methods, this chem. does not required a catalyst, elaborated work-up procedures, or the use of high-pressure equipment. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4COA of Formula: C8H6N2O2).

6-Nitro-1H-indole (cas: 4769-96-4) 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.COA of Formula: C8H6N2O2

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

Structure-based design and synthesis of 2,4-diaminopyrimidines as EGFR L858R/T790M selective inhibitors for NSCLC was written by Chen, Lingfeng;Fu, Weitao;Feng, Chen;Qu, Rong;Tong, Linjiang;Zheng, Lulu;Fang, Bo;Qiu, Yinda;Hu, Jie;Cai, Yuepiao;Feng, Jianpeng;Xie, Hua;Ding, Jian;Liu, Zhiguo;Liang, Guang. And the article was included in European Journal of Medicinal Chemistry in 2017.Category: indole-building-block This article mentions the following:

Mutated epidermal growth factor receptor (EGFR) is a major driver of non-small cell lung cancer (NSCLC). The EGFRT790M secondary mutation has become a leading cause of clin.-acquired resistance to gefitinib and erlotinib. Herein, structure-based design approach to increase the potency and selectivity of the previously reported reversible EGFR inhibitor I, at the kinase and cellular levels has been reported. Three-step structure-activity relationship exploration led to promising compounds II (R¹ = Br; R² = 1-methyl-1H-indol-6-yl, 2,3-dihydro-1H-inden-5-yl; R³ = OMe; R⁴ = 4-methyl-1-piperazinyl) with unique chem. structure and binding mode from the other third-generation tyrosine kinase inhibitors. In a human NSCLC xenograft model, the above compounds exhibited dose-dependent tumor growth suppression without toxicity. These selective inhibitors are promising drug candidates for EGFRT790M-driven NSCLC. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4Category: indole-building-block).

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.Category: indole-building-block

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

Asymmetric cross aldol addition of isatins with 伪,尾-unsaturated ketones catalyzed by a bifunctional Bronsted acid-Bronsted base organocatalyst was written by Liu, Guo-Gui;Zhao, Hua;Lan, Yu-Bao;Wu, Bin;Huang, Xiao-Fei;Chen, Jian;Tao, Jing-Chao;Wang, Xing-Wang. And the article was included in Tetrahedron in 2012.Quality Control of 5,6-Difluoroindoline-2,3-dione This article mentions the following:

The asym. cross-aldol reaction of isatins with 伪,尾-unsaturated ketones has been developed under catalysis by a Cinchona alkaloid-derived bifunctional Bronsted acid-Bronsted base catalyst, affording the aldol adducts in moderate to good yields (18-98%) with moderate to good enantioselectivities (30-97%). The noncovalent organo-catalyzed asym. cross-aldol reaction displays a broad substrate scope and wide functional-group tolerability, albeit the electronic and steric properties of both reaction partners have considerable and regular effects on the reactivity and stereocontrol. In the experiment, the researchers used many compounds, for example, 5,6-Difluoroindoline-2,3-dione (cas: 774-47-0Quality Control of 5,6-Difluoroindoline-2,3-dione).

5,6-Difluoroindoline-2,3-dione (cas: 774-47-0) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Quality Control of 5,6-Difluoroindoline-2,3-dione

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

Discovery of a New Class of Anilinoquinazoline Inhibitors with High Affinity and Specificity for the Tyrosine Kinase Domain of c-Src was written by Ple, Patrick A.;Green, Tim P.;Hennequin, Laurent F.;Curwen, Jon;Fennell, Michael;Allen, Jack;Lambert-van der Brempt, Christine;Costello, Gerard. And the article was included in Journal of Medicinal Chemistry in 2004.Quality Control of 1-Methyl-1H-indol-4-amine This article mentions the following:

Deregulated activity of the nonreceptor tyrosine kinase c-Src is believed to result in signal transduction, cytoskeletal and adhesion changes, ultimately promoting a tumor-invasive phenotype. We report here the discovery of a new class of anilinoquinazoline inhibitors with high affinity and specificity for the tyrosine kinase domain of the c-Src enzyme. Special attention was directed toward finding inhibitors selective against KDR tyrosine kinase in order to ensure that the in vivo profile of a specific Src inhibitor could be determined The 4-aminobenzodioxole quinazoline series gave compounds with excellent potency and selectivity. The most interesting compounds were evaluated in vivo and displayed good pharmacokinetics following oral dosing. Compounds such as the aminobenzodioxoles were shown to be potent inhibitors of tumor growth in a c-Src-transformed 3T3 xenograft model in vivo, resulting in more than 90% growth inhibition at doses as low as 6 mg/kg po once daily. Src tyrosine kinase inhibitors such as these may provide a novel therapeutic modality for targeting cancer invasion and metastasis. In the experiment, the researchers used many compounds, for example, 1-Methyl-1H-indol-4-amine (cas: 85696-95-3Quality Control of 1-Methyl-1H-indol-4-amine).

1-Methyl-1H-indol-4-amine (cas: 85696-95-3) 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. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Quality Control of 1-Methyl-1H-indol-4-amine

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

Antibacterial and cytotoxic activity of 3, 3′-(5,5′-methylene bis(3-mercapto-4H-1,2,4-triazole-5,4-diyl) bis (azan-1-yl-1-ylidene) diindolin-2-ones was written by Rani, S. Shobha;Ajitha, M.;Agaiah, Bairi;Sarangapani, M.. And the article was included in Journal of Chemical and Pharmaceutical Sciences in 2010.Related Products of 112656-95-8 This article mentions the following:

Indolinones I (R¹ = H, R² = 5-F, 5-Me, 6-Br, etc.) were synthesized by the condensation of an appropriate isatin with 5,5¹-methylenediyl-bis(4-amino-4H-1,2,4-triazole-3-thiol). Compounds I were screened for cytotoxic activity using A-549 Lung cancer and HT-29 Colon cancer cell lines by MTT method and antibacterial activity against B. subtilis, S. aureus, E. coli and S. typhi by cup plate method. In the experiment, the researchers used many compounds, for example, 7-Nitroindoline-2,3-dione (cas: 112656-95-8Related Products of 112656-95-8).

7-Nitroindoline-2,3-dione (cas: 112656-95-8) 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. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Related Products of 112656-95-8

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

Synthesis and characterization of cytotoxic activity of certain n-(6-benzoyl-1H-benzo [d] imidazol-2-yl)-2-(2-oxoindolin-3-ylidene) hydrazine carboxamides was written by Rani, B. Shoba;Priyanka, K. Blessi;Sammaiah, G.. And the article was included in International Journal of Pharmacy and Biological Sciences in 2014.Formula: C8H4N2O4 This article mentions the following:

A series of N-(6-benzoyl-1H-benzo[d]imidazol-2-yl)-2-(2-oxoindolin-3-ylidene) hydrazine carboxamides I [R = H, 5-CH₃, 5-Cl, 5-Br, 5-NO₂, 7-NO₂, 7-CH₃] were synthesized by treating (5-benzoyl-1H-benzo[d]imidazol-2-yl) carbamates II with different substituted isatins. All the synthesized derivatives I were screened for anticancer activity against Hela using MTT assay and produced a dose dependent inhibition of growth of the cells. The IC₅₀ values of all the synthetic test compounds were found between 16.03 to 41.75. The potency of (IC₅₀ values) of cytotoxicity of compounds was compared with that of known cytotoxic agent, Cisplatin. Among all the synthesized novel compound I (R = 5-Cl) showed the most potent activity against MCF-7 cell lines. In the experiment, the researchers used many compounds, for example, 7-Nitroindoline-2,3-dione (cas: 112656-95-8Formula: C8H4N2O4).

7-Nitroindoline-2,3-dione (cas: 112656-95-8) 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.Formula: C8H4N2O4

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

Electrochemically Enabled C3-Formylation and -Acylation of Indoles with Aldehydes was written by Yang, Liquan;Liu, Zhaoran;Li, Yujun;Lei, Ning;Shen, Yanling;Zheng, Ke. And the article was included in Organic Letters in 2019.Category: indole-building-block This article mentions the following:

Reported herein is an effective strategy for oxidative cross-coupling of indoles with various aldehydes. The strategy is based on a two-step transformation via a known Mannich-type reaction and a C-N bond cleavage for carbonyl introduction. The key step-the C-N bond cleavage of the Mannich product-was enabled by electrochem. This strategy (with over 40 examples) ensures excellent functional-group tolerance as well as late-stage functionalization of pharmaceutical mols. In the experiment, the researchers used many compounds, for example, 1,4-Dimethyl-1H-indole-3-carbaldehyde (cas: 170489-16-4Category: indole-building-block).

1,4-Dimethyl-1H-indole-3-carbaldehyde (cas: 170489-16-4) 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.Category: indole-building-block

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

Indolylalkyltriphenylphosphonium Analogues Are Membrane-Depolarizing Mycobactericidal Agents was written by Li, Ming;Nyantakyi, Samuel A.;Gopal, Pooja;Aziz, Dinah binte;Dick, Thomas;Go, Mei-Lin. And the article was included in ACS Medicinal Chemistry Letters in 2017.Recommanded Product: 4769-96-4 This article mentions the following:

Agents that selectively target the mycobacterial membrane could potentially shorten treatment time for tuberculosis, reduce relapse and curtail emergence of resistant strains. The lipophilicity and extensive charge delocalized state of the triphenylphosphonium (TPP) cation strongly favor accumulation within bacterial membranes. Here we explored the antimycobacterial activities and membrane targeting properties of indolylalkyltriphenylphosphonium analogs. The most active analogs preferentially inhibited growth of Mycobacterium tuberculosis H37Rv (MIC₅₀ 2-4 渭M) and were cidal against Mycobacterium bovis BCG (MBC99 3 渭M). In spite of their propensity to accumulate within membranes, we found no evidence that these compounds permeabilized mycobacterial membranes or induced cell-envelope stress. Our investigations indicated that the cidal effects of these compounds stem from sustained depolarization of mycobacterial membranes and ensuing disruptive effects on electron transfer and cell division. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4Recommanded Product: 4769-96-4).

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

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

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).

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

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