Month: December 2022

Christensen, Matthew D. published the artcileAn inhibitor screen identifies histone-modifying enzymes as mediators of polymer-mediated transgene expression from plasmid DNA, Recommanded Product: N-((4-Acetamidophenyl)carbamothioyl)-4-(tert-butyl)benzamide, the publication is Journal of Controlled Release (2018), 210-223, database is CAplus and MEDLINE.

Effective transgene expression in mammalian cells relies on successful delivery, cytoplasmic trafficking, and nuclear translocation of the delivered vector, but delivery is impeded by several formidable physicochem. barriers on the surface of and within the target cell. Although methods to overcome cellular exclu. and endosomal entrap. have been studied extensively, strategies to overcome ineffi. nuclear entry and subseq. intranuclear barriers to effec. transient gene expre. have only been sparsely explored. In particular, the role of nuclear packaging of DNA with histone proteins. In this work, a parallel screen of small mol. inhibitors of chromatin-modifying enzy. resulted in the identifi. of class I/II HDACs, sirtuins, LSD1, HATs, and the methyltransferases EZH2 and MLL as targets whose inhibi. led to the enhanc. of transgene expre. following polymer-mediated delivery of plasmid DNA. Quant. PCR studies revealed that HDAC inhibi. enhances the amount of plasmid DNA delivered to the nucleus in UMUC3 human bladder cancer cells. N-ChIP-qPCR experiments in CHO-K1 cells indicated that plasmids indeed interact with intracellular core Histone H3, and inhibitors of HDAC and LSD1 proteins. Pair-wise treatments of effective inhibitors led to synergistic enhanc. of transgene expression to varying extents in both cell types. Our results demonstrate that the ability to modulate enzy. that play a role in epigenetic processes can enhance the efficacy of non-viral gene delivery.

Journal of Controlled Release published new progress about 380315-80-0. 380315-80-0 belongs to amides-buliding-blocks, auxiliary class Apoptosis,p53, name is N-((4-Acetamidophenyl)carbamothioyl)-4-(tert-butyl)benzamide, and the molecular formula is C20H23N3O2S, Recommanded Product: N-((4-Acetamidophenyl)carbamothioyl)-4-(tert-butyl)benzamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Christensen, Matthew D. published the artcileAn inhibitor screen identifies histone-modifying enzymes as mediators of polymer-mediated transgene expression from plasmid DNA, Formula: C25H34N4O2S, the publication is Journal of Controlled Release (2018), 210-223, database is CAplus and MEDLINE.

Effective transgene expression in mammalian cells relies on successful delivery, cytoplasmic trafficking, and nuclear translocation of the delivered vector, but delivery is impeded by several formidable physicochem. barriers on the surface of and within the target cell. Although methods to overcome cellular exclu. and endosomal entrap. have been studied extensively, strategies to overcome ineffi. nuclear entry and subseq. intranuclear barriers to effec. transient gene expre. have only been sparsely explored. In particular, the role of nuclear packaging of DNA with histone proteins. In this work, a parallel screen of small mol. inhibitors of chromatin-modifying enzy. resulted in the identifi. of class I/II HDACs, sirtuins, LSD1, HATs, and the methyltransferases EZH2 and MLL as targets whose inhibi. led to the enhanc. of transgene expre. following polymer-mediated delivery of plasmid DNA. Quant. PCR studies revealed that HDAC inhibi. enhances the amount of plasmid DNA delivered to the nucleus in UMUC3 human bladder cancer cells. N-ChIP-qPCR experiments in CHO-K1 cells indicated that plasmids indeed interact with intracellular core Histone H3, and inhibitors of HDAC and LSD1 proteins. Pair-wise treatments of effective inhibitors led to synergistic enhanc. of transgene expression to varying extents in both cell types. Our results demonstrate that the ability to modulate enzy. that play a role in epigenetic processes can enhance the efficacy of non-viral gene delivery.

Journal of Controlled Release published new progress about 1011557-82-6. 1011557-82-6 belongs to amides-buliding-blocks, auxiliary class Epigenetics,Sirtuin, name is 4-(tert-Butyl)-N-((4-(5-(dimethylamino)pentanamido)phenyl)carbamothioyl)benzamide, and the molecular formula is C25H34N4O2S, Formula: C25H34N4O2S.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Takahashi, Hitoe published the artcileSelenoureas and thioureas are effective superoxide radical scavengers in vitro, Formula: C5H10N2OS, the publication is Life Sciences (2005), 76(19), 2185-2192, database is CAplus and MEDLINE.

The authors investigated scavenging of superoxide radicals by selenoureas and thioureas using a highly sensitive and quant. chemiluminescence method. At 330 nM, five selenoureas and five thioureas scavenged fractions of superoxide radicals (O^–₂) ranging from 8.4% to 87.6%. Among five N,N-unsubstituted selenoureas and N,N-unsubstituted thioureas, 1-selenocarbamoylpiperidine and 1-thiocarbamoylpyrrolidine were the most effective scavengers. The study showed that selenoureas could be used as new superoxide anion-scavenging substances.

Life Sciences published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C12H20O6, Formula: C5H10N2OS.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Xu-Xu, Qing-Feng published the artcileSynthesis of Benzoisoselenazolones via Rh(III)-Catalyzed Direct Annulative Selenation by Using Elemental Selenium, Recommanded Product: (3R,4R,5S,6R)-6-(Acetoxymethyl)-3-benzamidotetrahydro-2H-pyran-2,4,5-triyl triacetate, the publication is Chemistry – A European Journal (2021), 27(71), 17952-17959, database is CAplus and MEDLINE.

In this manuscript, a rhodium-catalyzed direct selenium annulation by using stable and tractable elemental selenium was introduced. A series of benzamides as well as acrylamides RNHC(O)R¹ (R = Me, cyclohexyl, Bn, etc.; R¹ = prop-1-en-2-yl, Ph, thiophen-2-yl, etc.) were successfully coupled with selenium under mild reaction conditions, and the obtained isoselenazolones I (R² = H, Me, Ph, Cl; R³ = H, Me, OMe, Cl; R⁴ = H, OMe, Br, F; R⁵ = H, Me, OMe, Cl) and II (R⁶ = Me, Ph; R⁷ = H; R⁶R⁷ = -SCH=CH-) could be pivotal synthetic precursors for several organoselenium compounds e.g., III. Based on the designed control experiments and X-ray absorption spectroscopy measurements, an unprecedented selenation mechanism involving a highly electrophilic Se(IV) species as the reactive selenium donor was proposed. The reaction mechanism was further verified by a computational study.

Chemistry – A European Journal published new progress about 14086-92-1. 14086-92-1 belongs to amides-buliding-blocks, auxiliary class Sugar Units,Glu, name is (3R,4R,5S,6R)-6-(Acetoxymethyl)-3-benzamidotetrahydro-2H-pyran-2,4,5-triyl triacetate, and the molecular formula is C9H13NO2, Recommanded Product: (3R,4R,5S,6R)-6-(Acetoxymethyl)-3-benzamidotetrahydro-2H-pyran-2,4,5-triyl triacetate.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Zhao, Mi-Na published the artcileIron-Catalyzed Cycloaddition of Amides and 2,3-Diaryl-2H-azirines To Access Oxazoles via C-N Bond Cleavage, Application In Synthesis of 79-07-2, the publication is Journal of Organic Chemistry (2021), 86(3), 2957-2964, database is CAplus and MEDLINE.

A novel and efficient iron-catalyzed cycloaddition reaction using readily available 2,3-diaryl-2H-azirines and primary amides is reported. A wide range of trisubstituted oxazoles could be achieved in good yields with good functional group compatibility. In this transformation, two C-N bonds were cleaved and new C-N and C-O bonds were formed.

Journal of Organic Chemistry published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C6H8O3, Application In Synthesis of 79-07-2.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Vangala, Venugopal published the artcileCombating Glioblastoma by Codelivering the Small-Molecule Inhibitor of STAT3 and STAT3siRNA with α5β1 Integrin Receptor-Selective Liposomes, Related Products of amides-buliding-blocks, the publication is Molecular Pharmaceutics (2020), 17(6), 1859-1874, database is CAplus and MEDLINE.

Glioblastoma multiforme (GBM) is one of the most aggressive tumors with a median survival of only 15 mo. Effective therapeutics need to overcome the formidable challenge of crossing the blood-brain barrier (BBB). Receptors and transporters overexpressed on BCECs are being used for designing liposomes, polymers, polymeric micelles, peptides, and dendrimer-based drug carriers for combating brain tumors. Herein, using the orthotopic mouse glioblastoma model, we show that codelivering a small-mol. inhibitor of the JAK/STAT pathway (WP1066) and STAT3siRNA with nanometric (100-150 nm) α5β1 integrin receptor-selective liposomes of RGDK-lipopeptide holds therapeutic promise in combating glioblastoma. Rh-PE (red)-labeled liposomes of RGDK-lipopeptide were found to be internalized in GL261 cells via integrin α5β1 receptors. I.v. administered near-IR (NIR)-dye-labeled α5β1 integrin receptor-selective liposomes of RGDK-lipopeptide were found to be accumulated preferentially in the mouse brain tumor tissue. Importantly, we show that iv injection of WP1066 (a com. sold small-mol. inhibitor of the JAK/STAT pathway) and STAT3siRNA cosolubilized within the liposomes of RGDK-lipopeptide leads to significant inhibition (>350% compared to the untreated mice group) of orthotopically growing mouse glioblastoma. The present strategy may find future use in combating GBM.

Molecular Pharmaceutics published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C12H16N2O2, Related Products of amides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Tung, Truong Thanh published the artcileAmide bond formation in aqueous solution: direct coupling of metal carboxylate salts with ammonium salts at room temperature, Quality Control of 79-07-2, the publication is Organic & Biomolecular Chemistry (2021), 19(46), 10073-10080, database is CAplus and MEDLINE.

A green, expeditious and practically simple protocol for direct coupling of carboxylate salts such as sodium benzoate, sodium nicotinate, sodium acrylate, etc. and ammonium salts such as methoxyamine hydrochloride, ammonium chloride, dimethylamine hydrochloride, etc. under ACN/H₂O conditions at room temperature without the addition of tertiary amine bases was reported. The water-soluble coupling reagent EDC·HCl is a key component in the reaction. The reaction runs smoothly with unsubstituted/substituted ammonium salts and provides a clean products e.g., N-methoxybenzamide without column chromatog. This reaction tolerates both carboxylate (which are unstable in other forms) and amine salts (which are unstable/volatile when present in free form). It was believed that the reported method could be used as an alternative and suitable method at the laboratory and industrial scales.

Organic & Biomolecular Chemistry published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C5H5BrN2, Quality Control of 79-07-2.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Cao, Yucheng published the artcileSynthesis, antifungal activity and potential mechanism of fusidic acid derivatives possessing amino-terminal groups, Safety of H-Lys(Boc)-OH, the publication is Future Medicinal Chemistry (2020), 12(9), 763-774, database is CAplus and MEDLINE.

Aim: Fusidic acid (FA) is a narrow-spectrum bacteriostatic antibiotic. We inadvertently discovered that a FA derivative modified by an amino-terminal group at the 3-OH position, namely 2, inhibited the growth of Cryptococcus neoformans. Methods & results: Multiscale mol. modeling approaches were used to analyze the binding modes of 2 with eEF2. FA derivatives modified at the 3-OH position were designed based on in silico models; seven derivatives possessing different amino-terminal groups were synthesized and tested in vitro for antifungal activity against C. neoformans. Conclusion: Compound 7 had the strongest min. inhibitory concentration Two protonated nitrogen atoms of 7 interacted with a neg. electrostatic pocket of eEF2 likely explain the superiority of 7-2.

Future Medicinal Chemistry published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Safety of H-Lys(Boc)-OH.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Spahn, Nathan A. published the artcileRegioselective Iron-Catalyzed [2 + 2 + 2] Cycloaddition Reaction Forming 4,6-Disubstituted 2-Aminopyridines from Terminal Alkynes and Cyanamides, Recommanded Product: N,N-Dibenzylcyanamide, the publication is Journal of Organic Chemistry (2017), 82(1), 234-242, database is CAplus and MEDLINE.

Fe complexes bound by redox-active pyridine dialdimine (PDAI) ligands catalyze the cycloaddition of two terminal alkynes and one cyanamide. The reaction is both chemo- and regioselective as only 4,6-disubstituted-2-aminopyridine products are formed in moderate to high yields. Isolation of a Fe-azametallacycle (4) suggests catalyst deactivation occurs with large excess of cyanamide over longer reaction times. Fe-catalyzed cycloaddition allowed for a straightforward synthesis of a variety of amino-pyridines, including known estrogen receptor ligands.

Journal of Organic Chemistry published new progress about 2451-91-4. 2451-91-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Benzene, name is N,N-Dibenzylcyanamide, and the molecular formula is C9H8BNO2, Recommanded Product: N,N-Dibenzylcyanamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Nguyen, Vu Thanh published the artcileOne-pot three-component synthesis of 1-amidoalkyl naphthols and polyhydroquinolines using a deep eutectic solvent: A green method and mechanistic insight, Name: 2-Chloroacetamide, the publication is New Journal of Chemistry (2021), 45(4), 2053-2059, database is CAplus.

The multicomponent synthesis of 1-amidoalkyl naphthols I [R¹ = n-Pr, Ph, 4-MeC₆H₄, 2-furyl, etc., R² = Ph, CH₂Cl] and polyhydroquinolines II [R = furan-2-yl, Ph, 2-ClC₆H₄, etc.] was developed as an atom-economic procedure catalyzed by a deep eutectic solvent ([CholineCl][ZnCl₂]₃). The reactions proceeded smoothly at low temperatures for a short reaction time without the use of toxic and volatile organic solvents. Deep eutectic solvents were capable of not only allowing multicomponent reactions to proceed in high yield but also controlling the selectivity towards desired products. Mechanistic insights were examined by HRMS (ESI) to propose a plausible mechanism. Furthermore, [CholineCl][ZnCl₂]₃ could be recycled up to three consecutive cycles with an insignificant loss of catalytic activity under the optimized conditions.

New Journal of Chemistry published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C2H4ClNO, Name: 2-Chloroacetamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics