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Structure Optimizing of Flavonoids against Both MRSA and VRE
Structure Optimizing of Flavonoids against Both MRSA and VRE
Antibiotic discovery has saved the lives of many people from most infectious diseases.[1] But antibiotic abuse has led to ...
Privileged Small Molecules against Neglected Tropical Diseases: A perspective from Structure Activity Relationships
Privileged Small Molecules against Neglected Tropical Diseases: A perspective from Structure Activity Relationships
Neglected tropical diseases (NTDs) include diverse infectious diseases that emerge predominantly in tropical and sub-tropi...
Discovery of the small molecular inhibitors against sclerostin loop3 as potential Anti-Osteoporosis agents by structural based virtual screening and molecular design
Discovery of the small molecular inhibitors against sclerostin loop3 as potential Anti-Osteoporosis agents by structural based virtual screening and molecular design
Osteoporosis, delineated as a disorder characterized by heightened fracture susceptibility, manifests through diminished b...
Design, Synthesis, and Evaluation of Novel Quindoline Derivatives with Fork-Shaped Side Chains as RNA G-Quadruplex Stabilizers for Repressing Oncogene NRAS Translation
Design, Synthesis, and Evaluation of Novel Quindoline Derivatives with Fork-Shaped Side Chains as RNA G-Quadruplex Stabilizers for Repressing Oncogene NRAS Translation
The number of newly diagnosed cases of melanoma worldwide in one year reached 300,000 in 2020, which raises a serious conc...
Design, Synthesis, and Biological Evaluation of Some 2-(3-oxo-5,6-diphenyl-1,2,4-triazin-2(3H)-yl)-N-phenylacetamide Hybrids as MTDLs for Alzheimer’s Disease Therapy
Design, Synthesis, and Biological Evaluation of Some 2-(3-oxo-5,6-diphenyl-1,2,4-triazin-2(3H)-yl)-N-phenylacetamide Hybrids as MTDLs for Alzheimer’s Disease Therapy
The incidence of AD, a leading cause of disability and death, is expected to grow rapidly over the next decade [1]. The fi...
Data-oriented protein kinase drug discovery
Data-oriented protein kinase drug discovery
The continued growth of data from biological screening and medicinal chemistry provides opportunities for data-driven expe...
Exploration of isoxazole analogs: Synthesis, COX inhibition, anticancer screening, 3D multicellular tumor spheroids, and molecular modeling
Exploration of isoxazole analogs: Synthesis, COX inhibition, anticancer screening, 3D multicellular tumor spheroids, and molecular modeling
Cancer is a broad term encompassing approximately 100 diseases, affecting various organs in the body. Typically, it arises...
Design, synthesis and evaluation of a pyrazolo[3,4-d]pyrimidine derivative as a novel and potent TGFβ1R1 inhibitor
Design, synthesis and evaluation of a pyrazolo[3,4-d]pyrimidine derivative as a novel and potent TGFβ1R1 inhibitor
The family of transforming growth factor-β (TGF-β) significantly impacts the regulation of many physiological processes. M...
Quantum chemistry calculation-aided discovery of potent small-molecule mimics of glutathione peroxidases for the treatment of cisplatin-induced hearing loss
Quantum chemistry calculation-aided discovery of potent small-molecule mimics of glutathione peroxidases for the treatment of cisplatin-induced hearing loss
According to the World Report of Hearing published by the WHO in 2021, hearing loss currently affects more than 1.5 billio...
Discovery and optimization of narrow spectrum inhibitors of Tousled like kinase 2 (TLK2) using quantitative structure activity relationships
Discovery and optimization of narrow spectrum inhibitors of Tousled like kinase 2 (TLK2) using quantitative structure activity relationships
The oxindole scaffold has been the center of several kinase drug discovery programs, some of which have led to approved me...
Design, synthesis, and biological evaluation of novel benzimidazole derivatives as anti-cervical cancer agents through PI3K/Akt/mTOR pathway and tubulin inhibition
Design, synthesis, and biological evaluation of novel benzimidazole derivatives as anti-cervical cancer agents through PI3K/Akt/mTOR pathway and tubulin inhibition
Cervical cancer (CC) is the eighth most frequently diagnosed cancer and the ninth leading cause of mortality in all cancer...
Novel selective agents for the degradation of AR/AR-V7 to treat advanced prostate cancer
Novel selective agents for the degradation of AR/AR-V7 to treat advanced prostate cancer
Prostate cancer (PCa) is the most prevalent male cancer in the western world and the second most frequent malignancy in me...
Opportunities and perspectives of small molecular phosphodiesterase inhibitors in neurodegenerative diseases
Opportunities and perspectives of small molecular phosphodiesterase inhibitors in neurodegenerative diseases
Neurodegenerative disease is a progressive and fatal disorder caused by chronic dysfunction in the central nervous system ...
Tetrazole derivatives in the management of neurological disorders: Recent advances on synthesis and pharmacological aspects
Tetrazole derivatives in the management of neurological disorders: Recent advances on synthesis and pharmacological aspects
Tetrazole 1 is a doubly unsaturated five-membered ring of aromatic heterocycles containing four nitrogen atoms and one car...
Research progress of fullerenes and their derivatives in the field of PDT
Research progress of fullerenes and their derivatives in the field of PDT
In history, our ancestors were already using light to treat various diseases, including psoriasis, leukoplakia, and even s...
Modulators for palmitoylation of proteins and small molecules
Modulators for palmitoylation of proteins and small molecules
Protein acylation, a common form of saturated or unsaturated lipid modification, has been found occurring on thousands of ...
8-Bicycloalkyl-CPFPX derivatives as potent and selective tools for in vivo imaging of the A1 adenosine receptor
8-Bicycloalkyl-CPFPX derivatives as potent and selective tools for in vivo imaging of the A1 adenosine receptor
Imaging of the A1 adenosine receptor (A1R) by positron emission tomography (PET) with 8-cyclopentyl-3-(3-[18F]fluoropropyl...
Discovery of novel amide derivatives as potent quorum sensing inhibitors of Pseudomonas aeruginosa
Discovery of novel amide derivatives as potent quorum sensing inhibitors of Pseudomonas aeruginosa
Microbial infections are one of the leading causes of death globally. The risks of such infections have become particularl...
Design, synthesis, and biological activity of D-bishomo-1α,25-dihydroxyvitamin D3 analogs and their crystal structures with the vitamin D nuclear receptor
Design, synthesis, and biological activity of D-bishomo-1α,25-dihydroxyvitamin D3 analogs and their crystal structures with the vitamin D nuclear receptor
Since the discovery of 1α,25-dihydroxyvitamin D3 [1α,25-(OH)2D3, calcitriol, 1; Fig. 1] as an active form of vitamin D3 re...
Synthesis and structure-activity optimization of azepane-containing derivatives as PTPN2/PTPN1 inhibitors
Synthesis and structure-activity optimization of azepane-containing derivatives as PTPN2/PTPN1 inhibitors
Clinical efficacy of anti PD-1/PD-L1 immunotherapy is greatly limited by upregulation of PD-1 signaling and mediators of P...
Discovery of novel Thymol-TPP antibiotics that eradicate MRSA persisters
Discovery of novel Thymol-TPP antibiotics that eradicate MRSA persisters
Since the discovery of penicillin in 1928, antibiotics have become the most commonly used drugs for treating a variety of ...
Discovery and optimization of 4-pyrazolyl-2-aminopyrimidine derivatives as potent spleen tyrosine kinase (SYK) inhibitors
Discovery and optimization of 4-pyrazolyl-2-aminopyrimidine derivatives as potent spleen tyrosine kinase (SYK) inhibitors
Spleen tyrosine kinase (Syk) is a 72 kDa cytosolic non-receptor protein tyrosine kinase predominantly expressed in hematop...
Discovery of indolylacryloyl-derived oxacins as novel potential broad-spectrum antibacterial candidates
Discovery of indolylacryloyl-derived oxacins as novel potential broad-spectrum antibacterial candidates
Oxacins represent a crucial class of synthetic first-line antibacterial drugs extensively employed in clinical anti-infect...
Design, synthesis, anti-infective potency and mechanism study of novel Ru-based complexes containing substituted adamantane as antibacterial agents
Design, synthesis, anti-infective potency and mechanism study of novel Ru-based complexes containing substituted adamantane as antibacterial agents
In recent years, pathogenic bacteria evolved multiple types of resistance mechanisms due to the overuse of antibiotics [1,...
Advances in TRPV6 inhibitors for tumors by targeted therapies: Macromolecular proteins, synthetic small molecule compounds, and natural compounds
Advances in TRPV6 inhibitors for tumors by targeted therapies: Macromolecular proteins, synthetic small molecule compounds, and natural compounds
Thirty years ago, a very interesting channel was discovered in Drosophila melanogaster, which revealed the mechanism by wh...
Schiff bases and their metal complexes to target and overcome (multidrug) resistance in cancer
Schiff bases and their metal complexes to target and overcome (multidrug) resistance in cancer
After cardiovascular diseases, cancer is the second leading cause of mortality in the world. If diagnosed in an early stag...
ML162 derivatives incorporating a naphthoquinone unit as ferroptosis/apoptosis inducers: Design, synthesis, anti-cancer activity, and drug-resistance reversal evaluation
ML162 derivatives incorporating a naphthoquinone unit as ferroptosis/apoptosis inducers: Design, synthesis, anti-cancer activity, and drug-resistance reversal evaluation
In recent years, a large number of studies have been devoted to the various pathways that non-classically regulate cell de...
Active site-directed probes targeting dipeptidyl peptidases 8 and 9
Active site-directed probes targeting dipeptidyl peptidases 8 and 9
Dipeptidyl peptidases 8 and 9 (DPP8 and DPP9, respectively) are intracellular proteases widely expressed in mammalian tiss...
Quinoxaline derivatives: Recent discoveries and development strategies towards anticancer agents
Quinoxaline derivatives: Recent discoveries and development strategies towards anticancer agents
According to the World Health Organization (WHO), cancer is a leading cause of death worldwide, accounting for nearly 10 m...
Synthesis and biological evaluation of 4-imidazolidinone–containing compounds as potent inhibitors of the MDM2/p53 interaction
Synthesis and biological evaluation of 4-imidazolidinone–containing compounds as potent inhibitors of the MDM2/p53 interaction
p53 is the guardian of the genome and a tumor suppressor that protects cells from DNA damages [[1], [2], [3]]. To gain cel...
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