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Synthesis of novel furan-based chalcone derivatives as anti-tuberculosis agents: in vitro, cytotoxicity assessment and in silico
Synthesis of novel furan-based chalcone derivatives as anti-tuberculosis agents: in vitro, cytotoxicity assessment and in silico
Background: The aim of the study is to identify a novel furan-based chalcone derivative as potent inhibitor against the H3...
Cheminformatics-driven discovery of hit compounds against Paracoccidioides spp.
Cheminformatics-driven discovery of hit compounds against Paracoccidioides spp.
Aims: The development of safe and effective therapies for treating paracoccidioidomycosis using computational strategies w...
An overview of imidazole and its analogues as potent anticancer agents
An overview of imidazole and its analogues as potent anticancer agents
The quest for novel, physiologically active imidazoles remains an exciting topic of research among medicinal chemists. The...
Diphenyl-substituted triazine derivatives: synthesis, α-glucosidase inhibitory activity, kinetics and in silico studies
Diphenyl-substituted triazine derivatives: synthesis, α-glucosidase inhibitory activity, kinetics and in silico studies
Background: Diabetes mellitus (DM) is a chronic disorder considered a major global health challenge in the 21st century. α...
Novel 4-aminoquinoline analogs targeting the HIF-1α signaling pathway
Novel 4-aminoquinoline analogs targeting the HIF-1α signaling pathway
Background: The aminoquinoline core exhibits versatile pharmacological properties, particularly in the area of anticancer ...
Current in silico methods for multi-target drug discovery in early anticancer research: the rise of the perturbation-theory machine learning approach
Current in silico methods for multi-target drug discovery in early anticancer research: the rise of the perturbation-theory machine learning approach
This work was financially supported by the Foundation for Science and Technology/the Ministry of Science, Technology and H...
Synthesis and HDAC1 inhibitory activity of a novel series of coumarin-based amide derivatives for treatment of cancer
Synthesis and HDAC1 inhibitory activity of a novel series of coumarin-based amide derivatives for treatment of cancer
Background: Histone deacetylases (HDACs) play a vital role in the epigenetic regulation of transcription and expression. H...
Research progress on tamoxifen and its analogs associated with nuclear receptors
Research progress on tamoxifen and its analogs associated with nuclear receptors
Tamoxifen, a triphenylethylene-based selective estrogen-receptor modulator, is a landmark drug for the treatment of breast...
Latest advancements in the study of the relationship between NSAIDs and three prostaglandin E2 synthases
Latest advancements in the study of the relationship between NSAIDs and three prostaglandin E2 synthases
Tweetable abstract This work describes novel evidence of the relationship between NSAIDs and three prostaglandin E2 syntha...
Multitask learning-driven identification of novel antitrypanosomal compounds
Multitask learning-driven identification of novel antitrypanosomal compounds
Background: Chagas disease and human African trypanosomiasis cause substantial death and morbidity, particularly in low- a...
Novel diamides inspired by protein kinase inhibitors as anti-Trypanosoma cruzi agents: in vitro and in vivo evaluations
Novel diamides inspired by protein kinase inhibitors as anti-Trypanosoma cruzi agents: in vitro and in vivo evaluations
Background: Chagas disease is a life-threatening illness caused by Trypanosoma cruzi. The involvement of serine-arginine-r...
Multicomponent diastereoselective synthesis of tetrahydropyridines as α-amylase and α-glucosidase enzymes inhibitors
Multicomponent diastereoselective synthesis of tetrahydropyridines as α-amylase and α-glucosidase enzymes inhibitors
Background: Researchers seeking new drug candidates to treat diabetes mellitus have been exploring bioactive molecules fou...
Design, synthesis and biological evaluation of novel oxindole analogs as antitubercular agents
Design, synthesis and biological evaluation of novel oxindole analogs as antitubercular agents
Aim: To design, synthesize and evaluate oxindole derivatives for antitubercular activity. Methodology: We synthesized the ...
α-amylase inhibition and in silico studies of novel naphtho[2,3-d]imidazole-4,9-dione linked N-acyl hydrazones
α-amylase inhibition and in silico studies of novel naphtho[2,3-d]imidazole-4,9-dione linked N-acyl hydrazones
Aim: To enrich the pool of α-amylase inhibitors to manage Type 2 diabetes. Methods: Synthesis, conformational study, α-amy...
Current development of pyrazole–azole hybrids with anticancer potential
Current development of pyrazole–azole hybrids with anticancer potential
Chemotherapy is a critical treatment modality for cancer patients, but multidrug resistance remains one of the major chall...
New opportunities for treatment and prevention of neurodegenerative diseases with PTP1B inhibitors
New opportunities for treatment and prevention of neurodegenerative diseases with PTP1B inhibitors
The authors have no relevant affiliations or financial involvement with any organization or entity with a financial intere...
Enhancing the affinity of novel GLS1 allosteric inhibitors by targeting key residue Lys320
Enhancing the affinity of novel GLS1 allosteric inhibitors by targeting key residue Lys320
Aim: A series of novel GLS1 irreversible allosteric inhibitors targeting Lys320 might have robust enzyme inhibitory activi...
Small-molecule oligonucleotides as smart modality for antiviral therapy: a medicinal chemistry perspective
Small-molecule oligonucleotides as smart modality for antiviral therapy: a medicinal chemistry perspective
Small-molecule oligonucleotides could be exploited therapeutically to silence the expression of viral infection-causing ge...
Aminopyridone-linked benzimidazoles: a fragment-based drug design for the development of CDK9 inhibitors
Aminopyridone-linked benzimidazoles: a fragment-based drug design for the development of CDK9 inhibitors
Aim: A fragment-based design and synthesis of three novel series of aminopyridone-linked benzimidazoles as potential antic...
In vitro biological activity of cobalt(II) complexes with salicylaldimine ligands in microbial and cancer cells
In vitro biological activity of cobalt(II) complexes with salicylaldimine ligands in microbial and cancer cells
Background: More studies using cobalt complexes as drugs are needed. Results: The drug action of two cobalt salicylaldimin...
Novel antimicrobial iodo-dihydro-pyrrole-2-one compounds
Novel antimicrobial iodo-dihydro-pyrrole-2-one compounds
Aim: A series of new hybrid molecules with two iodine atoms on the sides were synthesized. Methods: A one-pot, two-compone...
Click synthesis, antimicrobial, DNA photocleavage and computational studies of oxindole-tethered 1H-1,2,3-triazoles
Click synthesis, antimicrobial, DNA photocleavage and computational studies of oxindole-tethered 1H-1,2,3-triazoles
Aim: To obtain new hybrids derived from isatin and triazole. Materials & methods: A series of oxindole–1-H-1,2,3-triaz...
Design, synthesis and biological evaluation of novel selective PI3Kδ inhibitors containing pyridopyrimidine scaffold
Design, synthesis and biological evaluation of novel selective PI3Kδ inhibitors containing pyridopyrimidine scaffold
Aim: In our study compounds with pyrido[3,2-d]pyrimidine and pyrido[3,4-d]pyrimidine were designed, synthesized and evalua...
Novel pyrimidine-1,3,4-oxadiazole hybrids and their precursors as potential antimycobacterial agents
Novel pyrimidine-1,3,4-oxadiazole hybrids and their precursors as potential antimycobacterial agents
Background: Molecular hybridization and isostery are proven approaches in medicinal chemistry, and as such we used them to...
Synthesis of hydrazinylthiazole carboxylates: a mechanistic approach for treatment of diabetes and its complications
Synthesis of hydrazinylthiazole carboxylates: a mechanistic approach for treatment of diabetes and its complications
Aim: The deaths of thousands of people and millions affected by diabetes mellitus triggered us to look for alternative pos...
Thiazolidinedione–triazole conjugates: design, synthesis and probing of the α-amylase inhibitory potential
Thiazolidinedione–triazole conjugates: design, synthesis and probing of the α-amylase inhibitory potential
Aim: The primary objective of this investigation was the synthesis, spectral interpretation and evaluation of the α-amylas...
Novel hydroxy- and amidino-substituted benzimidazoles and benzothiazoles as antibacterial and antiproliferative agents
Novel hydroxy- and amidino-substituted benzimidazoles and benzothiazoles as antibacterial and antiproliferative agents
Aim: The aim was synthesis of novel benzazoles bearing amidino and 2-hydroxyphenyl substituents to explore their biologica...
Medicinal chemistry approaches for the discovery of Plasmodium falciparum dihydroorotate dehydrogenase inhibitors as antimalarial agents
Medicinal chemistry approaches for the discovery of Plasmodium falciparum dihydroorotate dehydrogenase inhibitors as antimalarial agents
Malaria is a severe human disease and a global health problem because of drug-resistant strains. Drugs reported to prevent...
Discovery of new thieno[2,3-d]pyrimidines as EGFR tyrosine kinase inhibitors for cancer treatment
Discovery of new thieno[2,3-d]pyrimidines as EGFR tyrosine kinase inhibitors for cancer treatment
Background: EGFR has been considered a vital molecular target in cancer management. Aim: The discovery of new thieno[2,3-d...
Quinazolinone derivatives as new potential CDK4/6 inhibitors, apoptosis inducers and radiosensitizers for breast cancer
Quinazolinone derivatives as new potential CDK4/6 inhibitors, apoptosis inducers and radiosensitizers for breast cancer
Background: Targeting CDK4/6 has advanced breast cancer treatment. Herein, new quinazolinones were synthesized with acetam...
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