Tag: 200-300

Palladium-mediated in situ synthesis of an anticancer agent was written by Indrigo, Eugenio;Clavadetscher, Jessica;Chankeshwara, Sunay V.;Lilienkampf, Annamaria;Bradley, Mark. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2016.Product Details of 754214-56-7 This article mentions the following:

As a novel prodrug activation strategy Pd(0) nanoparticles, entrapped within a modular polymeric support, were used in cell culture, to synthesize the anticancer agent PP-121 from two non-toxic precursors, thereby inducing cell death in the first example of in situ mediated drug synthesis. In the experiment, the researchers used many compounds, for example, 7-Azaindole-5-boronic Acid Pinacol Ester (cas: 754214-56-7Product Details of 754214-56-7).

7-Azaindole-5-boronic Acid Pinacol Ester (cas: 754214-56-7) 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. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Product Details of 754214-56-7

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

Optimization, Structure-Activity Relationship, and Mode of Action of Nortopsentin Analogues Containing Thiazole and Oxazole Moieties was written by Guo, Jincheng;Hao, Yanan;Ji, Xiaofei;Wang, Ziwen;Liu, Yuxiu;Ma, Dejun;Li, Yongqiang;Pang, Huailin;Ni, Jueping;Wang, Qingmin. And the article was included in Journal of Agricultural and Food Chemistry in 2019.Computed Properties of C9H5BrN2 This article mentions the following:

Plant diseases seriously endanger plant health, and it is very difficult to control them. A series of nortopsentin analogs were designed, synthesized, and evaluated for their antiviral activities and fungicidal activities. Most of these compounds displayed higher antiviral activities than ribavirin. Compounds (CAS 224434-76-8, 265110-91-6, 272104-33-3), with excellent antiviral activities, emerged as novel antiviral lead compounds, among which compound (CAS 265110-91-6) was selected for further antiviral mechanism research. The mechanism research results indicated that these compounds may play an antiviral role by aggregating viral particles to prevent their movement in plants. Further fungicidal activity tests revealed that nortopsentin analogs displayed broad-spectrum fungicidal activities. Compounds (CAS 2376842-39-4 and 2376840-03-6) displayed higher antifungal activities against Alternaria solani than the com. fungicides carbendazim and chlorothalonil. Current research has laid a foundation for the application of nortopsentin analogs in plant protection. In the experiment, the researchers used many compounds, for example, 5-Bromo-3-cyanoindole (cas: 90271-86-6Computed Properties of C9H5BrN2).

5-Bromo-3-cyanoindole (cas: 90271-86-6) 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.Computed Properties of C9H5BrN2

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

Reactions of imides with samarium(II) iodide was written by Brandukova, N. E.;Vygodskii, Ya. S.;Komarova, L. I.;Strelkova, T. V.. And the article was included in Izvestiya Akademii Nauk, Seriya Khimicheskaya in 1996.Category: indole-building-block This article mentions the following:

One of the carbonyl groups of N-phenylphthalimide is reduced by SmI₂ to a CHOH or CH₂ group at ∼20°. The reaction pathway depends mainly on the reactant ratio and the sequence of reactant addition to the reaction mixture Under similar conditions, both CO groups of N-acetylcaprolactam are reduced by SmI₂, whereas the CO group of ε-caprolactam is not reduced. In the experiment, the researchers used many compounds, for example, 2-Phenylisoindolin-1-one (cas: 5388-42-1Category: indole-building-block).

2-Phenylisoindolin-1-one (cas: 5388-42-1) 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.Category: indole-building-block

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

New Arylthioindoles and Related Bioisosteres at the Sulfur Bridging Group. 4. Synthesis, Tubulin Polymerization, Cell Growth Inhibition, and Molecular Modeling Studies was written by La Regina, Giuseppe;Sarkar, Taradas;Bai, Ruoli;Edler, Michael C.;Saletti, Roberto;Coluccia, Antonio;Piscitelli, Francesco;Minelli, Lara;Gatti, Valerio;Mazzoccoli, Carmela;Palermo, Vanessa;Mazzoni, Cristina;Falcone, Claudio;Scovassi, Anna Ivana;Giansanti, Vincenzo;Campiglia, Pietro;Porta, Amalia;Maresca, Bruno;Hamel, Ernest;Brancale, Andrea;Novellino, Ettore;Silvestri, Romano. And the article was included in Journal of Medicinal Chemistry in 2009.HPLC of Formula: 210345-56-5 This article mentions the following:

A series of arylthioindoles, e.g., I (X = S, R¹ = H, CO₂Me, CO₂Et, R² = H, Cl, Br, OMe), the corresponding ketones I (X = CO) and diarylmethanes I (X = CH₂), as well as pyrrole II (Y = CH₂, CO, Z = CH, R³ = CO₂Et, R⁴ = R⁵ = H; etc.) and imidazole analogs II (Y = CO, Z = N, R³ = R⁵ = H, R⁴ = CO₂Et; etc.) were synthesized and their activity as tubulin polymerization and cancer cell growth inhibitors assessed. As growth inhibitors of MCF-7 cells, sulfur derivatives were superior or sometimes equivalent to the ketones, while methylene derivatives were substantially less effective. Indoles I (X = S, R¹ = H, R² = Br; X = S, CO, CH₂, R¹ = CO₂Me, R² = Br, OMe) showed ∼50% of inhibition on human HeLa and HCT116/chr3 cells at 0.5 μM, and these compounds inhibited the growth of HEK, M14, and U937 cells with IC₅₀‘s in the 78-220 nM range. While murine macrophage J744.1 cell growth was significantly less affected (20% at higher concentrations), four other non-transformed cell lines remained sensitive to these indoles. The effect of drug treatment on cell morphol. was examined by time-lapse microscopy. In a protocol set up to evaluate toxicity on the Saccharomyces cerevisiae BY4741 wild type strain, compounds I (X = S, R¹ = H, R² = Br) and II (Y = CH₂, Z = CH, R³ = CO₂H, R⁴ = R⁵ = H) strongly reduced cell growth, and I (X = CH₂, R¹ = CO₂Me, R² = Br; X = S, CO, R¹ = CO₂Me, R² = OMe) also showed significant inhibition. In the experiment, the researchers used many compounds, for example, Methyl 5-bromo-1H-indole-2-carboxylate (cas: 210345-56-5HPLC of Formula: 210345-56-5).

Methyl 5-bromo-1H-indole-2-carboxylate (cas: 210345-56-5) 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. 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.HPLC of Formula: 210345-56-5

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

2,6-Disubstituted imidazo[2,1-b][1,3,4]thiadiazole derivatives as potent Staphylococcal biofilm inhibitors was written by Cascioferro, Stella;Parrino, Barbara;Petri, Giovanna Li;Cusimano, Maria Grazia;Schillaci, Domenico;Di Sarno, Veronica;Musella, Simona;Giovannetti, Elisa;Cirrincione, Girolamo;Diana, Patrizia. And the article was included in European Journal of Medicinal Chemistry in 2019.COA of Formula: C9H5BrN2 This article mentions the following:

A class of 36 new 2-(6-phenylimidazo[2,-1-b][1,3,4]thiadiazol-2-yl)-1H-indoles, compounds I [R = H, Cl, Br; R¹ = H, Me; R² = H, 3-MeO, 4F, etc.] was efficiently synthesized and evaluated for their anti-biofilm properties against the Gram-pos. bacterial reference strains Staphylococcus aureus ATCC 25923, S. aureus ATCC 6538 and Staphylococcus epidermidis ATCC 12228, and the Gram-neg. strains Pseudomonas aeruginosa ATCC 15442 and Escherichia coli ATCC 25922. Many of these new compounds, were able to inhibit biofilm formation of the tested Staphylococcal strains showing BIC₅₀ lower than 10 μg/mL. In particular, compounds I [R = H, R¹ = H, R² = 2,5-diMeO; R = H, R¹ = Me, R² = 3-MeO] showed remarkable anti-biofilm activity against S. aureus ATCC 25923 with BIC₅₀ values of 0.5 and 0.8 μg/mL, resp., whereas compound I [R = Cl, R¹ = H, R² = 2,5-diMeO] was the most potent against S. aureus ATCC 6538, with a BIC₅₀ of 0.3 μg/mL. Remarkably, these compounds showed effects in the early stages of the biofilm formation without affecting the mature biofilm of the same strains and the viability of the planktonic form. Their ability in counteracting a virulence factor (biofilm formation) without interfering with the bacterial growth in the free life form make them novel valuable anti-virulence agents. In the experiment, the researchers used many compounds, for example, 5-Bromo-3-cyanoindole (cas: 90271-86-6COA of Formula: C9H5BrN2).

5-Bromo-3-cyanoindole (cas: 90271-86-6) 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. 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.COA of Formula: C9H5BrN2

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

Relation between electronic structure and auxin activity of chlorinated β-indolylacetic acids was written by Cocordano, Maurice;D’Amato, Franck;Turcat, Jean J.. And the article was included in Annales de la Faculte des Sciences de Marseille in 1970.Recommanded Product: 1912-45-4 This article mentions the following:

Five chlorinated β-indolylacetic acids (I) were prepared by the cyclization of ClC6H4NHN:CHCH2CH2CO2H in ethanolic H2SO4 followed by saponification The auxinic activity of I derivatives was in the order 6-Cl- > nonchlorinated > 6,7-Cl2 > 7-Cl > 5,7-Cl2. The electronic structure of I was calculated by LCAO method. I forms by, its CO2H group, a conjugated unstable complex with the protein of the cell. In the experiment, the researchers used many compounds, for example, 2-(5-Chloro-1H-indol-3-yl)acetic acid (cas: 1912-45-4Recommanded Product: 1912-45-4).

2-(5-Chloro-1H-indol-3-yl)acetic acid (cas: 1912-45-4) 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.Recommanded Product: 1912-45-4

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

A facile synthesis of pyrrolo[2,3-j]phenanthridines via the cascade reaction of indoleanilines and aldehydes was written by Huang, Wen-Jun;Chen, Zhi-Peng;Liu, Li-Xia;Zhou, Yong-Gui;Wu, Bo;Jiang, Guo-Fang. And the article was included in Journal of Heterocyclic Chemistry in 2022.Category: indole-building-block This article mentions the following:

A facile method for the synthesis of pyrrolo[2,3-j]phenanthridines from indoleanilines and aldehydes in the presence of Broensted acid catalyst and benzoquinone oxidant were established. This approach featured excellent yields, high efficiency and a wide range of substrate scope. Mechanism studies exhibited that this reaction was a cascade process including acid-catalyzed condensation of indoleanilines with aldehydes, cyclization and oxidative aromatization. In the experiment, the researchers used many compounds, for example, 5-Bromo-2,3-dimethyl-1H-indole (cas: 4583-55-5Category: indole-building-block).

5-Bromo-2,3-dimethyl-1H-indole (cas: 4583-55-5) 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. 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.Category: indole-building-block

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