Category: 622-40-2

Kim, Jinwoong published the artcileComputer-aided design and synthesis of 3-carbonyl-5-phenyl-1H-pyrazole as highly selective and potent BRAFV600E and CRAF inhibitor, Product Details of C6H13NO2, the publication is Journal of Enzyme Inhibition and Medicinal Chemistry (2019), 34(1), 1314-1320, database is CAplus and MEDLINE.

BRAF belongs to the upstream portion of the MAPK pathway, which is involved in cell proliferation and survival. When mutations occur in BRAF, downstream MEK and ERK are phosphorylated irresp. of RAS, resulting in melanoma-like cancer. Over the years, small mols. targeting BRAFV600E have been discovered to be very effective melanoma drugs, but they are known to cause the BRAF paradox. Recently, it was shown that this paradox is caused by the heterodimer phenomenon of BRAF/CRAF. Here, we suggest one method by which paradoxical activation can be avoided by selectively inhibiting BRAFV600E and CRAF but not wild-type BRAF. From previous report of N-(3-(3-alkyl-1H-pyrazol-5-yl) phenyl) aryl amide as a selective inhibitor of BRAFV600E and CRAF, we present compounds that offer enhanced selectivity and efficacy with the aid of mol. modeling.

Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C6H13NO2, Product Details of C6H13NO2.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Payne, China M. published the artcile5-Bromo-norborn-2-en-7-one derivatives as a carbon monoxide source for palladium catalyzed carbonylation reactions, HPLC of Formula: 622-40-2, the publication is RSC Advances (2019), 9(53), 30736-30740, database is CAplus and MEDLINE.

Norbornenone derivative, obtained from the reaction of 2,5-dimethyl-3,4-diphenylcyclopentadienone dimer with bromomaleic anhydride, provided an excellent base-triggered source of carbon monoxide for palladium-catalyzed carbonylation reactions. Aminocarbonylation, ketoamide synthesis, and Suzuki-Miyaura reactions of aryl iodides carried out in a two-chamber reaction vessel gave good to excellent yields of carbonylated products.

RSC Advances published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C6H13NO2, HPLC of Formula: 622-40-2.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Xia, Xi published the artcileSynthesis of diosgenyl quaternary ammonium derivatives and their antitumor activity, Computed Properties of 622-40-2, the publication is Steroids (2021), 108774, database is CAplus and MEDLINE.

Giosgenin is a naturally steroidal saponin exhibiting a variety of biol. activities including antitumor ones. A series of novel diosgenyl quaternary ammonium derivatives were designed and synthesized to develop potential anti-tumor agents in our research. All novel derivatives were characterized by ¹H NMR, ¹³C NMR and HR-MS, and evaluated for their in vitro anti-proliferative activities using MTT assay. The human cancer cell lines were A549 (human lung cancer cell), H1975 (human lung adenocarcinoma cell), A431 (human skin squamous cell carcinoma), HCT-116 (human colorectal adenocarcinoma cell), Aspc-1 (human metastatic pancreatic cancer cell), Ramos (human B lymphoma cell), HBE (human bronchial epithelioid cell) and LO2 (human normal hepatocyte).

Steroids published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C8H13NO3, Computed Properties of 622-40-2.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Guo, Qiumei published the artcileMorpholinyl dendrimer phthalocyanine: synthesis, photophysical properties and photoinduced intramolecular electron transfer, Quality Control of 622-40-2, the publication is Dalton Transactions (2018), 47(37), 13164-13170, database is CAplus and MEDLINE.

A novel series of morpholinyl dendrimer phthalocyanines were synthesized. Their structures were characterized by ¹H NMR, IR, elemental anal., ESI-MS as well as MALDI-TOF MS. The photophys. properties of these phthalocyanines were studied by UV/visible and fluorescence spectroscopic methods. The photophys. properties of these dendrimer phthalocyanines exhibited dependence on the number of morpholinyl groups and the central ion. The photoinduced intramol. electron transfer from the morpholinyl groups to the phthalocyanine ring was evidenced by the remarkably quenched fluorescence intensity and shortened lifetime of the silicon phthalocyanine. This difference in photoinduced intramol. electron transfer effect for axially and peripherally substituted morpholinyl dendrimer phthalocyanines was also studied. Besides, introduction of morpholinyl groups on the dendrimer structure could enhance water solubility as well as increase the singlet oxygen quantum yield.

Dalton Transactions published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C6H13NO2, Quality Control of 622-40-2.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Islam, Koushikul published the artcileStructural Modifications and Biological Evaluations of Rift Valley Fever Virus Inhibitors Identified from Chemical Library Screening, Recommanded Product: 2-Morpholinoethanol, the publication is ACS Omega (2022), 7(8), 6854-6868, database is CAplus and MEDLINE.

The Rift Valley fever virus (RVFV) is an emerging high-priority pathogen endemic in Africa with pandemic potential. There is no specific treatment or approved antiviral drugs for the RVFV. We previously developed a cell-based high-throughput assay to screen small mols. targeting the RVFV and identified a potential effective antiviral compound (1-N-(2-(biphenyl-4-yloxy)ethyl)propane-1,3-diamine) as a lead compound Here, we investigated how structural modifications of the lead compound affected the biol. properties and the antiviral effect against the RVFV. We found that the length of the 2-(3-aminopropylamino)ethyl chain of the compound was important for the compound to retain its antiviral activity. The antiviral activity was similar when the 2-(3-aminopropylamino)ethyl chain was replaced with a Bu piperazine chain. However, we could improve the cytotoxicity profile of the lead compound by changing the Ph piperazine linker from the para-position (compound 9a) to the meta-position (compound 13a). Results from time-of-addition studies suggested that compound 13a might be active during virus post-entry and/or the replication phase of the virus life cycle and seemed to affect the K⁺ channel. The modifications improved the properties of our lead compound, and our data suggest that 13a (I) is a promising candidate to evaluate further as a therapeutic agent for RVFV infection.

ACS Omega published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C6H13NO2, Recommanded Product: 2-Morpholinoethanol.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Shu, Bing published the artcileSyntheses and evaluation of new acridone derivatives for selective binding of oncogene c-myc promoter i-motifs in gene transcriptional regulation, SDS of cas: 622-40-2, the publication is Chemical Communications (Cambridge, United Kingdom) (2018), 54(16), 2036-2039, database is CAplus and MEDLINE.

We synthesized a series of acridone derivatives for specific binding ligands of i-motifs. Subsequent evaluations showed that B19 (I) could selectively bind to and stabilize the c-myc promoter i-motif without significant binding to the G-quadruplex and duplex DNA. This caused down-regulation of c-myc transcription and expression, resulting in tumor cell apoptosis.

Chemical Communications (Cambridge, United Kingdom) published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C6H4ClNO2, SDS of cas: 622-40-2.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Di Profio, Pietro published the artcileChemoinformatic design of amphiphilic molecules for methane hydrate inhibition, Name: 2-Morpholinoethanol, the publication is Journal of Chemometrics (2018), 32(6), n/a, database is CAplus.

Cationic surfactants and other low mol. weight compounds are known to inhibit nucleation and agglomeration of methane hydrates. In particular, tetralkylammonium salts are kinetic hydrate inhibitors; ie, they reduce the rate of hydrate formation. This work relates to the in-silico determination of structural features of mols. modulating methane hydrate formation, as found exptl., and the prediction of novel structures to be tested as candidate inhibitors. Exptl. data for each mol. are the amount of absorbed methane. By inserting these numerical values into a chemoinformatic model, it was possible to find a mutual correlation between structural features and inhibition properties. A maximum amount of information is extracted from the structural features and exptl. variables, and a model is generated to explain the relationship therebetween. Chemometric anal. was performed by using the software package Volsurf+ with the aim of finding a primary correlation between surfactant structures and their properties. Exptl. parameters (pressure, temperature, and concentration) were further processed through an optimization procedure. A careful study of the chemometric anal. responses and the numerical descriptors of tested surfactants allowed to define the features of a good inhibitor, as far as the amount of absorbed gas is concerned. An external prediction is finally made to project external compounds, whose structures and critical micellar concentration are known, in a statistical model, to predict the inhibition properties of a particular mol. in advance of synthesis and testing. This method allowed to find novel amphiphilic mols. for testing as candidate inhibitors in flow-assurance.

Journal of Chemometrics published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C6H13NO2, Name: 2-Morpholinoethanol.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Smolinski, Michael P. published the artcileDiscovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361), Formula: C6H13NO2, the publication is Journal of Medicinal Chemistry (2018), 61(11), 4704-4719, database is CAplus and MEDLINE.

The discovery of potent, peptide site directed, tyrosine kinase inhibitors has remained an elusive goal. Herein we describe the discovery of two such clin. candidates that inhibit the tyrosine kinase Src. Compound 1 is a phase 3 clin. trial candidate that is likely to provide a first in class topical treatment for actinic keratosis (AK) with good efficacy and dramatically less toxicity compared to existing standard therapy. Compound 2 is a phase 1 clin. trial candidate that is likely to provide a first in class treatment of malignant glioblastoma and induces 30% long-term complete tumor remission in animal models. The discovery strategy for these compounds iteratively utilized mol. modeling, along with the synthesis and testing of increasingly elaborated proof of concept compounds, until the final clin. candidates were arrived at. This was followed with mechanism of action (MOA) studies that revealed tubulin polymerization inhibition as the second MOA.

Journal of Medicinal Chemistry published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C22H12F6O6S2, Formula: C6H13NO2.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

De Gasparo, Raoul published the artcileBiological Evaluation and X-ray Co-crystal Structures of Cyclohexylpyrrolidine Ligands for Trypanothione Reductase, an Enzyme from the Redox Metabolism of Trypanosoma, Safety of 2-Morpholinoethanol, the publication is ChemMedChem (2018), 13(9), 957-967, database is CAplus and MEDLINE.

The tropical diseases human African trypanosomiasis, Chagas disease, and the various forms of leishmaniasis are caused by parasites of the family of trypanosomatids. These protozoa possess a unique redox metabolism based on trypanothione and trypanothione reductase (TR), making TR a promising drug target. We report the optimization of properties and potency of cyclohexylpyrrolidine inhibitors of TR by structure-based design. The best inhibitors were freely soluble and showed competitive inhibition constants (K_i) against Trypanosoma (T.) brucei TR and T. cruzi TR and in vitro activities (half-maximal inhibitory concentration, IC₅₀) against these parasites in the low micromolar range, with high selectivity against human glutathione reductase. X-ray co-crystal structures confirmed the binding of the ligands to the hydrophobic wall of the “mepacrine binding site” with the new, solubility-providing vectors oriented toward the surface of the large active site.

ChemMedChem published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C6H13NO2, Safety of 2-Morpholinoethanol.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Meshram, Anju published the artcileCharacterization of Pyrrolidine Alkaloids of Epipremnum aureum for Their Antitermite Activity Against Subterranean Termites with SEM Studies, Recommanded Product: 2-Morpholinoethanol, the publication is Proceedings of the National Academy of Sciences, India, Section B: Biological Sciences (2019), 89(1), 53-62, database is CAplus.

Epipremnum aureum (Linden and Andre) G. S. Bunting (E. aureum) is an ornamental foliage rich in phytoconstituents and serves as a potential source of bioactive compounds possessing beneficial biol. activities. The present study was carried out to isolate the pyrrolidine alkaloids of leaves with in vitro antitermite and antirepellant efficacy on paper and soil by direct-choice and no-choice assay. Spectrometric anal. of alkaloid fractions via UV-visible spectroscopy (UV-VIS), Fourier transform IR spectroscopy (FTIR) and gas chromatog. mass spectrometry (GC-MS) helped in the characterization of pyrrolidine alkaloids. Superior antitermite activities were observed, associated with high levels of 5-Oxoproline as compare to Me 5-oxo-2-pyrrolidinecarboxylate. Presence of higher contents of 4-Morpholineethanol showed effective antitermite activity and even low levels of 3-Amino-4-Hydroxybutanoic acid and 1H-1,2,4-Triazol-3-amine, N-methyl- also exposed significant activities for repellence and mortality of termites. Repellence and percentage mortality of termites by these alkaloid fractions were similar in results when compared with the standard alkaloid Nicotine and chem. termiticide Monocrotophos. These findings were also supported by SEM studies. Pyrrolidine alkaloids present in E. aureum have exposed strong in vitro antitermite and antirepellant activities against subterranean termites Odontotermes obesus. These findings strongly support the use of E. aureum to bear potential termiticidal properties, however further details need to be carried out.

Proceedings of the National Academy of Sciences, India, Section B: Biological Sciences published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C6H13NO2, Recommanded Product: 2-Morpholinoethanol.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts