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About 357,745 results

Screening and identification of 3-aryl-quinolin-2-one derivatives as antiviral agents a...
https://doi.org/10.1002/jmv.28327
Journal of Medical Virology; Cheng H, Fu L et. al.

Nov 24th, 2022 - Quinolin-2-one represents an important and valuable chemical motif that possesses a wide variety of biological activities; however, the anti-influenza activities of quinolin-2-one-containing compounds were rarely reported. Herein we describe the screening and identification of 3-aryl-quinolin-2-one derivatives as a novel class of antiviral agents. The 3-aryl-quinolinone derivatives were synthes...

Synthesis and Bioactivity of Thiocarboxylic A and Derivatives.
https://doi.org/10.1021/acs.jnatprod.2c00870
Journal of Natural Products; Gillsch F, Mbui F et. al.

Nov 24th, 2022 - The Penicillium metabolite thiocarboxylic A (1a) and three close analogues were synthesized in 14 steps. The stereogenic elements were installed via stereoselective Sharpless epoxidation, (E)-selective reduction of a dibromide, and a Suzuki cross coupling. Thiocarboxylic A (1a) was obtained in 6% overall yield. The synthetic product and the natural isolate differed markedly in their specific ro...

Macrophage-Derived 25-Hydroxycholesterol Promotes Vascular Inflammation, Atherogenesis,...
https://doi.org/10.1161/CIRCULATIONAHA.122.059062
Circulation Canfrán-Duque A, Rotllan N et. al.

Nov 24th, 2022 - Cross-talk between sterol metabolism and inflammatory pathways has been demonstrated to significantly affect the development of atherosclerosis. Cholesterol biosynthetic intermediates and derivatives are increasingly recognized as key immune regulators of macrophages in response to innate immune activation and lipid overloading. 25-Hydroxycholesterol (25-HC) is produced as an oxidation product ...

Self-assembled glycyrrhetinic acid derivatives for functional applications: a review.
https://doi.org/10.1039/d2fo02472a
Food & Function; Zou L, Li Q et. al.

Nov 23rd, 2022 - Glycyrrhetinic acid (GA), a famous natural product, has been attracting more attention recently because of its remarkable biological activity, natural sweetness, and good biocompatibility. In the past few years, a considerable amount of literature has grown up around the theme of GA-based chemical modification to broaden its functional applications. Promising structures including gels, micelles...

Simultaneous depletion of RB, RBL1 and RBL2 affects endoderm differentiation of human e...
https://doi.org/10.1371/journal.pone.0269122
PloS One; Nakanoh S, Kadiwala J et. al.

Nov 23rd, 2022 - RB is a well-known cell cycle regulator controlling the G1 checkpoint. Previous reports have suggested that it can influence cell fate decisions not only by regulating cell proliferation and survival but also by interacting with transcription factors and epigenetic modifiers. However, the functional redundancy of RB family proteins (RB, RBL1 and RBL2) renders it difficult to investigate their r...

In silico and in vitro ADME-Tox analysis and in vivo pharmacokinetic study of represent...
https://doi.org/10.1016/j.taap.2022.116318
Toxicology and Applied Pharmacology; Wójcik-Pszczoła K, Szafarz M et. al.

Nov 23rd, 2022 - Phosphodiesterase (PDE) inhibitors represent a wide class of chemically different compounds that have been extensively studied in recent years. Their anti-inflammatory and anti-fibrotic effects are particularly desirable in the treatment of chronic respiratory diseases, including asthma and chronic obstructive pulmonary disease (COPD). Due to diversified expression of individual PDEs within cel...

The flutemetamol analogue cyano-flutemetamol detects myocardial AL and ATTR amyloid dep...
https://doi.org/10.1080/13506129.2022.2141623
Amyloid : the International Journal of Experimental and C... Abrahamson EE, Padera RF et. al.

Nov 23rd, 2022 - [18F]flutemetamol is a PET radioligand used to image brain amyloid, but its detection of myocardial amyloid is not well-characterized. This histological study characterized binding of fluorescently labeled flutemetamol (cyano-flutemetamol) to amyloid deposits in myocardium. Myocardial tissue was obtained post-mortem from 29 subjects with cardiac amyloidosis including transthyretin wild-type (AT...

A theory-driven synthesis of symmetric and unsymmetric 1,2-bis(diphenylphosphino)ethane...
https://doi.org/10.1038/s41467-022-34546-5
Nature Communications; Takano H, Katsuyama H et. al.

Nov 22nd, 2022 - 1,2-Bis(diphenylphosphino)ethane (DPPE) and its synthetic analogues are important structural motifs in organic synthesis, particularly as diphosphine ligands with a C2-alkyl-linker chain. Since DPPE is known to bind to many metal centers in a bidentate fashion to stabilize the corresponding metal complex via the chelation effect originating from its entropic advantage over monodentate ligands, ...

A selective and sensitive detection system for 4-thiouridine modification in RNA.
https://doi.org/10.1261/rna.079445.122
RNA (New York, N.Y.); Sugio Y, Yamagami R et. al.

Nov 22nd, 2022 - 4-Thiourdine (s4U) is a modified nucleoside, found at positions 8 and 9 in tRNA from eubacteria and archaea. Studies of the biosynthetic pathway and physiological role of s4U in tRNA are ongoing in the tRNA modification field. s4U has also recently been utilized as a biotechnological tool for analysis of RNAs. Therefore, a selective and sensitive system for the detection of s4U is essential for...

JAK-STAT signaling in inflammatory breast cancer enables chemotherapy-resistant cell st...
https://doi.org/10.1158/0008-5472.CAN-22-0423
Cancer Research; Stevens LE, Peluffo G et. al.

Nov 22nd, 2022 - Inflammatory breast cancer (IBC) is a difficult-to-treat disease with poor clinical outcomes due to high risk of metastasis and resistance to treatment. In breast cancer, CD44+CD24- cells possess stem cell-like features and contribute to disease progression, and we previously described a CD44+CD24-pSTAT3+ breast cancer cell subpopulation that is dependent on JAK2/STAT3 signaling. Here we report...

Unique peptidic agonists of a juvenile hormone receptor with species-specific effects o...
https://doi.org/10.1073/pnas.2215541119
Proceedings of the National Academy of Sciences of the Un... Tumova S, Milacek M et. al.

Nov 22nd, 2022 - Juvenile hormones (JHs) control insect metamorphosis and reproduction. JHs act through a receptor complex consisting of methoprene-tolerant (Met) and taiman (Tai) proteins to induce transcription of specific genes. Among chemically diverse synthetic JH mimics (juvenoids), some of which serve as insecticides, unique peptidic juvenoids stand out as being highly potent yet exquisitely selective to...

Identification of Novel F508del-CFTR traffic correctors among triazole derivatives.
https://doi.org/10.1016/j.ejphar.2022.175396
European Journal of Pharmacology; Bacalhau M, Ferreira FC et. al.

Nov 22nd, 2022 - The most prevalent cystic fibrosis (CF)-causing mutation - F508del - impairs the folding of CFTR protein, resulting in its defective trafficking and premature degradation. Small molecules termed correctors may rescue F508del-CFTR and therefore constitute promising pharmacotherapies acting on the fundamental cause of the disease. Here, we screened a collection of triazole compounds to identify n...

Neuroprotective potential of cinnamoyl derivatives against Parkinson's disease indicato...
https://doi.org/10.1016/j.neuro.2022.11.010
Neurotoxicology Tibashailwa N, Stephano F et. al.

Nov 22nd, 2022 - Parkinson's disease (PD) is a movement disorder resulting from the loss of dopaminergic neurons over time. While there is no cure for PD, available conventional therapies aid to manage the motor symptoms. Natural products (NPs) derived from plants are among the most potent alternative therapies for PD. This study explored the neuroprotective potential of selected cinnamoyl derivatives namely to...

Thiadiazine-thione derivatives ameliorate STZ-induced diabetic neuropathy by regulating...
https://doi.org/10.1016/j.intimp.2022.109421
International Immunopharmacology; Qureshi S, Ali G et. al.

Nov 21st, 2022 - Diabetes Mellitus is accompanied by chronic hyperglycemia, inflammation, and related molecular processes, which leads to diabetic neuropathy. In this work, we tested Thiadiazine-thione (TDT) synthetic derivatives TDT1 and TDT2 against streptozotocin (STZ)-induced diabetic neuropathy. Sprague Dawley's rats, SH-SY5Y neuronal and BV2 microglial cells were employed in this work, followed by behavio...

SELECTIVE AND REVERSIBLE DISRUPTION OF MITOCHONDRIAL INNER MEMBRANE PROTEIN COMPLEXES B...
https://doi.org/10.1016/j.mito.2022.11.006
Mitochondrion Kafkova A, Tilokani L et. al.

Nov 20th, 2022 - Triphenylphosphonium (TPP) derivatives are commonly used to target chemical into mitochondria. We show that alkyl-TPP cause reversible, dose- and hydrophobicity-dependent alterations of mitochondrial morphology and function and a selective decrease of mitochondrial inner membrane proteins including subunits of the respiratory chain complexes, as well as components of the mitochondrial calcium u...

Recognition and release of uridine and hCNT3: From multivariate interactions to molecul...
https://doi.org/10.1016/j.ijbiomac.2022.11.145
International Journal of Biological Macromolecules; Duan H, Hu K et. al.

Nov 20th, 2022 - As a vital target for the development of novel anti-cancer drugs, human concentrative nucleoside transporter 3 (hCNT3) has been widely concerned. Nevertheless, the lack of a comprehensive understanding of molecular interactions and motion mechanism has greatly hindered the development of novel inhibitors against hCNT3. In this paper, molecular recognition of hCNT3 with uridine was investigated ...

Characterization of binding properties of ephedrine derivatives to human alpha-1-acid g...
https://doi.org/10.1016/j.ejps.2022.106333
European Journal of Pharmaceutical Sciences : Official Jo... Schmidt S, Zehe M et. al.

Nov 20th, 2022 - Most drugs, especially those with acidic or neutral moieties, are bound to the plasma protein albumin, whereas basic drugs are preferentially bound to human alpha-1-acid glycoprotein (AGP). The protein binding of the long-established drugs ephedrine and pseudoephedrine, which are used in the treatment of hypotension and colds, has so far only been studied with albumin. Since in a previous study...

Photocatalytic direct borylation of carboxylic acids.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9675845
Nature Communications; Wei Q, Lee Y et. al.

Nov 20th, 2022 - The preparation of high value-added boronic acids from cheap and plentiful carboxylic acids is desirable. To date, the decarboxylative borylation of carboxylic acids is generally realized through the extra step synthesized redox-active ester intermediate or in situ generated carboxylic acid covalent derivatives above 150 °C reaction temperature. Here, we report a direct decarboxylative borylati...

Synthesis of Functionalized Indolobenzazepinones via Sc(OTf)3-Induced Ring Expansion/An...
https://doi.org/10.1021/acs.joc.2c02076
The Journal of Organic Chemistry; Xie J, Suleman M et. al.

Nov 19th, 2022 - Herein, we report an unexpected cascade ring expansion/annulation reaction between 4-diazo-1,4-dihydroisoquinolin-3-ones and a variety of isatin derivatives in the presence of Sc(OTf)3 catalyst. A series of novel indolobenzazepinones were synthesized in good to excellent yields with the exclusion of nitrogen and carbon dioxide gases. High bond-forming efficiency, novel reaction mechanism, readi...

Synthesis of β-Deuterated Amino Acids via Palladium-Catalyzed H/D Exchange.
https://doi.org/10.1021/acs.joc.2c01654
The Journal of Organic Chemistry; Sheng FF, Gu JG et. al.

Nov 18th, 2022 - Despite several synthetic approaches that have been developed for α-deuterated amino acids, the synthesis of β-deuterated amino acids has remained a challenge. Herein, we disclose a palladium catalyzed H/D exchange protocol for a β-deuterated N-protected amino amide, which can be converted to a β-deuterated amino acid simply by removal of protecting groups. This protocol is highly efficient, si...