Day: November 21, 2022

Kim, Kee-Pyo published the artcilePermissive epigenomes endow reprogramming competence to transcriptional regulators, Recommanded Product: 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 Nature Chemical Biology (2021), 17(1), 47-56, database is CAplus and MEDLINE.

Abstract: Identifying mol. and cellular processes that regulate reprogramming competence of transcription factors broadens our understanding of reprogramming mechanisms. In the present study, by a chem. screen targeting major epigenetic pathways in human reprogramming, we discovered that inhibiting specific epigenetic roadblocks including disruptor of telomeric silencing 1-like (DOT1L)-mediated H3K79/K27 methylation, but also other epigenetic pathways, catalyzed by lysine-specific histone demethylase 1A, DNA methyltransferases and histone deacetylases, allows induced pluripotent stem cell generation with almost all OCT factors. We found that simultaneous inhibition of these pathways not only dramatically enhances reprogramming competence of most OCT factors, but in fact enables dismantling of species-dependent reprogramming competence of OCT6, NR5A1, NR5A2, TET1 and GATA3. Harnessing these induced permissive epigenetic states, we performed an addnl. screen with 98 candidate genes. Thereby, we identified 25 transcriptional regulators (OTX2, SIX3, and so on) that can functionally replace OCT4 in inducing pluripotency. Our findings provide a conceptual framework for understanding how transcription factors elicit reprogramming in dependency of the donor cell epigenome that differs across species.

Nature Chemical Biology 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, Recommanded Product: 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

Zhu, Jiayi published the artcileNiSO₄-catalyzed C-H activation/C-S cross-coupling of 1,2,3-triazole N-oxides with thiols, Computed Properties of 57124-87-5, the publication is Organic & Biomolecular Chemistry (2015), 13(12), 3711-3720, database is CAplus and MEDLINE.

An efficient nickel-catalyzed protocol for C-S cross-coupling through the direct functionalization of 2-aryl-1,2,3-triazole N-oxide C-H bonds with aryl or alkyl thiols, or di-Ph disulfide has been developed. The targeted N⁺-O^– bond cleavage can be observed during the reaction, and thus obviates the need to use an addnl. deoxygenation step. This new protocol for the preparation of thiolated 2-aryl-1,2,3-triazoles, e.g., I, appears to offer good yields with high regioselectivity, mild conditions, and a wide substrate scope.

Organic & Biomolecular Chemistry 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 C18H26ClN3O, Computed Properties of 57124-87-5.

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

Xie, Long-Yong published the artcileVisible-light-promoted direct C-H/S-H cross-coupling of quinoxalin-2(1H)-ones with thiols leading to 3-sulfenylated quinoxalin-2(1H)-ones in air, Category: tetrahydrofurans, the publication is Organic Chemistry Frontiers (2019), 6(24), 3950-3955, database is CAplus.

A new and efficient visible-light-mediated strategy was developed for the synthesis of 3-sulfenylated quinoxalin-2(1H)-ones via direct C-H sulfenylation of quinoxalin-2(1H)-ones with thiols in air at room temperature Through this photochem. reaction, various 3-sulfenylated quinoxalin-2(1H)-ones were be efficiently and conveniently obtained in excellent yields with good functional group tolerance by simple use of rhodamine B as the cheap photocatalyst and air as the green oxidant.

Organic Chemistry Frontiers 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 C7H7ClN2S, Category: tetrahydrofurans.

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

Liang, Jiajin published the artcileComprehensive insights into xylan structure evolution via multi-perspective analysis during slow pyrolysis process, Synthetic Route of 19444-84-9, the publication is Fuel Processing Technology (2019), 1-7, database is CAplus.

Comprehension in hemicellulose pyrolysis is critical to generate renewable fuel and valuable chem. Herein, a self-designed tubular reactor was applied to observe the appearance alteration and chem. structure evolution during the whole xylan pyrolysis process. Before 200°C, it was free moisture removal stage without significant chem. structure alteration. Xylan began to depolymerize at 200°C corresponding with the appearance change from its original state to dark brown, cleavage of branched-chain and primary product acids & ketones generation. The main chain of xylan was completely broken at 250-350°C via β-1,4-glycosidic bond cleavage, dehydration, decarboxylation, and decarbonylation reaction. Acids were mainly originated from hemicellulose pyrolysis. The typical signals from FTIR, ¹³C CP/MAS NMR were disappeared at 350°C. In the carbonation stage, the C/H and C/O ratio reached 2.01 and 4.54, leading to the aromaticity enhancement of char and formation of carbon-centered radicals.

Fuel Processing Technology 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, Synthetic Route of 19444-84-9.

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

Liu, Yuping published the artcileSynthesis and odor evaluation of five new sulfur-containing ester flavor compounds from 4-ethyloctanoic acid, Category: tetrahydrofurans, the publication is Molecules (2010), 5104-5111, database is CAplus and MEDLINE.

Five sulfur-containing flavor compounds were designed. and the synthesis of the target compounds was achieved using 4-ethyloctanoyl chloride and thiols and alcs. as starting materials. The products thus obtained [i.e., 4-ethyloctanoic acid 3-(methylthio)propyl ester, 4-ethyloctanethioic acid S-(2-furanylmethyl) ester, 4-ethyloctanethioic acid S-(2-methyl-3-furanyl) ester, 4-ethyloctanoic acid 2-(4-methyl-5-thiazolyl)ethyl ester, 4-ethyloctanethioic acid S-(tetrahydro-2-methyl-3-furanyl) ester] are synthetic sulfur-containing ester flavor compounds which all possess a meaty odor and might be used in foods if approved for this purpose.

Molecules 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, Category: tetrahydrofurans.

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

Hartman, Guy J. published the artcileVolatile products formed from the thermal degradation of thiamin at high and low moisture levels, Name: 2-Methyl-3-tetrahydrofuranthiol, the publication is Journal of Agricultural and Food Chemistry (1984), 32(5), 1015-18, database is CAplus.

Volatile products formed during the heating (135°) of thiamin  [59-43-8] in water and propylene glycol  [57-55-6] were examined Carbonyls, furans, thiophenes, thiazoles, dioxolanes, and other S-containing compounds were identified. Quant. and qual. greater amounts of compounds were identified in the water system. Qual. comparisons of systems studied were made.

Journal of Agricultural and Food Chemistry 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, Name: 2-Methyl-3-tetrahydrofuranthiol.

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

Tao, Zeyu published the artcileDesign, synthesis and in vitro anti-Zika virus evaluation of novel Sinefungin derivatives, Synthetic Route of 1338466-77-5, the publication is European Journal of Medicinal Chemistry (2018), 994-1004, database is CAplus and MEDLINE.

We report herein the design and synthesis of a series of novel Sinefungin (SIN) derivatives, based on the structures of SIN and its analog EPZ004777. Our results reveal that target compounds(I) (R¹ = F, R² = 4-t-Bu-C₆H₄, 4-CF₃-C₆H₄, 3-CF₃-C₆H₄; R¹ = Cl, R² = 4-F-C₆H₄, 4-Me-C₆H₄, 3-CF₃-C₆H₄, tert-Bu, cyclohexyl) show better activity (IC₅₀ = 4.56-20.16 μM) than EPZ004777 (IC₅₀ = 35.19 μM). Surprisingly, SIN was founded to be not as active (IC₅₀ > 50 μM) as we and other research groups predicted. Interestingly, the intermediates (II) and (III) (R¹ = F, Cl) display potent anti-ZIKV potency (IC₅₀ = 6.33-29.98 μM), and compound II (R¹ = F) also exhibits acceptable cytotoxicity (CC₅₀ > 200 μM), suggesting their promising potential to be leads for further development.

European Journal of 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 C28H29NO4, Synthetic Route of 1338466-77-5.

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

Chava, Suresh published the artcileDisruptor of telomeric silencing 1-like promotes ovarian cancer tumor growth by stimulating pro-tumorigenic metabolic pathways and blocking apoptosis, Name: 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 Oncogenesis (2021), 10(7), 48, database is CAplus and MEDLINE.

Ovarian cancer is the leading cause of gynecol. malignancy-related deaths. Current therapies for ovarian cancer do not provide meaningful and sustainable clin. benefits, highlighting the need for new therapies. We show that the histone H3K79 methyltransferase disruptor of telomeric silencing 1-like (DOT1L) is overexpressed in ovarian cancer and that a higher level of DOT1L expression correlates with shorter progression-free and overall survival (OS). Pharmacol. inhibition of DOT1L (EPZ-5676, EPZ004777, and SGC0946) or genetic inhibition of DOT1L attenuates the growth of ovarian cancer cells in cell culture and in a mouse xenograft model of ovarian cancer. Transcriptome-wide mRNA expression profiling shows that DOT1L inhibition results in the downregulation of genes involved in cellular biosynthesis pathways and the upregulation of proapoptotic genes. Consistent with the results of transcriptome anal., the unbiased large-scale metabolomic anal. showed reduced levels of several metabolites of the amino acid and nucleotide biosynthesis pathways after DOT1L inhibition. DOT1L inhibition also resulted in the upregulation of the NKG2D ligand ULBP1 and subsequent increase in natural killer (NK) cell-mediated ovarian cancer eradication. Collectively, our results demonstrate that DOT1L promotes ovarian cancer tumor growth by regulating apoptotic and metabolic pathways as well as NK cell-mediated eradication of ovarian cancer and identifies DOT1L as a new pharmacol. target for ovarian cancer therapy.

Oncogenesis 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, Name: 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

Drenichev, Mikhail S. published the artcileSelective cleavage of acyl protecting groups in 3′,5′-O-(tetraisopropyldisiloxane-1,3-diyl)ribonucleosides, Formula: C26H45N5O7Si2, the publication is Collection Symposium Series (2011), 403-404, database is CAplus.

Stability of TIPDS protection in nucleosides in ammonia/amine solutions in MeOH and EtOH was studied. It was found that MeNH₂-EtOH solution is a reagent of choice for selective deacylation of N- and O-acyl protected nucleosides without notable cleavage of 3′,5′-TIPDS group.

Collection Symposium Series 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, Formula: C26H45N5O7Si2.

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

Travers, Jon published the artcileTargeting leukemia on the DOT, Product Details of C28H41N7O4, the publication is Nature Chemical Biology (2011), 7(10), 663-665, database is CAplus and MEDLINE.

A review. A combination of chem. and genetic approaches has established a proof of concept in mouse models – with strong mechanistic underpinning – indicating that targeting the aberrantly recruited histone methyltransferase activity of DOT1L has therapeutic potential in aggressive leukemias driven by MLL fusion genes.

Nature Chemical Biology 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 C4Br2N2O4S, Product Details of C28H41N7O4.

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