Tag: M.W=300-350

Uddin, Jashim Md. published the artcileDiscovery of Furanone-Based Radiopharmaceuticals for Diagnostic Targeting of COX-1 in Ovarian Cancer, Safety of Tetrabutylammonium hydrogencarbonate, the publication is ACS Omega (2019), 4(5), 9251-9261, database is CAplus and MEDLINE.

In vivo targeting and visualization of cyclooxygenase-1 (COX-1) using multimodal positron emission tomog./computed tomog. imaging represents a unique opportunity for early detection and/or therapeutic evaluation of ovarian cancer because overexpression of COX-1 has been characterized as a pathol. hallmark of the initiation and progression of this disease. The furanone core is a common building block of many synthetic and natural products that exhibit a wide range of biol. activities. We hypothesize that furanone-based COX-1 inhibitors can be designed as imaging agents for the early detection, delineation of tumor margin, and evaluation of treatment response of ovarian cancer. We report the discovery of 3-(4-fluorophenyl)-5,5-dimethyl-4-(p-tolyl)furan-2(5H)-one (FDF), a furanone-based novel COX-1-selective inhibitor that exhibits adequate in vivo stability, plasma half-life, and pharmacokinetic properties for use as an imaging agent. We describe a novel synthetic scheme in which a Lewis acid-catalyzed nucleophilic aromatic deiodo[¹⁸F]fluorination reaction is utilized for the radiosynthesis of [¹⁸F]FDF. [¹⁸F]FDF binds efficiently to COX-1 in vivo and enables sensitive detection of ovarian cancer in s.c. and peritoneal xenograft models in mice. These results provide the proof of principle for COX-1-targeted imaging of ovarian cancer and identify [¹⁸F]FDF as a promising lead compound for further preclin. and clin. development.

ACS Omega published new progress about 17351-62-1. 17351-62-1 belongs to catalysis-chemistry, auxiliary class Salt,Amine, name is Tetrabutylammonium hydrogencarbonate, and the molecular formula is C13H11NO, Safety of Tetrabutylammonium hydrogencarbonate.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Ackermann, Sarah L. published the artcileCrystallographic Snapshot of an Arrested Intermediate in the Biomimetic Activation of CO₂, Application In Synthesis of 17351-62-1, the publication is Angewandte Chemie, International Edition (2015), 54(1), 164-168, database is CAplus and MEDLINE.

The design of mol. catalysts that mimic the behavior of enzymes is a topical field of activity in emerging technologies, and can lead to an improved understanding of biol. systems. Herein, we report how the bulky arms of the cations in [(n-C₄H₉)₄N]⁺[HCO₃]^– give rise to a host scaffold that emulates the substrate binding sites in carbonic anhydrase enzymes, affording a unique glimpse of an arrested intermediate in the base-mediated binding and activation of CO₂.

Angewandte Chemie, International Edition published new progress about 17351-62-1. 17351-62-1 belongs to catalysis-chemistry, auxiliary class Salt,Amine, name is Tetrabutylammonium hydrogencarbonate, and the molecular formula is C17H37NO3, Application In Synthesis of 17351-62-1.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Wang, Junping published the artcileA highly sensitive fluorescent probe for hydrogen sulfide based on dicyanoisophorone and its imaging in living cells, COA of Formula: C14H10O4S2, the publication is Sensors and Actuators, B: Chemical (2019), 141-147, database is CAplus.

Due to the importance of hydrogen sulfide (H₂S) in physiol. and pathol., the development of fluorescence probes for the detection of H₂S has attracted extensive attention of researchers. We developed a H₂S fluorescence probe (DCN-S) based on dicyanoisopentanone using dithioether and ester groups as the reaction sites. Under the nucleophilic substitution of H₂S, disulfide bond of DCN-S was broken. Then the probe changed into dicyanoisophorone derivative and emitted an orange fluorescence band from 530 nm to 700 nm (centered 580 nm). Upon response for H₂S, DCN-S exhibited high sensitivity (88 nM detection limit) and large stokes shift (155 nm). Importantly, the probe also was successfully used for endogenous and exogenous imaging of living cells.

Sensors and Actuators, B: Chemical published new progress about 119-80-2. 119-80-2 belongs to catalysis-chemistry, auxiliary class sulfides,Carboxylic acid,Benzene, name is 2,2′-Dithiodibenzoic acid, and the molecular formula is C39H35N5O8, COA of Formula: C14H10O4S2.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Bijian, Krikor published the artcileNovel Aurora A and Protein Kinase C (¦Á, ¦Â1, ¦Â2, and ¦È) Multitarget Inhibitors: Impact of Selenium Atoms on the Potency and Selectivity, Quality Control of 119-80-2, the publication is Journal of Medicinal Chemistry (2022), 65(4), 3134-3150, database is CAplus and MEDLINE.

Aurora kinases and protein kinase C (PKC) have been shown to be involved in different aspects of cancer progression. To date, no dual Aurora/PKC inhibitor with clin. efficacy and low toxicity is available. Here, we report the identification of compound 2e as a potent small mol. capable of selectively inhibiting Aurora A kinase and PKC isoforms ¦Á, ¦Â1, ¦Â2 and ¦È. Compound 2e demonstrated significant inhibition of the colony forming ability of metastatic breast cancer cells in vitro and metastasis development in vivo. In vitro kinase screening and mol. modeling studies revealed the critical role of the selenium-containing side chains within 2e, where selenium atoms were shown to significantly improve its selectivity and potency by forming addnl. interactions and modulating the protein dynamics. In comparison to other H-bonding heteroatoms such as sulfur, our studies suggested that these selenium atoms also confer more favorable PK properties.

Journal of Medicinal Chemistry published new progress about 119-80-2. 119-80-2 belongs to catalysis-chemistry, auxiliary class sulfides,Carboxylic acid,Benzene, name is 2,2′-Dithiodibenzoic acid, and the molecular formula is C14H10O4S2, Quality Control of 119-80-2.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Liu, Mengjie published the artcileEngineering of a biologically active insulin dimer, Synthetic Route of 71989-31-6, the publication is Journal of Medicinal Chemistry (2021), 64(23), 17448-17454, database is CAplus and MEDLINE.

The growing epidemic of diabetes means that there is a need for therapies that are more efficacious, safe, and convenient. Here, we report the efficient synthesis of a novel disulfide dimer of human insulin tethered at the N-terminus of its B-chain through placement of a cysteine residue. The resulting peptide was shown to bind to both the insulin receptor isoform B and insulin-like growth factor-1 receptor with comparable affinity to native insulin. In in vivo insulin tolerance tests, the dimer was equipotent to Actrapid insulin and possessed a sustained duration of action greater than that of Actrapid and Glargine. While the secondary structure of our dimeric insulin was similar to that of insulin, it was more resistant to proteolysis. More importantly, our analog was produced in quant. yield from a monomeric thiol insulin scaffold. Our results suggest that this dimer has significant potential to address the clin. needs in the treatment of diabetes.

Journal of Medicinal Chemistry published new progress about 71989-31-6. 71989-31-6 belongs to catalysis-chemistry, auxiliary class Amino acide derivatives,pyrrolidine, name is Fmoc-Pro-OH, and the molecular formula is C20H19NO4, Synthetic Route of 71989-31-6.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Fox, C. P. published the artcileFlame out! End-Triassic mass extinction polycyclic aromatic hydrocarbons reflect more than just fire, Recommanded Product: Coronene, the publication is Earth and Planetary Science Letters (2022), 117418, database is CAplus.

Global warming induced-wildfires of the 21st century reveal the catastrophic effects that widespread biomass burning has on flora and fauna. During mass extinction events, similar wildfire episodes are considered to play an important role in driving perturbations in terrestrial ecosystems. To better evaluate the record of biomass burning and potential carbon cycle feedbacks at the end-Triassic mass extinction (~202 Ma; ETE), we investigated the relative abundances of a range of polycyclic aromatic hydrocarbons (PAHs) and the ¦Ä13C values of regular isoprenoids and n-alkanes at key sections in the SW UK. These data reveal little evidence for intensive wildfire activity during the extinction event, in contrast to what has been reported elsewhere in European, Chinese, and Greenland ETE sections. Herein, PAHs instead reflect greater contributions from an episode of soil erosion that we attribute to Large Igneous Province (LIP)-driven acid rain, and possible distal sources of smoke, suggestive of fire elsewhere in the UK/European basins. This terrestrial ecosystem perturbation is coincident with those in the marine realm, indicating ecosystem perturbations occurred across multiple habitats throughout the latest Rhaetian in the SW UK. Addnl., this geochem. approach reveals that the precursor carbon isotope excursion (CIE) routinely used in chemostratigraphic correlations is unrelated to LIP activity, but instead results from the increased input of terrestrially derived 13C-depleted plant material. Furthermore, we find the initial CIE (commonly used to mark the extinction level, but which is now known to precede the ETE) is also unrelated to biomass burning. Collectively, these data reveal that processes other than combustion of terrestrial material are important for the terrestrial phase of the ETE in the SW UK. Similar investigations are required on other ETE sections, both those in close proximity to the LIP driving the extinction and those further afield, to more clearly determine the neg. effect(s) of LIPs and their geog. extent in the terrestrial realm.

Earth and Planetary Science Letters published new progress about 191-07-1. 191-07-1 belongs to catalysis-chemistry, auxiliary class Electronic Materials, name is Coronene, and the molecular formula is C24H12, Recommanded Product: Coronene.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Xie, Shiwei published the artcileDietary fish oil levels modulated lipid metabolism, immune response, intestinal health and salinity stress resistance of juvenile Penaeus monodon fed a low fish-meal diet, Synthetic Route of 6217-54-5, the publication is Animal Feed Science and Technology (2022), 115321, database is CAplus.

Dietary fish meal (FM) and fish oil (FO) replacement are crucial for the sustainable development of aquaculture. An eight weeks feeding trial was conducted to evaluate the potential replacing FM with soy protein concentrate, and the suitable FO level for a low FM diet of Penaeus monodon. The experiment was conducted in quadruplicates (30 shrimp per replicate, average weight 1.00 ¡À 0.01 g). The results indicated that besides the final body weight, there were no differences in weight gain, feed efficiency and survival rate observed among the four groups. The results of the acute salinity stress showed that shrimp fed the C and MF diets showed a similar survival rate, which was significantly higher than those fed a LF diet. Shrimp that were fed a LF diet showed the lowest expression levels of inhibitor of apoptosis proteins, Toll and tumor necrosis factor receptor associated factor 6 (TRAF6) in the hepatopancreas, as well as the highest expression levels of Toll, extracellular signal-regulated kinase, Relish and TRAF6 in the intestine among four groups. Intestinal microstructure damage was observed in shrimp that were fed a LF diet, and intestinal endoplasmic reticulum (ER) swelling was observed in shrimp fed MF and LF diets. In conclusion, these results indicated that the growth performance of shrimp was not affected when the FM and FO contents decreased, whereas a low content of FM neg. influenced the immune response in shrimp by modulating IMD and ER stress related gene expression.

Animal Feed Science and Technology published new progress about 6217-54-5. 6217-54-5 belongs to catalysis-chemistry, auxiliary class Alkenyl,Carboxylic acid,Aliphatic hydrocarbon chain,Metabolic Enzyme,RAR/RXR,Natural product, name is Docosahexaenoic Acid, and the molecular formula is C5H5F3O2, Synthetic Route of 6217-54-5.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Liu, Jiamei published the artcileEnabling chemical protein (semi)synthesis via reducible solubilizing tags (RSTs), Application In Synthesis of 71989-31-6, the publication is Chemical Science (2022), 13(5), 1367-1374, database is CAplus and MEDLINE.

Chem. synthesis of proteins with poor solubility presents a challenging task. The existing solubilizing tag strategies are not suitable for the expressed protein segment. To address this issue, we report herein that solubilizing tags could be introduced at the side chain of the peptide and C-terminal peptide salicylaldehyde esters via a disulfide linker. Such reducible solubilizing tags (RSTs) are compatible with peptide salicylaldehyde ester-mediated Ser/Thr ligation and Cys/Pen ligation for purifying and ligating peptides with poor solubility This strategy features operational simplicity and readily accessible materials. Both the protein 2B4 cytoplasmic tail and FCER1G protein have been successfully synthesized via this strategy. Of particular note, the RST strategy could be used for solubilizing the expressed protein segment for protein semi-synthesis of the HMGB1 protein.

Chemical Science published new progress about 71989-31-6. 71989-31-6 belongs to catalysis-chemistry, auxiliary class Amino acide derivatives,pyrrolidine, name is Fmoc-Pro-OH, and the molecular formula is C20H19NO4, Application In Synthesis of 71989-31-6.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Yu, Jiahui published the artcileEvaluation of total, sn-2 fatty acid, and triacylglycerol composition in commercial infant formulas on the Chinese market: A comparative study of preterm and term formulas, Category: catalysis-chemistry, the publication is Food Chemistry (2022), 132477, database is CAplus and MEDLINE.

Preterm infants with physiol. immaturity require higher lipid provision than term infants. This study compared the lipid composition, including total, sn-2 fatty acid, and triacylglycerol (TAG) compositions in 14 preterm formulas and 25 term formulas in the Chinese market, in 2020-2021. Preterm formula had higher medium-chain fatty acid (MCFA) and comparable C22:6n-3 (DHA) contents than term formula. Notably, significantly lower C16:0 and C18:0 (p < 0.001) were distributed on the sn-2 position in preterm formula. Two hundred and thirteen kinds of TAG mol. species were identified using UPLC-Q-TOF-MS. In preterm formula, significantly higher Ca-Ca-Cy and Ca-Ca-Ca (p < 0.001) existed. These clear distinctions showed the challenge of the progress in preterm formula, such as DHA status, MCFA pattern, and TAG esterified with palmitic acid on the sn-2 position.

Food Chemistry published new progress about 6217-54-5. 6217-54-5 belongs to catalysis-chemistry, auxiliary class Alkenyl,Carboxylic acid,Aliphatic hydrocarbon chain,Metabolic Enzyme,RAR/RXR,Natural product, name is Docosahexaenoic Acid, and the molecular formula is C9H8BNO2, Category: catalysis-chemistry.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Li, Mingming published the artcileAdaptable peptide-based therapeutics modulating tumor microenvironment for combinatorial radio-immunotherapy, Category: catalysis-chemistry, the publication is Journal of Controlled Release (2021), 35-47, database is CAplus and MEDLINE.

Radiotherapy is one of the conventional tumor treatments, while its abscopal therapeutic efficacy is severely hampered by the immunosuppressive tumor microenvironment. To address this challenge, we herein report on the morphol.-adaptable peptide-based therapeutics for efficiently reversing the immunosuppression in the combinatorial radio-immunotherapy through simultaneous checkpoint blocking and induction of immunogenic cell death. The peptide-based therapeutics were created via co-assembling a pentapeptide containing a 4-amino proline residue with its derivatives containing IDO-1 inhibitor NLG919. The resulting therapeutics underwent pH-adaptable morphol. transformation between nanofibrils and nanoparticles and released NLG919 upon GSH cleavage. In vivo studies confirmed that the pH-adaptable morphologies of the therapeutics facilitated their tumor accumulation and retention at tumor sites compared to morphol.-persistent counterparts, thus resulting in efficient delivery of IDO-1 inhibitors. Simultaneously treating the tumor-bearing mice with the therapeutics and external ¦Ã-ray radiation boosted the tumor immunogenicity via inducing ICD cascade of the tumor cells and reverse the immunosuppressive tumor microenvironment due to the inhibition of IDO-1 for depletion of tryptophan. Our findings strongly demonstrate that the morphol.-adaptable peptide-based therapeutics exhibit the capability to reverse the immunosuppressive tumor microenvironment during irradiation, thus providing a new strategy for the combinatorial radio-immunotherapy.

Journal of Controlled Release published new progress about 71989-31-6. 71989-31-6 belongs to catalysis-chemistry, auxiliary class Amino acide derivatives,pyrrolidine, name is Fmoc-Pro-OH, and the molecular formula is C20H19NO4, Category: catalysis-chemistry.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia