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Exploring novel anticancer pyrazole benzenesulfonamides featuring tail approach strategy as carbonic anhydrase inhibitors
Exploring novel anticancer pyrazole benzenesulfonamides featuring tail approach strategy as carbonic anhydrase inhibitors
Carbonic anhydrases (CAs) are essential metalloenzymes, present in both prokaryotes and eukaryotes, that catalyse the reve...
Synthesis, cytotoxic activity evaluation and mechanistic investigation of novel 3,7-diarylsubstituted 6-azaindoles
Synthesis, cytotoxic activity evaluation and mechanistic investigation of novel 3,7-diarylsubstituted 6-azaindoles
All four positional isomers of the azaindole (1H-pyrrolopyridine) fused ring system can be considered as isosteric structu...
Synthesis and biological evaluation of fluoroquinolones containing a pyridoxine derivatives moiety
Synthesis and biological evaluation of fluoroquinolones containing a pyridoxine derivatives moiety
Nowadays, the increasing emergence of antibiotic resistance in pathogenic bacteria is one of the biggest problems of the h...
Targeting protein kinases for the treatment of Alzheimer's disease: Recent progress and future perspectives
Targeting protein kinases for the treatment of Alzheimer's disease: Recent progress and future perspectives
Alzheimer's disease (AD), the most common neurodegenerative disease, was first described by German psychiatrist Alos Alzhe...
Progress in the development of TRPV1 small-molecule antagonists: Novel Strategies for pain management
Progress in the development of TRPV1 small-molecule antagonists: Novel Strategies for pain management
Pain management represents a global challenge. Pain arising from various causes, such as trauma, disease, surgery, chemoth...
Applications of oxetanes in drug discovery and medicinal chemistry
Applications of oxetanes in drug discovery and medicinal chemistry
Oxetane is an oxygen-containing four-membered heterocycle, which exhibits significant strain energy (c.a. 106 kJ mol−1) [1...
Fragment-based and structure-guided discovery of perforin inhibitors
Fragment-based and structure-guided discovery of perforin inhibitors
Perforin is a pore-forming protein whose normal function enables cytotoxic T and natural killer (NK) cells to kill virus-i...
Current advances and development strategies of orally bioavailable PROTACs
Current advances and development strategies of orally bioavailable PROTACs
Target protein degradation (TPD) is a promising therapeutic strategy for disease treatment. Proteolysis-targeting chimera ...
Technologies of targeting histone deacetylase in drug discovery: Current progress and emerging prospects
Technologies of targeting histone deacetylase in drug discovery: Current progress and emerging prospects
The post-translational modification (PTM) process of histones can modulate changes in chromatin machinery to participate i...
The latest perspectives of small molecules FMS kinase inhibitors
The latest perspectives of small molecules FMS kinase inhibitors
FMS kinase, also known as c-FMS, CSF-1R, M-CSFR, and CD115, is a type III tyrosine kinase receptor (TKR) that belongs to t...
Synthesis and mechanism of action of new purine derivatives against triple negative breast cancer
Synthesis and mechanism of action of new purine derivatives against triple negative breast cancer
The International Agency for Research on Cancer released the latest data showing that breast cancer has surpassed lung can...
Identification of novel dithiocarbamate-copper complexes targeting p97/NPL4 pathway in cancer cells
Identification of novel dithiocarbamate-copper complexes targeting p97/NPL4 pathway in cancer cells
Drug repurposing became an exciting strategy for finding new oncological drugs [1]. One such candidate is the long-term ap...
Recent advances in small molecule and peptide inhibitors of glucose-regulated protein 78 for cancer therapy
Recent advances in small molecule and peptide inhibitors of glucose-regulated protein 78 for cancer therapy
The 70-kDa heat shock protein 70 (Hsp70) family is a class of highly conserved chaperones that play a central role in prot...
Discovery of Pyrazolo[1,5-a]pyrimidine derivative as a potent and selective PI3Kγ/δ dual inhibitor
Discovery of Pyrazolo[1,5-a]pyrimidine derivative as a potent and selective PI3Kγ/δ dual inhibitor
Phosphoinositide-3 kinases (PI3Ks) are key cellular signaling proteins involved in cell proliferation, growth, differentia...