SCI时时刷

search
+
Chemical constituents isolated from Actinidia polygama and their α-glucosidase inhibitory activity and insulin secretion effect
Actinidia polygama has been used as a traditional medicine for treating various diseases. In the present study, 13 compoun...
Engineered aldoxime dehydratase to enable the chemoenzymatic conversion of benzyl amines to aromatic nitriles
A chemoenzymatic strategy has been implemented to synthesize nitriles from benzyl amines under mild conditions. Aldoxime d...
Hypoglycemic oligostilbenes from the stems of Caragana sinica
Six new oligostilbenes, carastilphenols A-E (1–5) and (–)-hopeachinol B (6), with three reported oligostilbenes were obtai...
Fusion of Michael-acceptors enhances the anti-inflammatory activity of ginsenosides as potential modulators of the NLRP3 signaling pathway
Ginsenosides are a promising group of secondary metabolites for developing anti-inflammatory agents. In this study, Michae...
Ugi reaction-assisted assembly of covalent PROTACs against glutathione peroxidase 4
Inducing cell ferroptosis by inactivating glutathione peroxidase 4 (GPX4) is a popular cancer treatment strategy. However,...
Structural optimization of tetrahydroisoquinoline-hydroxamate hybrids as potent dual ERα degraders and HDAC inhibitors
Both estrogen receptor α (ERα) and histone deacetylases (HDACs) are valid therapeutic targets for anticancer drug developm...
Exploring chromone sulfonamides and sulfonylhydrazones as highly selective ectonucleotidase inhibitors: Synthesis, biological evaluation and in silico study
Ectonucleotidases, a well-known superfamily of plasma membrane located metalloenzymes plays a central role in mediating th...
Rapid discovery and crystallography study of highly potent and selective butylcholinesterase inhibitors based on oxime-containing libraries and conformational restriction strategies
KeywordsAlzheimer's diseaseButylcholinesterase inhibitorsCombinatorial chemistryConformational restrictionMicroscale synth...
Phenyldivinylsulfonamides for the construction of antibody–drug conjugates with controlled four payloads
Phenyldivinylsulfonamides emerged from a series of divinylsulfonamides, demonstrating their ability to effectively re-brid...
Spectroscopic analysis, kinetic mechanism, computational docking, and molecular dynamics of active metabolites from the aerial parts of Astragalus membranaceus Bunge as tyrosinase inhibitors
A new isoflavane derivative (2), a new natural isoflavane (6), four new oleanane-type triterpenoid saponins (23, 25, 28, a...
Oxazolo[5,4-f]quinoxaline-type selective inhibitors of glycogen synthase kinase-3α (GSK-3α): Development and impact on temozolomide treatment of glioblastoma cells
The 2-(3-pyridyl)oxazolo[5,4-f]quinoxalines CD-07 and FL-291 are ATP-competitive GSK-3 kinase inhibitors. Here, we investi...
Evaluation of honokiol, magnolol and of a library of new nitrogenated neolignans as pancreatic lipase inhibitors
Obesity is a complex disease defined as an excessive amount of body fat. It is considered a risk factor for several pathol...
Efficient synthesis and anticancer evaluation of spider toxin peptide LVTX-8-based analogues with enhanced stability
Cytotoxic peptides derived from spider venoms have been considered as promising candidates for anticancer treatment. The n...
Chemoproteomics reveals arctigenin as a phagophore-closure blocker via targeting ESCRT-I subunit VPS28
Arctigenin is the active ingredient of the traditional medicines Arctium lappa and Fructus Arctii and has been extensively...
Discovery of new small molecule inhibitors of the BPTF bromodomain
Volume 134, May 2023, 106453Author links open overlay panel, , , , , , , , Highlights•A novel BPTF inhibitor scaffold Sang...
New chromones from the roots of Saposhnikovia divaricata (Turcz.) Schischk with anti-inflammatory activity
Fifteen new chromones, sadivamones A-E (1–5), cimifugin monoacetate (6), sadivamones F-N (7–15), together with fifteen kno...
Synthesis, in-Silico studies and biological evaluation of pyrimidine based thiazolidinedione derivatives as potential anti-diabetic agent
Despite the advancements in the management of Diabetes mellitus, the design and synthesis of drug molecule which ameliorat...
Design, synthesis, cytotoxic activities, and molecular docking of chalcone hybrids bearing 8-hydroxyquinoline moiety with dual tubulin/EGFR kinase inhibition
The present study established thirteen novel 8-hydroxyquinoline/chalcone hybrids 3a–m of hopeful anticancer activity. Acco...
Design, synthesis, modeling studies and biological evaluation of pyrazole derivatives linked to oxime and nitrate moieties as nitric oxide donor selective COX-2 and aromatase inhibitors with dual anti-inflammatory and anti-neoplastic activities
Two new series of pyrazole derivatives 10a-f and 11a-f with selective COX-2 inhibition pharmacophore and oxime/nitrate moi...
An ultrasensitive GSH-specific fluorescent probe unveils celastrol-induced ccRCC ferroptosis
Glutathione (GSH) is closely related to the occurrence and development of tumors. The intracellular GSH levels are abnorma...
Wang resin catalysed sonochemical synthesis of pyrazolo[4,3-d]pyrimidinones and 2,3-dihydroquinazolin-4(1H)-ones: Identification of chorismate mutase inhibitors having effects on Mycobacterium tuberculosis cell viability
Volume 134, May 2023, 106452Dedicated to Professor Seyed E. Hasnain (National Science Chair, Indian Institute of Technolog...
Novel lignans from Zanthoxylum nitidum and antiproliferation activity of sesaminone in osimertinib-resistant non-small cell lung cancer cells
KeywordsZanthoxylum nitidumTetrahydrofuran lignansAntiproliferation activityCell cycle arrestApoptosisOsimertinib-resistan...
2-Aminopyrimidine derivatives as selective dual inhibitors of JAK2 and FLT3 for the treatment of acute myeloid leukemia
Dual inhibitors of JAK2 and FLT3 can synergistically control the development of acute myeloid leukemia (AML), and overcome...
Design, synthesis and bioevaluation of 1,2,4-thiadiazolidine-3,5-dione derivatives as potential GSK-3β inhibitors for the treatment of Alzheimer's disease
Tideglusib is a non-competitive GSK-3β inhibitor which contain 1,2,4-thiadiazolidine-3,5-dione moiety, and now mainly used...
Design and synthesis of novel N-terminal peptides of integrin and aminopeptidase are new finding for anticancer activity
The short peptides, containing the amino acid sequence asparagine-glycine-arginine (NGR) and arginine-glycine-aspartic aci...
Discovery of endosomalytic cell-penetrating peptides based on bacterial membrane-targeting sequences
Cell-penetrating peptides (CPPs) are prominent scaffolds for drug developments and related research, particularly the endo...
Introduction of a β-leucine residue instead of leucine9 and glycine10 residues in Temporin L for improved cell selectivity, stability and activity against planktonic and biofilm of methicillin resistant S. aureus
KeywordsAntimicrobial peptideTemporin LMethicillin resistant S. aureusβ-leucineMRSA biofilmAbbreviationsFmocFluorenylmetho...
A win-win scenario for antibacterial activity and skin mildness of cationic surfactants based on the modulation of host-guest supramolecular conformation
The commercial cationic surfactants (CSAa) with quaternary ammonium (QA) groups have proved to be broad-spectrum bacterici...
Recent advances of LSD1/KDM1A inhibitors for disease therapy
KeywordsEpigeneticsHistone demethylaseLSD1 inhibitorsStructure-activity relationshipsTAK-418AbbreviationsAIDSacquired immu...
Immunosuppressive diarylpropane dimer and spirocyclic-monomers from Horsfieldia kingii
Horsfiequinone G (1), a dimeric diarylpropane featuring an unprecedentedly oxo-6/7/6 fused ring system, a new flavane, hor...
阅读更多
format_indent_increase