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Inhibition of SARS-CoV-2 replication in cells by G-quadruplex ligands
Inhibition of SARS-CoV-2 replication in cells by G-quadruplex ligands
The coronavirus SARS-CoV-2 continues to spread worldwide. Dozens of compounds have been discovered based on the structure ...
Evaluation of cholinesterase enzyme inhibitory potential of dipterocarpol derivatives
Evaluation of cholinesterase enzyme inhibitory potential of dipterocarpol derivatives
Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) - are depression and neurodegenerative diseases that target e...
Review: Chemical and biological features of genus Paralemnalia soft corals
Review: Chemical and biological features of genus Paralemnalia soft corals
Marine soft corals are plentiful sources of a wide range of natural products. They include an extensive array of chemical ...
Thiophene ring-opening reactions. Part VII: synthesis and antitumor, anti-inflammatory, and antioxidant properties of 1,3,4‒thiadiazoline‒6-sulfanylthiopyran-4(1H)-one hybrids
Thiophene ring-opening reactions. Part VII: synthesis and antitumor, anti-inflammatory, and antioxidant properties of 1,3,4‒thiadiazoline‒6-sulfanylthiopyran-4(1H)-one hybrids
The reaction of N′’(aryl)benzothiohydrazides with 2-chloro-6-((substituted)amino)-3-nitro-4-oxo-4H-thieno[2,3-...
The versatile NDI-based compounds: emerging anticancer and antimicrobial agents
The versatile NDI-based compounds: emerging anticancer and antimicrobial agents
G-quadruplexes (G4s) are non-canonical nucleic acid structures present in guanine-rich sequences, notably within cancer-as...
Investigating novel tubulin polymerization inhibitors: design, synthesis, LC/MS cellular permeability, in silico studies, and in vitro assessment
Investigating novel tubulin polymerization inhibitors: design, synthesis, LC/MS cellular permeability, in silico studies, and in vitro assessment
In this study, chalcones 5, and 6 and pyrazolines 7, and 8 were designed and synthesized as combrestatin A-4 (CA-4) analog...
Monoamine oxidase inhibition by thiazole derivatives substituted with the benzenesulfonamide moiety
Monoamine oxidase inhibition by thiazole derivatives substituted with the benzenesulfonamide moiety
Based on a report that 1,3,4-oxadiazol-2-ylbenzenesulfonamides act as inhibitors of monoamine oxidase B (MAO-B), the prese...
Design and synthesis of aminothiazole-benzazole based amide: antiproliferative, antimigration activity and molecular docking studies
Design and synthesis of aminothiazole-benzazole based amide: antiproliferative, antimigration activity and molecular docking studies
In this study, we synthesized a series of amide-functionalized aminothiazole-benzazole analogs for potential application i...
Design of novel benzimidazole-propane hydrazide derivatives as α-glucosidase and α-amylase inhibitors: in vitro and in silico studies
Design of novel benzimidazole-propane hydrazide derivatives as α-glucosidase and α-amylase inhibitors: in vitro and in silico studies
A new series of benzimidazole-propane hydrazide derivatives 9a-k were designed, synthesized, and evaluated for their inhib...
Triphenylphosphonium (TPP) conjugates of 1,2,3-triazolyl nucleoside analogues. Synthesis, cytotoxicity and antimicrobial activity
Triphenylphosphonium (TPP) conjugates of 1,2,3-triazolyl nucleoside analogues. Synthesis, cytotoxicity and antimicrobial activity
A series of new triphenylphosphonium (TPP) conjugates of 1,2,3-triazolyl nucleoside analogues were synthesised by coupling...
Synthesis of the dibenzylbutane lignan LCA derivatives and evaluation of their anti-inflammatory activities
Synthesis of the dibenzylbutane lignan LCA derivatives and evaluation of their anti-inflammatory activities
The roots of Litsea cubeba (Lour.) Pers have been used for the treatment of rheumatism. We previously extracted and isolat...
Synthesis and in vitro antiproliferative evaluation of novel drimane oxepinyl triazoles from labdane diterpene sclareol
Synthesis and in vitro antiproliferative evaluation of novel drimane oxepinyl triazoles from labdane diterpene sclareol
A series of new oxepinyl triazoles were synthesized using labdane diterpene sclareol as a template. The synthesis process ...
Design, synthesis, and evaluation of antitumor activity of quinazoline derivatives containing different terminal segments of basic amine groups
Design, synthesis, and evaluation of antitumor activity of quinazoline derivatives containing different terminal segments of basic amine groups
In this study, we designed and synthesized 41 quinazoline derivatives with different base amine termini. Compound 15n show...
Antivirulence therapy: type IV pilus as a druggable target for bacterial infections
Antivirulence therapy: type IV pilus as a druggable target for bacterial infections
Virulence is an organism’s ability to infect the host and cause disease, and this ability is determined by the prese...
Shaping the future of medicine through diverse therapeutic applications of tetralin derivatives
Shaping the future of medicine through diverse therapeutic applications of tetralin derivatives
Tetralin is an ortho-fused bicyclic hydrocarbon notable for its odour of a mixture of benzene and menthol and high boiling...
Structure-based virtual screening and molecular dynamics simulations of FDA-approved drugs targeting MALAT1
Structure-based virtual screening and molecular dynamics simulations of FDA-approved drugs targeting MALAT1
In recent decades, RNA has emerged as an attractive target for the discovery of new small molecules with a wide range of p...
Design, synthesis, molecular docking, and antibacterial activity of novel amide-linked tetrahydrobenzothienopyrimidinone derivatives as potential DNA gyrase and topoisomerase IV inhibitors
Design, synthesis, molecular docking, and antibacterial activity of novel amide-linked tetrahydrobenzothienopyrimidinone derivatives as potential DNA gyrase and topoisomerase IV inhibitors
A series of tetrahydrobenzo [4, 5] thieno [2, 3-d] pyrimidinone derivatives 3a–j and 4–6 was synthesized, and ...
Design, synthesis and investigating the in vitro and in silico HDAC8 inhibitory activities of derivatives of [6]-shogaol and [6]-gingerol isolated from ginger (Zingiber officinale)
Design, synthesis and investigating the in vitro and in silico HDAC8 inhibitory activities of derivatives of [6]-shogaol and [6]-gingerol isolated from ginger (Zingiber officinale)
The main components, [6]-shogaol (6) and [6]-gingerol (7), were obtained from the rhizome of Zingiber officinale. Both nat...
Dual inhibition strategy addressing hyperuricemia and oxidative stress: design, biological evaluation and stability studies of febuxostat-probenecid mutual prodrug
Dual inhibition strategy addressing hyperuricemia and oxidative stress: design, biological evaluation and stability studies of febuxostat-probenecid mutual prodrug
The mutual prodrug approach appears as a promising strategy for developing candidates with great therapeutic effectiveness...
Naturally occurring organosulfur for treating metabolic disorders and infectious diseases
Naturally occurring organosulfur for treating metabolic disorders and infectious diseases
Sulfur has been used as a medicinal agent by the Greeks since ancient times. Approximately 350 sulfur-containing compounds...
New derivatives of dipicolinic acid as metallo-β-lactamase NDM-1 inhibitors
New derivatives of dipicolinic acid as metallo-β-lactamase NDM-1 inhibitors
Resistance to β-lactam antibiotics caused by β-lactamases such as New-Delhi lactamase (NDM-1) has become one of ...
CO prodrugs: a new scaffold of adamantane-fused norbornen-7-ones with tunable water solubility
CO prodrugs: a new scaffold of adamantane-fused norbornen-7-ones with tunable water solubility
We have had a long-standing interest in developing organic prodrugs for controlled delivery of CO for various therapeutic ...
Synthesis of tetrahydro-β-carboline analogs with N11 modifications and study of their antimalarial activities
Synthesis of tetrahydro-β-carboline analogs with N11 modifications and study of their antimalarial activities
Tetrahydro-β-carbolines are medicinal important class of compounds have their place in indole family. N-benzylation v...
Harmine and its derivatives: an In-depth review of antitumor mechanisms and structure-activity relationship
Harmine and its derivatives: an In-depth review of antitumor mechanisms and structure-activity relationship
Harmine is a naturally occurring heterocyclic compound belonging to the β-carboline alkaloid class, found in various ...
Multi-targeted pharmacological properties of cinnamyl piperazine derivatives: a comprehensive review
Multi-targeted pharmacological properties of cinnamyl piperazine derivatives: a comprehensive review
The cinnamyl piperazine motif is a crucial element in drugs targeting various biological targets. Medicinal chemistry rese...
Esters and amides of benzofuroxan-1-N–oxide derivatives as trypanocidal and leishmanicidal agents
Esters and amides of benzofuroxan-1-N–oxide derivatives as trypanocidal and leishmanicidal agents
American trypanosomiasis and leishmaniasis are worldwide health problems that warrant attention given the current ineffect...
Synthesis of 6-dialkylaminopyrimidine carboxamide analogues and their anti-tubercular properties
Synthesis of 6-dialkylaminopyrimidine carboxamide analogues and their anti-tubercular properties
Tuberculosis (TB) continues to be a threat to global health stability. Pyrimidine carboxamides have demonstrated potent an...
Design, synthesis and biological evaluation of novel pyrimidine-phenylsulfonylfuroxan hybrids
Design, synthesis and biological evaluation of novel pyrimidine-phenylsulfonylfuroxan hybrids
In this study, a series of novel pyrimidine-phenylsulfonylfuroxan hybrids were designed, synthesized and evaluated for the...
Structural modifications of berberine and the lipid-regulating effects of its derivatives
Structural modifications of berberine and the lipid-regulating effects of its derivatives
Hyperlipidemia refers to one or more diseases with unbalanced lipid structure in plasma, which is called dyslipidemia in m...
Quinazoline derivatives and hybrids: recent structures with potent bioactivity
Quinazoline derivatives and hybrids: recent structures with potent bioactivity
Quinazolines represent a class of nitrogen-containing heterocyclics with a broad spectrum of biological applications. Many...
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