SCI时时刷

search
Discovery of novel 1,2,4-triazole derivatives as xanthine oxidoreductase inhibitors with hypouricemic effects
Xanthine oxidoreductase (XOR) is a clinically validated target for the treatment of hyperuricemia and gout. A series of no...
Photodynamic antitumor activity of Gallium(III) and Phosphorus(V) complexes of trimethoxyl A2B triaryl corrole
Two new trimethoxyl A2B triaryl corroles 10-(2,4,6-trimethoxyphenyl)-5,15-bis(pentafluorophenyl)- corrole (1) and 10-(3,4,...
Anti-inflammatory butanolides and lignanoids from the root of Machilus zuihoensis var. mushaensis
From the anti-inflammatory screening of Formosan Lauraceous plants, the methanolic extract of the root of Machilus zuihoen...
Discovery of novel β-carboline-1,2,3-triazole hybrids as AChE/GSK-3β dual inhibitors for Alzheimer's disease treatment
Alzheimer's disease (AD) is characterized by progressive cognitive impairment and mental behavior. The combination inhibit...
SAR study of oxidative DIMs analogs targeting the Nur77-mediated apoptotic pathway of cancer cells
Nur77, an orphan nuclear receptor, is implicated in regulating diverse cellular biological processes including apoptosis a...
Discovery of bicyclic polyprenylated acylphloroglucinols from Hypericum himalaicum with glucose transporter 4 translocation activity
Volume 129, December 2022, 106160Highlights•Sixteen novel bicyclic polyprenylated acylphloroglucinols were isolated from H...
3-Substituted-2,3-Dihydrothiazole as a promising scaffold to design EGFR inhibitors
Volume 129, December 2022, 106172Highlights•A novel series of 2-hydrazino-3-substituted-1,3-dihydrothiazole derivatives wa...
Mahanimbine isolated from Murraya koenigii inhibits P-glycoprotein involved in lung cancer chemoresistance
P-glycoprotein (P-gp), a transmembrane glycoprotein, is mainly involved in lung cancer multidrug resistance. Several P-gp ...
Mitochondria targeted dual-fluorescent probe for bio-imaging viscosity and F− with different fluorescence signals
Volume 129, December 2022, 106169Highlights•DMAS-Si bio-images both viscosity and F− ions in mitochondria of HeLa cells.•D...
Hemicyanine-based pH-responsive probes for rapid hypoxia detection in cancer cells
As pH-sensitive and hypoxia-responsive probes, three hemicyanine derivatives based on vanillin and the indole ring (Val-Hc...
Fragment-based discovery of orphan nuclear receptor Nur77/NGFI-B ligands
Volume 129, December 2022, 106164Highlights•Drug fragment screening identified new Nur77 modulators with reduced lipophili...
Dual-modal polypeptide-containing contrast agents for magnetic resonance/fluorescence imaging
Volume 129, December 2022, 106161Highlights•Dual-modal MRI/FI gents were made by incorporation of Gd-DTPA and RhB to Lamin...
Nitroreductase-induced bioorthogonal ligation for prodrug activation: A traceless strategy for cancer-specific imaging and therapy
Prodrug development is of great interest in cancer therapy. From bio-friendly standpoints, traceless prodrug activation wo...
Rational development of an ESIPT-based fluorescent probe with large Stokes shift for imaging of hydrogen sulfide in live cells
Volume 129, December 2022, 106158Highlights•BTDI was designed and synthesised based on the excited-state intramolecular pr...
Targeting neuronal calcium channels and GSK3β for Alzheimer’s disease with naturally-inspired Diels-Alder adducts
The complexity of neurodegenerative diseases, among which Alzheimer’s disease plays a pivotal role, poses one of the tough...
Novel diaryl ether derivatives as InhA inhibitors: Design, synthesis and antimycobacterial activity
A new series of triclosan (TCL)-mimicking diaryl ether derivatives 7–25 were synthesized and evaluated as inhibitors of en...
Novel 5,6-diphenyl-1,2,4-triazine-3-thiol derivatives as dual COX-2/5-LOX inhibitors devoid of cardiotoxicity
A novel series of 5,6-diphenyl-1,2,4-triazine-3-thiol derivatives were designed, synthesized, and screened for their inhib...
Allyl phenyl selenides as H2O2 acceptors to develop ROS-responsive theranostic prodrugs
Volume 129, December 2022, 106154Highlights•Synthesis of ROS-responsive camptothecin prodrugs containing allyl phenyl sele...
Synthesis and in vivo evaluation of new steviol derivatives that protect against cardiomyopathy by inhibiting ferroptosis
Cardiovascular diseases (CVDs) remain the leading cause of death globally. Inhibiting ferroptosis and thus preventing card...
Targeting the kinetics mechanism of AMPA receptor inhibition by 2-oxo-3H-benzoxazole derivatives
Ionotropic glutamate receptors are ligand-gated ion channels found in most excitatory synapses in the brain that allow for...
Prospect of ULK1 modulators in targeting regulatory T cells
Volume 129, December 2022, 106141Highlights•Treg cells coordinate immune homeostasis via potent inhibitory effects.•Modula...