Day: November 21, 2022

Min, Hyun Su published the artcileChemical gas-generating nanoparticles for tumor-targeted ultrasound imaging and ultrasound-triggered drug delivery, Computed Properties of 19444-84-9, the publication is Biomaterials (2016), 57-70, database is CAplus and MEDLINE.

Although there is great versatility of ultrasound (US) technologies in the real clin. field, one main tech. challenge is the compromising of high quality of echo properties and size engineering of ultrasound contrast agents (UCAs); a high echo property is offset by reducing particle size. Herein, a new strategy for overcoming the dilemma by devising chem. gas (CO₂) generating carbonate copolymer nanoparticles (Gas-NPs), which are clearly distinguished from the conventional gas-encapsulated micro-sized UCAs. More importantly, Gas-NPs could be readily engineered to strengthen the desirable in vivo physicochem. properties for nano-sized drug carriers with higher tumor targeting ability, as well as the high quality of echo properties for tumor-targeted US imaging. In tumor-bearing mice, anticancer drug-loaded Gas-NPs showed the desirable theranostic functions for US-triggered drug delivery, even after i.v. injection. In this regard, and as demonstrated in the aforementioned study, our technol. could serve a highly effective platform in building theranostic UCAs with great sophistication and therapeutic applicability in tumor-targeted US imaging and US-triggered drug delivery.

Biomaterials published new progress about 19444-84-9. 19444-84-9 belongs to tetrahydrofurans, auxiliary class Tetrahydrofuran,Ester,Alcohol, name is 3-Hydroxydihydrofuran-2(3H)-one, and the molecular formula is C4H6O3, Computed Properties of 19444-84-9.

Referemce:
https://en.wikipedia.org/wiki/Tetrahydrofuran,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Yu, Wenyu published the artcileBromo-deaza-SAH: A potent and selective DOT1L inhibitor, Application of 1-(3-((((2R,3S,4R,5R)-5-(4-Amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)(isopropyl)amino)propyl)-3-(4-(tert-butyl)phenyl)urea, the publication is Bioorganic & Medicinal Chemistry (2013), 21(7), 1787-1794, database is CAplus and MEDLINE.

Chem. inhibition of proteins involved in chromatin-mediated signaling is an emerging strategy to control chromatin compaction with the aim to reprogram expression networks to alter disease states. Protein methyltransferases constitute one of the protein families that participate in epigenetic control of gene expression, and represent a novel therapeutic target class. Recruitment of the protein lysine methyltransferase DOT1L at aberrant loci is a frequent mechanism driving acute lymphoid and myeloid leukemias, particularly in infants, and pharmacol. inhibition of DOT1L extends survival in a mouse model of mixed lineage leukemia. A better understanding of the structural chem. of DOT1L inhibition would accelerate the development of improved compounds Here, we report that the addition of a single halogen atom at a critical position in the cofactor product S-adenosylhomocysteine (SAH, an inhibitor of SAM-dependent methyltransferases) results in an 8-fold increase in potency against DOT1L, and reduced activities against other protein and non-protein methyltransferases. We solved the crystal structure of DOT1L in complex with Bromo-deaza-SAH and rationalized the observed effects. This discovery reveals a simple strategy to engineer selectivity and potency towards DOT1L into the adenosine scaffold of the cofactor shared by all methyltransferases, and can be exploited towards the development of clin. candidates against mixed lineage leukemia.

Bioorganic & Medicinal Chemistry published new progress about 1338466-77-5. 1338466-77-5 belongs to tetrahydrofurans, auxiliary class Epigenetics,Histone Methyltransferase, name is 1-(3-((((2R,3S,4R,5R)-5-(4-Amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)(isopropyl)amino)propyl)-3-(4-(tert-butyl)phenyl)urea, and the molecular formula is C7H7IN2O, Application of 1-(3-((((2R,3S,4R,5R)-5-(4-Amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)(isopropyl)amino)propyl)-3-(4-(tert-butyl)phenyl)urea.

Referemce:
https://en.wikipedia.org/wiki/Tetrahydrofuran,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Coutinho, Nathalia M. published the artcileProcessing chocolate milk drink by low-pressure cold plasma technology, Related Products of tetrahydrofurans, the publication is Food Chemistry (2019), 276-283, database is CAplus and MEDLINE.

This study aimed to evaluate the effect of the process time (5, 10, and 15 min) and flow rate (10, 20, and 30 mL/min) of cold plasma technol. on physio-chem. characteristics (pH), bioactive compounds (DPPD, Total Phenolic Compounds, ACE-inhibitory activity values), fatty acid composition, and volatile compounds profile of chocolate milk drink. The mild (lower flow rate and process time) and more severe (higher flow rate and process time) conditions led to a reduction of the bioactive compounds (total phenolic compounds and ACE-inhibitory activity), changes in fatty acid composition (increased saturated fatty acid and decreased monounsaturated fatty acid and polyunsaturated fatty acid), less favorable health indexes (higher atherogenic, thrombogenic and hypercholesterolemic saturated fatty acids and lower desired fatty acids), and lower number of volatile compounds In contrast, in intermediate cold plasma conditions, an adequate concentration of bioactive compounds, fatty acid composition, and health indexes, and increased number of volatile compounds (ketones, esters, and lactones) were observed Overall, cold plasma technol. has proven to be an interesting alternative to chocolate milk drinks, being of paramount importance the study of the cold plasma process parameters.

Food Chemistry published new progress about 19444-84-9. 19444-84-9 belongs to tetrahydrofurans, auxiliary class Tetrahydrofuran,Ester,Alcohol, name is 3-Hydroxydihydrofuran-2(3H)-one, and the molecular formula is C4H6O3, Related Products of tetrahydrofurans.

Referemce:
https://en.wikipedia.org/wiki/Tetrahydrofuran,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Monteiro, Sara H. M. C. published the artcileEffects of ultrasound energy density on the non-thermal pasteurization of chocolate milk beverage, Recommanded Product: 3-Hydroxydihydrofuran-2(3H)-one, the publication is Ultrasonics Sonochemistry (2018), 1-10, database is CAplus and MEDLINE.

This study presents the emerging high-intensity ultrasound (HIUS) processing as a non-thermal alternative to high-temperature short-time pasteurization (HTST). Chocolate milk beverage (CMB) was subjected to different ultrasound energy densities (0.3-3.0 kJ/cm³), as compared to HTST pasteurization (72°C/15 s) aimed to verify the effect of the HIUS processing on the microbiol. and physicochem. characteristics of the beverage. The application of HIUS at an energy d. of 3.0 kJ/cm³ was able to reduce 3.56 ± 0.02 logarithmic cycles in the total aerobic counts. In addition, the ultrasound energy d. affected the phys. properties of the beverage as the size distribution of fat globule and rheol. behavior, as well as the chem. properties such as antioxidant activity, ACE inhibitory activity, fatty acid profile, and volatile profile. In general, the different energetic densities used as a non-thermal method of pasteurization of CMB were more effective when compared to the conventional pasteurization by HTST, since they improved the microbiol. and physicochem. quality, besides preserving the bioactive compounds and the nutritional quality of the product.

Ultrasonics Sonochemistry published new progress about 19444-84-9. 19444-84-9 belongs to tetrahydrofurans, auxiliary class Tetrahydrofuran,Ester,Alcohol, name is 3-Hydroxydihydrofuran-2(3H)-one, and the molecular formula is C4H6O3, Recommanded Product: 3-Hydroxydihydrofuran-2(3H)-one.

Referemce:
https://en.wikipedia.org/wiki/Tetrahydrofuran,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Efimtseva, Ekaterina V. published the artcileSynthesis and Conformational Properties of O-β-D-Ribofuranosyl-(1”-2′)-guanosine and (Adenosine)-5”-phosphate, Recommanded Product: N-(9-((6aR,8R,9R,9aS)-9-Hydroxy-2,2,4,4-tetraisopropyltetrahydro-6H-furo[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl)-6-oxo-6,9-dihydro-1H-purin-2-yl)isobutyramide, the publication is Nucleosides, Nucleotides & Nucleic Acids (2003), 22(5-8), 1109-1111, database is CAplus and MEDLINE.

The efficient synthesis of Grp and Arp, minor tRNA components, has been developed. According to NMR studies and mol. modeling these mols. are rather flexible and show free rotation around the O- and N-glycosidic bonds.

Nucleosides, Nucleotides & Nucleic Acids published new progress about 87865-78-9. 87865-78-9 belongs to tetrahydrofurans, auxiliary class Nucleosides and Nucleotides,Nucleoside Analogues, name is N-(9-((6aR,8R,9R,9aS)-9-Hydroxy-2,2,4,4-tetraisopropyltetrahydro-6H-furo[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl)-6-oxo-6,9-dihydro-1H-purin-2-yl)isobutyramide, and the molecular formula is C26H45N5O7Si2, Recommanded Product: N-(9-((6aR,8R,9R,9aS)-9-Hydroxy-2,2,4,4-tetraisopropyltetrahydro-6H-furo[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl)-6-oxo-6,9-dihydro-1H-purin-2-yl)isobutyramide.

Referemce:
https://en.wikipedia.org/wiki/Tetrahydrofuran,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Efimtseva, Ekaterina V. published the artcileSynthesis and properties of O-β-D-ribofuranosyl-(1”→2′)-guanosine-5”-O-phosphate and its derivatives, Related Products of tetrahydrofurans, the publication is Helvetica Chimica Acta (2003), 86(2), 504-514, database is CAplus.

The efficient synthesis of O-β-D-ribofuranosyl-(1” → 2′)-guanosine-5”-O-phosphate and O-β-D-ribofuranosyl-(1”→2′)-adenosine-5”-O-phosphate, minor tRNA components, have been developed, and their conformational properties were examined by NMR spectroscopy.

Helvetica Chimica Acta published new progress about 87865-78-9. 87865-78-9 belongs to tetrahydrofurans, auxiliary class Nucleosides and Nucleotides,Nucleoside Analogues, name is N-(9-((6aR,8R,9R,9aS)-9-Hydroxy-2,2,4,4-tetraisopropyltetrahydro-6H-furo[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl)-6-oxo-6,9-dihydro-1H-purin-2-yl)isobutyramide, and the molecular formula is C26H45N5O7Si2, Related Products of tetrahydrofurans.

Referemce:
https://en.wikipedia.org/wiki/Tetrahydrofuran,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Chakraborty, Amit published the artcileDisulfide-based protecting groups for the cysteine side chain, Formula: C5H10OS, the publication is Organic Letters (2020), 22(24), 9644-9647, database is CAplus and MEDLINE.

Two new disulfide-based protecting groups (SIT and MOT) (I and II) are proposed for Cys thiol in the substitution of StBu, which is often difficult to remove. Both groups are based on a secondary thiol with a branched point in the β-position for an efficient modulation of its lability and/or stability. This unique structure allows them to be fully compatible with Fmoc/tBu SPPS (Fmoc = 9-fluorenylmethoxycarbonyl). At the end of the synthesis, these groups are removed in a straightforward manner with dithiothreitol with some H₂O.

Organic Letters published new progress about 57124-87-5. 57124-87-5 belongs to tetrahydrofurans, auxiliary class Tetrahydrofuran,Thiol, name is 2-Methyl-3-tetrahydrofuranthiol, and the molecular formula is C5H10OS, Formula: C5H10OS.

Referemce:
https://en.wikipedia.org/wiki/Tetrahydrofuran,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Niu, Ningning published the artcileBromodomain and Extra-terminal (BET) Protein Inhibitors Suppress Chondrocyte Differentiation and Restrain Bone Growth, Product Details of C28H41N7O4, the publication is Journal of Biological Chemistry (2016), 291(52), 26647-26657, database is CAplus and MEDLINE.

Small mol. inhibitors for bromodomain and extra-terminal (BET) proteins have recently emerged as potential therapeutic agents in clin. trials for various cancers. However, to date, it is unknown whether these inhibitors have side effects on bone structures. Here, we report that inhibition of BET bromodomain proteins may suppress chondrocyte differentiation and restrain bone growth. We generated a luciferase reporter system using the chondrogenic cell line ATDC5 in which the luciferase gene was driven by the promoter of Col2a1, an elementary collagen of the chondrocyte. The Col2a1-luciferase ATDC5 system was used for rapidly screening both activators and repressors of human collagen Col2a1 gene expression, and we found that BET bromodomain inhibitors reduce the Col2a1-luciferase. Consistent with the luciferase assay, BET inhibitors decrease the expression of Col2a1. Furthermore, we constructed a zebrafish line in which the enhanced green fluorescent protein (EGFP) expression was driven by col2a1 promoter. The transgenic (col2a1-EGFP) zebrafish line demonstrated that BET inhibitors I-BET151 and (+)-JQ1 may affect EGFP expression in zebrafish. Furthermore, we found that I-BET151 and (+)-JQ1 may affect chondrocyte differentiation in vitro and inhibit zebrafish growth in vivo. Mechanistic anal. revealed that BET inhibitors influenced the depletion of RNA polymerase II from the Col2a1 promoter. Collectively, these results suggest that BET bromodomain inhibition may have side effects on skeletal bone structures.

Journal of Biological Chemistry published new progress about 1338466-77-5. 1338466-77-5 belongs to tetrahydrofurans, auxiliary class Epigenetics,Histone Methyltransferase, name is 1-(3-((((2R,3S,4R,5R)-5-(4-Amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)(isopropyl)amino)propyl)-3-(4-(tert-butyl)phenyl)urea, and the molecular formula is C28H41N7O4, Product Details of C28H41N7O4.

Referemce:
https://en.wikipedia.org/wiki/Tetrahydrofuran,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Premkumar, Kavitha published the artcileIdentification of EPZ004777 and FG2216 as inhibitors of TGF-β1 induced Treg cells by screening a library of epigenetic compounds, Computed Properties of 1338466-77-5, the publication is Life Sciences (2022), 120643, database is CAplus and MEDLINE.

Regulatory T cells play an essential role in immune tolerance and homeostasis. Their long-term stability depends on epigenetic modifications and identification of small mol. modulators of Treg differentiation therefore has many applications. In this study, we performed a novel functional screen of an epigenetic compound library to identify compounds that can modulate generation of TGF-β1 induced T regulatory cells. A screening strategy based on IFN-γ ELISA was designed to screen epigenetic compound library. Effect of hit compounds on Treg phenotype and function was assessed by RT-PCR, flow cytometry and suppression assays. TGF-β signalling proteins were assayed by western blotting. Chromatin Immunoprecipitation (ChIP) assay was used to assess epigenetic modifications at Foxp3 gene locus. We screened 160 compounds to identify hits capable of reversing TGF-β induced inhibition of IFN-γ production in activated spleen cells and CD4+ T cells. Two compounds EPZ004777 and FG-2216 consistently reversed TGF-β1 iTregs in terms of (a) differentiation of naive T cells into CD4+CD25+Foxp3+Treg cells, (b) Foxp3 target gene expression and (c) Treg suppressive function without affecting TGF-β downstream signalling. ChIP assay revealed that the compounds were able to reverse – TGF- β mediated decrease in epigenetic marks H3K27me3 and 5-mC and an increase in epigenetic marks H3K4me3 and H3K27Ac in the promoter and conserved non coding sequence (CNS1) regions of the Foxp3 gene. EPZ004777 and FG-2216 have been identified as potent epigenetic modulators that can reverse TGF-β1 induced T regulatory cells and may be used to treat diverse immune disorders.

Life Sciences published new progress about 1338466-77-5. 1338466-77-5 belongs to tetrahydrofurans, auxiliary class Epigenetics,Histone Methyltransferase, name is 1-(3-((((2R,3S,4R,5R)-5-(4-Amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)(isopropyl)amino)propyl)-3-(4-(tert-butyl)phenyl)urea, and the molecular formula is C28H41N7O4, Computed Properties of 1338466-77-5.

Referemce:
https://en.wikipedia.org/wiki/Tetrahydrofuran,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Wu, Haijun published the artcileEthanol-Assisted Hydrothermal Liquefaction of Poplar Using Fe-Co/Al₂O₃ as Catalyst, Recommanded Product: 3-Hydroxydihydrofuran-2(3H)-one, the publication is Energies (Basel, Switzerland) (2022), 15(9), 3057, database is CAplus.

Although the conversion of lignocellulosic biomass into bio-oil with high yield/quality through hydrothermal liquefaction (HTL) is promising, it still faces many challenges. In this study, a Fex-Co(1-x)/Al₂O₃ catalyst was prepared with the coprecipitation method and low-content ethanol was used as the cosolvent for the HTL of poplar. The results showed that the Fex-Co(1-x)/Al₂O₃ catalyst significantly promoted the yield and energy recovery rate (ERR) of bio-oil compared with the control (10% ethanol content). At 260 °C for 30 min, 60Fe-40Co/Al₂O₃ had the best catalytic effect, achieving the highest bio-oil yield (67.35%) and ERR (93.07%). As a multifunctional bimetallic catalyst, Fex-Co(1-x)/Al₂O₃ could not only increase the degree of hydrogenation deoxidization of the product but also promote the diversity of phenolic compounds gained from lignin. The bio-oil obtained from HTL with Fex-Co(1-x)/Al₂O₃ as catalyst contained lower heterocyclic nitrogen, promoting the transfer of more bio-oil components to substances with lower b.p.

Energies (Basel, Switzerland) published new progress about 19444-84-9. 19444-84-9 belongs to tetrahydrofurans, auxiliary class Tetrahydrofuran,Ester,Alcohol, name is 3-Hydroxydihydrofuran-2(3H)-one, and the molecular formula is C22H18O2, Recommanded Product: 3-Hydroxydihydrofuran-2(3H)-one.

Referemce:
https://en.wikipedia.org/wiki/Tetrahydrofuran,
Tetrahydrofuran | (CH2)3CH2O – PubChem