Tag: 200-300

The author of 《Structure-guided development of purine amide, hydroxamate, and amidoxime for the inhibition of non-small cell lung cancer》 were Huang, Meng-Ruo; Hsu, Yuan-Ling; Lin, Tzu-Chen; Cheng, Ting-Jen; Li, Ling-Wei; Tseng, Yu-Wei; Chou, Yu-shu; Liu, Jyung-Hurng; Pan, Szu-Hua; Fang, Jim-Min; Wong, Chi-Huey. And the article was published in European Journal of Medicinal Chemistry in 2019. Application In Synthesis of tert-Butyl (5-aminopentyl)carbamate The author mentioned the following in the article:

An 8-oxopurine-6-carboxamide compound, 2-(4-ethoxyphenyl)-9-(2-methoxyphenyl)-8-oxo-8,9-dihydro-7H-purine-6-carboxamide [869069-21-6], (1a) was previously identified as an inhibitor of non-small cell lung cancer (NSCLC). In this study, more than 30 purine-6-carboxamide derivatives with variations at the C2, N7, C8, and N9 positions were synthesized to investigate the structure-activity relationship as a basis for the construction of an advanced pharmacophore model. This model suggests that purine-6-hydroxamate and purine-6-amidoxime analogs could form more hydrogen bonds with a target protein to enhance the inhibitory activities against H1975 cells. Among the series of analogs, the hydroxamate, 2-(4-ethoxyphenyl)-9-(2-methoxyphenyl)-8-oxopurine-6(N-hydroxy)carboxamide [2124217-41-8] (17) and amidoxime, (Z)-2-(4-ethoxyphenyl)-N0-hydroxy-9-(2-methoxyphenyl)8-oxo-8,9-dihydro-7H-purine-6-carboximidamide (19a), exhibited excellent potency against H1975 cells (IC50 < 1.5 μM) and other lung cancer cells with either wild-type or mutated epidermal growth factor receptor (EGFR). Mouse experiments indicated that (17) and (19a) were efficient anticancer agents with no appreciable toxicity. The mechanisms of action for the induction of cell apoptosis were determined to involve microtubule fragmentation and p53-mediated signaling pathways. The results came from multiple reactions, including the reaction of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Application In Synthesis of tert-Butyl (5-aminopentyl)carbamate)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Application In Synthesis of tert-Butyl (5-aminopentyl)carbamate

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Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

In 2019,Iranian Journal of Pharmaceutical Research included an article by Dahiya, Rajiv; Singh, Sunil; Gupta, Sheeba Varghese; Sutariya, Vijaykumar B.; Bhatia, Deepak; Mourya, Rita; Chennupati, Suresh V.; Sharma, Ajay. HPLC of Formula: 7524-52-9. The article was titled 《First total synthesis and pharmacological potential of a plant based hexacyclopeptide》. The information in the text is summarized as follows:

A new bioactive proline-rich cyclohexapeptide – diandrine C (6), previously isolated from whole plant of Drymaria diandra (Caryophyllaceae), was synthesized through coupling reactions of tetrapeptide unit Boc-Gly-L-Pro-L-Tyr-L-Trp-OH with dipeptide unit L-ProGly-OMe using N,N-diisopropylcarbodiimide (DIPC) as the coupling agent, followed by cyclization of linear hexapeptide unit under alk. condition. Structure of cyclohexapeptide was confirmed by means of chem., and spectroscopic analyses and also was screened for its antimicrobial and anthelmintic properties. Bioevaluation results indicated that the newly synthesized hexacyclopeptide exhibited potent antimicrobial activity against Gram-neg. bacteria Pseudomonas aeruginosa, Klebsiella pneumoniae and pathogenic Candida albicans at 6 μg/mL. Moderate to good level of antihelmintic activity against three earthworm species Megascoplex konkanensis, Pontoscotex corethruses and Eudrilus eugeniae was also observed at concentration of 2 mg/mL. The experimental process involved the reaction of H-Trp-OMe.HCl(cas: 7524-52-9HPLC of Formula: 7524-52-9)

H-Trp-OMe.HCl(cas:7524-52-9) is one of amino acid derivatives. Amino acid derivatives represent an important category of skin penetration promoters. These compounds possess hydrophobic chains attached to an amino acid headgroup via a biodegradable ester bond. Due to the amphiphilic nature of these derivatives, it is possible for them to enter into the SC lipid barrier and significantly disorganize skin membrane lipids.HPLC of Formula: 7524-52-9

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

In 2019,European Journal of Inorganic Chemistry included an article by Syrgiannis, Zois; Trautwein, Guido; Calvaresi, Matteo; Modugno, Gloria; Zerbetto, Francesco; Carraro, Mauro; Prato, Maurizio; Bonchio, Marcella. Application of 7524-52-9. The article was titled 《Controlling Size-Dispersion of Single Walled Carbon Nanotubes by Interaction with Polyoxometalates Armed with a Tryptophan Tweezer》. The information in the text is summarized as follows:

A bis-tryptophan tweezer was installed on a polyoxometalate (POM) surface via a bis-amide covalent bond, yielding the enantiopure hybrid POM with C2 symmetry, as a result of the regioselective functionalization of decatungosilicate [γ-SiW10O36]8- at the lacunary site. The combined polyanionic and receptor properties are instrumental for a POM-driven solubilization and enrichment of single walled C nanotubes (SWCNTs) with diameter < 1.1 nm, as demonstrated by Raman and UV/visible-NIR evidence, in agreement with the calculated energetics of the tryptophan tweezer-SWCNT interaction. In the experiment, the researchers used H-Trp-OMe.HCl(cas: 7524-52-9Application of 7524-52-9)

H-Trp-OMe.HCl(cas:7524-52-9) is one of amino acid derivatives. Amino acid derivatives represent an important category of skin penetration promoters. These compounds possess hydrophobic chains attached to an amino acid headgroup via a biodegradable ester bond. Due to the amphiphilic nature of these derivatives, it is possible for them to enter into the SC lipid barrier and significantly disorganize skin membrane lipids.Application of 7524-52-9

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

In 2017,D’Errico, Stefano; Borbone, Nicola; Piccialli, Vincenzo; Di Gennaro, Elena; Zotti, Andrea; Budillon, Alfredo; Vitagliano, Carlo; Piccialli, Ilaria; Oliviero, Giorgia published 《Synthesis and Evaluation of the Antitumor Properties of a Small Collection of PtII Complexes with 7-Deazaadenosine as Scaffold》.European Journal of Organic Chemistry published the findings.Quality Control of tert-Butyl (5-aminopentyl)carbamate The information in the text is summarized as follows:

Herein the authors report on the synthesis and evaluation of the preliminary antitumor properties of a small collection of Pt(II) complexes in which a cisplatin-like unit is tethered to 7-deazaadenosine through linear alkyl chains (from two to six C atoms) installed at the purine C6 position. The complexation was performed by exploiting the reactivity of the bidentate amino ligands (R)- and (S)-2,3-diaminopropanoic acids (DAPA) attached to the end of the alkyl chain spacer. By varying the length of the alkyl chain and the chirality of the DAPA moiety the authors obtained 10 novel nucleoside-Pt complexes, the anticancer properties of which were evaluated against the A549 and Cal27 human cancer cell lines. In the experiment, the researchers used tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Quality Control of tert-Butyl (5-aminopentyl)carbamate)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Quality Control of tert-Butyl (5-aminopentyl)carbamate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

In 2016,Healy, Alan R.; Nikolayevskiy, Herman; Patel, Jaymin R.; Crawford, Jason M.; Herzon, Seth B. published 《A Mechanistic Model for Colibactin-Induced Genotoxicity》.Journal of the American Chemical Society published the findings.Safety of tert-Butyl (5-aminopentyl)carbamate The information in the text is summarized as follows:

Precolibactins and colibactins represent a family of natural products that are encoded by the clb gene cluster and are produced by certain commensal, extraintestinal, and probiotic E. coli. Clb+ E. coli induce megalocytosis and DNA double-strand breaks in eukaryotic cells, but paradoxically, this gene cluster is found in the probiotic Nissle 1917. Evidence suggests precolibactins are converted to genotoxic colibactins by colibactin peptidase (ClbP)-mediated cleavage of an N-acyl-D-Asn side chain, and all isolation efforts have employed ΔclbP strains to facilitate accumulation of precolibactins. It was hypothesized that colibactins form unsaturated imines that alkylate DNA by cyclopropane ring opening (2→3, Scheme 1). However, as no colibactins have been isolated, this hypothesis has not been tested exptl. Addnl., precolibactins A-C (7-9, Figure 1) contain a pyridone that cannot generate the unsaturated imines that form the basis of this hypothesis. To resolve this, we prepared 13 synthetic colibactin derivatives and evaluated their DNA binding and alkylation activity. We show that unsaturated imines, but not the corresponding pyridone derivatives, potently alkylate DNA. The imine, unsaturated lactam, and cyclopropane are essential for efficient DNA alkylation. A cationic residue enhances activity. These studies suggest that precolibactins containing a pyridone are not responsible for the genotoxicity of the clb cluster. Instead, we propose that these are off-pathway fermentation products produced by a facile double cyclodehydration route that manifests in the absence of viable ClbP. The results presented herein provide a foundation to begin to connect metabolite structure with the disparate phenotypes associated with clb+ E. coli. After reading the article, we found that the author used tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Safety of tert-Butyl (5-aminopentyl)carbamate)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Safety of tert-Butyl (5-aminopentyl)carbamate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

《Synthesis and in vitro evaluation of vanillin derivatives as multi-target therapeutics for the treatment of Alzheimer’s disease》 was written by Blaikie, Laura; Kay, Graeme; Kong Thoo Lin, Paul. Product Details of 51857-17-1This research focused onvanillin naphthalimido phthalimido preparation Alzheimer agent mol modeling; cholinesterase inhibitor naphthalimido phthalimido vanillin; Alzheimer’s disease; Antioxidant; Binding conformation; Cholinesterase inhibitor; Multi-target strategy; Vanillin derivatives. The article conveys some information:

A number of novel naphthalimido and phthalimido vanillin derivatives were synthesized, and evaluated as antioxidants and cholinesterase inhibitors in vitro. Antioxidant activity was assessed using DPPH, FRAP, and ORAC assays. All compounds demonstrated enhanced activity compared to the parent compound, vanillin. They also exhibited BuChE selectivity in Ellman’s assay. A lead compound, naphthalimido derivative I, was identified and displayed strong antioxidant activity (IC50 of 16.67μM in the DPPH assay, a 25-fold increase in activity compared to vanillin in the FRAP assay, and 9.43 TE in the ORAC assay). Furthermore, I exhibited potent BuChE selectivity, with an IC50 of 0.27μM which was around 53-fold greater than the corresponding AChE inhibitory activity. Mol. modeling studies showed that mols. with bulkier groups, as in I, exhibited better BuChE selectivity. This work provides a promising basis for the development of multi-target hybrid compounds based on vanillin as potential AD therapeutics. After reading the article, we found that the author used N-Boc-1,6-Diaminohexane(cas: 51857-17-1Product Details of 51857-17-1)

N-Boc-1,6-Diaminohexane(cas: 51857-17-1) is used to prepare 1,3-Bis[6-(Boc-amino)hexyl]urea by reacting with carbonyl dichloride in the presence of triethylamine. Further, it is used as a reagent for the introduction of a C6-spacer.Product Details of 51857-17-1

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

《Synthesis and crystal structure differences between fully and partially fluorinated β-diketonate metal (Co2+, Ni2+, and Cu2+) complexes》 was published in International Journal of Inorganic Chemistry in 2011. These research results belong to Hori, Akiko; Mizutani, Masaya. Synthetic Route of C9H5F5O2 The article mentions the following:

Coordination complexes, [Co2(1)4(H2O)2] (2), [Ni2(1)4(H2O)2] (3), and [Cu(1)2] (4), by using an asym. and partially fluorinated 3-hydroxy-3-pentafluorophenyl-1-phenyl-2-propen-1-one (H1) were prepared, and the structures were studied to compare with the corresponding fully fluorinated complexes of [Co2(5)4(H2O)2] (6), [Ni2(5)4(H2O)2] (7), and [Cu(5)2] (8) with bis(pentafluorobenzoyl)methane (H5) and to understand the fluorine-substituted effects. While the coordination mode of the partially fluorinated complexes was quite similar to the fully fluorinated complexes, the intra- and inter-mol. π-interactions of the ligand moieties were highly influenced by the fluorination effects; the arene-perfluoroarene interactions were observed in complexes 2 and 3 as a reason of the dinucleation. The authors describe detail structures of the protonated form of the ligand, H1, and complexes 2-4 by x-ray crystallog. studies. In the experiment, the researchers used Ethyl 2,3,4,5,6-pentafluorobenzoate(cas: 4522-93-4Synthetic Route of C9H5F5O2)

Ethyl 2,3,4,5,6-pentafluorobenzoate(cas: 4522-93-4) belongs to esters.Synthetic Route of C9H5F5O2 They are important in biology, being one of the main classes of lipids and comprising the bulk of animal fats and vegetable oils.Esters typically have a pleasant smell; those of low molecular weight are commonly used as fragrances and are found in essential oils and pheromones.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Recommanded Product: 51644-96-3In 2017 ,《Solvent-free mechanochemical deprotection of N-Boc group》 was published in International Journal of Organic Chemistry. The article was written by Djud, Mateja; Margetic, Davor. The article contains the following contents:

Boc protection group could be readily removed in a very mild mechanochem. conditions. In a short reaction time, ball milling of Boc-protected amines with p-toluenesulfonic acid in solvent-free conditions affords corresponding amine p-TsOH salts. In addition to this study using tert-Butyl (5-aminopentyl)carbamate, there are many other studies that have used tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Recommanded Product: 51644-96-3) was used in this study.

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Recommanded Product: 51644-96-3

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Patinote, Cindy; Deleuze-Masquefa, Carine; Kaddour, Kamel Hadj; Vincent, Laure-Anais; Larive, Romain; Zghaib, Zahraa; Guichou, Jean-Francois; Assaf, Mona Diab; Cuq, Pierre; Bonnet, Pierre-Antoine published an article in 2021. The article was titled 《Imidazo[1,2-a]quinoxalines for melanoma treatment with original mechanism of action》, and you may find the article in European Journal of Medicinal Chemistry.Reference of N-Boc-1,6-Diaminohexane The information in the text is summarized as follows:

The malignant transformation of melanocytes causes several thousand deaths each year, making melanoma an important public health concern. Melanoma is the most aggressive skin cancer, which incidence has regularly increased over the past decades. We described here the preparation of new compounds based on the 1-(3,4-dihydroxyphenyl)imidazo[1,2-a]quinoxaline structure. Different positions of the quinoxaline moiety were screened to introduce novel substituents in order to study their influence on the biol. activity. Several alkylamino or alkyloxy groups were also considered to replace the methylamine of our first generation of Imiqualines. Imidazo[1,2-a]pyrazine derivatives were also designed as potential minimal structure. The investigation on A375 melanoma cells displayed interesting in vitro low nanomolar cytotoxic activity. Among them, 9d (EAPB02303) is particularly remarkable since it is 20 times more potent than vemurafenib, the reference clin. therapy used on BRAF mutant melanoma. Contrary to the first generation, EAPB02303 does not inhibit tubulin polymerization, as confirmed by an in vitro assay and a mol. modelisation study. The mechanism of action for EAPB02303 highlighted by a transcriptomic anal. is clearly different from a panel of 12 well-known anticancer drugs. In vivo EAPB02303 treatment reduced tumor size and weight of the A375 human melanoma xenografts in a dose-dependent manner, correlated with a low mitotic index but not with necrosis. The experimental part of the paper was very detailed, including the reaction process of N-Boc-1,6-Diaminohexane(cas: 51857-17-1Reference of N-Boc-1,6-Diaminohexane)

N-Boc-1,6-Diaminohexane(cas: 51857-17-1) is a compound useful in organic synthesis used in the preparation of mixed self-assembled monolayers (SAMs) that resist adsorption of proteins using the reaction of amines with a SAM that presents interchain carboxylic anhydride groupsReference of N-Boc-1,6-Diaminohexane

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Ruiz-Santaquiteria, Marta; Illescas, Beatriz M.; Abdelnabi, Rana; Boonen, Arnaud; Mills, Alberto; Marti-Mari, Olaia; Noppen, Sam; Neyts, Johan; Schols, Dominique; Gago, Federico; San-Felix, Ana; Camarasa, Maria-Jose; Martin, Nazario published an article in 2021. The article was titled 《Multivalent Tryptophan- and Tyrosine-Containing [60]Fullerene Hexa-Adducts as Dual HIV and Enterovirus A71 Entry Inhibitors》, and you may find the article in Chemistry – A European Journal.HPLC of Formula: 7524-52-9 The information in the text is summarized as follows:

Unprecedented 3D hexa-adducts of [60]fullerene peripherally decorated with twelve tryptophan (Trp) or tyrosine (Tyr) residues have been synthesized. Studies on the antiviral activity of these novel compounds against HIV and EV71 reveal that they are much more potent against HIV and equally active against EV71 than the previously described dendrimer prototypes AL-385 and AL-463, which possess the same number of Trp/Tyr residues on the periphery but attached to a smaller and more flexible pentaerythritol core. These results demonstrate the relevance of the globular 3D presentation of the peripheral groups (Trp/Tyr) as well as the length of the spacer connecting them to the central core to interact with the viral envelopes, particularly in the case of HIV, and support the hypothesis that [60]fullerene can be an alternative and attractive biocompatible carbon-based scaffold for this type of highly sym. dendrimers. In addition, the functionalized fullerenes here described, which display twelve peripheral neg. charged indole moieties on their globular surface, define a new and versatile class of compounds with a promising potential in biomedical applications. The experimental process involved the reaction of H-Trp-OMe.HCl(cas: 7524-52-9HPLC of Formula: 7524-52-9)

H-Trp-OMe.HCl(cas:7524-52-9) is one of amino acid derivatives. Amino acid derivatives represent an important category of skin penetration promoters. These compounds possess hydrophobic chains attached to an amino acid headgroup via a biodegradable ester bond. Due to the amphiphilic nature of these derivatives, it is possible for them to enter into the SC lipid barrier and significantly disorganize skin membrane lipids.HPLC of Formula: 7524-52-9

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics