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Sulfonamide-substituted oxindoles as inhibitors of carbonic anhydrase II with potential antiglaucoma activity
Sulfonamide-substituted oxindoles as inhibitors of carbonic anhydrase II with potential antiglaucoma activity
In present work a series of sulfonamide-containing 3-hydroxy-2-oxindoles was designed and synthesized via condensation of ...
New structural scaffold discovery via fragment-based drug design: Hydroxymethyl indazole derivatives as XOR/URAT1 dual inhibitors
New structural scaffold discovery via fragment-based drug design: Hydroxymethyl indazole derivatives as XOR/URAT1 dual inhibitors
Hyperuricemia arises from disrupted uric acid metabolism, where xanthine oxidoreductase (XOR) and uric acid transporter 1 ...
Natural products in medicinal chemistry: targeting inflammatory pathways with plant-derived compounds
Natural products in medicinal chemistry: targeting inflammatory pathways with plant-derived compounds
Inflammation is an immediate physiological response for defense and tissue repair against external stress, however it cont...
Design, synthesis and biological evaluation of novel hydroxamic acids bearing coumarin moieties as histone deacetylase inhibitors and cytotoxic agents
Design, synthesis and biological evaluation of novel hydroxamic acids bearing coumarin moieties as histone deacetylase inhibitors and cytotoxic agents
In this study, we successfully designed and synthesized a new series of coumarin-based hydroxamate derivatives as potent h...
Macrocyclization in medicinal chemistry: updated strategies and applications
Macrocyclization in medicinal chemistry: updated strategies and applications
Macrocyclization has emerged as a versatile design strategy in medicinal chemistry, offering unique opportunities to addre...
Discovery of novel nuciferine-based URAT1 inhibitors for hyperuricemia: synthesis, biological evaluation, and computational insights
Discovery of novel nuciferine-based URAT1 inhibitors for hyperuricemia: synthesis, biological evaluation, and computational insights
URAT1 represents a critical therapeutic target for the treatment of hyperuricemia. However, current URAT1 inhibitors are l...
Synthesis and evaluation of symmetric (1,4-diazepane-1,4-diyl)bis(phenylmethanone) derivatives as amyloid-beta aggregation inhibitors
Synthesis and evaluation of symmetric (1,4-diazepane-1,4-diyl)bis(phenylmethanone) derivatives as amyloid-beta aggregation inhibitors
A group of sixteen symmetric (1,4-diazepane-1,4-diyl)bis(phenylmethanone) derivatives (3a–p) containing a 1,4-diazep...
Synthesis and biological evaluation of coumarin-based urea derivatives demonstrating apoptosis-inducing and anti-angiogenic properties for non-small cell lung cancer treatment
Synthesis and biological evaluation of coumarin-based urea derivatives demonstrating apoptosis-inducing and anti-angiogenic properties for non-small cell lung cancer treatment
Lung cancer represents a substantial public health challenge, with NSCLC being the most prevalent subtype. There is an imp...
Discovery and development of inhibitors of heat shock factor 1 by a fluorescence polarization assay
Discovery and development of inhibitors of heat shock factor 1 by a fluorescence polarization assay
Heat shock proteins (HSPs) play a major role in cell survival in response to stress. Cancer cells in particular rely on th...
Synthesis of new phosphonylated bis-1,3,4-oxadiazoles and study of their antimicrobial and antiviral activity
Synthesis of new phosphonylated bis-1,3,4-oxadiazoles and study of their antimicrobial and antiviral activity
A series of new bis-1,3,4-oxadiazoles was synthesized by reacting the corresponding dicarboxylic acid bishydrazides with d...
Small-molecule drug discovery in malignant melanoma: current status and prospective developments
Small-molecule drug discovery in malignant melanoma: current status and prospective developments
Malignant melanoma, a heterogeneous neoplasm arising from melanocytes, is driven by mutations in critical signaling pathwa...
Design and synthesis of Cereblon-based PROTAC as novel potent degraders of α/β-tubulin
Design and synthesis of Cereblon-based PROTAC as novel potent degraders of α/β-tubulin
The therapeutic target tubulin, which is of great clinical significance, was previously believed to be an undegradable pro...
Advances in quercetin-based therapeutics for breast cancer: natural, synthetic, and nanotechnology-driven approaches
Advances in quercetin-based therapeutics for breast cancer: natural, synthetic, and nanotechnology-driven approaches
Breast cancer remains one of the leading causes of cancer-related deaths among women worldwide, despite significant advanc...
Flavonoids as colchicine binding site inhibitors: emerging scaffolds in anticancer drug design
Flavonoids as colchicine binding site inhibitors: emerging scaffolds in anticancer drug design
Tubulin inhibition remains a well-established strategy in anticancer therapy, mediated primarily through three binding sit...
Direct targeting of GLUT1 in cancer: A decade of inhibitor discovery and medicinal chemistry insights
Direct targeting of GLUT1 in cancer: A decade of inhibitor discovery and medicinal chemistry insights
Glucose transporter 1 (GLUT1), the most extensively distributed member of the glucose transporter protein family, plays a ...
Recent advances in piperidones as privileged scaffolds for drug discovery and development
Recent advances in piperidones as privileged scaffolds for drug discovery and development
Piperidone, a chemically versatile cyclic amine incorporating a ketone functional group, has emerged as a privileged scaff...
4-methylbenzyl 5-arylthiophene-2-carboxylates as Multitarget Directed Ligands Scaffolds (MTDLs): Synthesis, in-silico docking studies, and evaluation of dual selective enzymatic inhibition (AChE & MAO-B)
4-methylbenzyl 5-arylthiophene-2-carboxylates as Multitarget Directed Ligands Scaffolds (MTDLs): Synthesis, in-silico docking studies, and evaluation of dual selective enzymatic inhibition (AChE & MAO-B)
Single-target ligands have insufficient effectiveness in treating Alzheimer’s disease (AD), leading to the developme...
Acylhydrobenzoquinones influence the susceptibility of towards abietanes and the speciation within
Acylhydrobenzoquinones influence the susceptibility of towards abietanes and the speciation within
The genus Plectranthus sensu lato is known to produce abietanes, which exhibit significant potency against Gram-positive b...
Anticancer activity of amide and ester derivatives of the labdane 2α-hydroxyeperuic acid obtained via sonochemical synthesis
Anticancer activity of amide and ester derivatives of the labdane 2α-hydroxyeperuic acid obtained via sonochemical synthesis
Medicinal plants are an invaluable source of specialized metabolites with unique and complex chemical structures. This che...
Beilschmiedia species: from chemistry to pharmacological values
Beilschmiedia species: from chemistry to pharmacological values
Beilschmiedia (the family Lauraceae) is a large tropical genus containing species traditionally used to treat rheumatism, ...
Design, synthesis and antitumor activity study of tubulin/HDAC6 dual targeting inhibitor
Design, synthesis and antitumor activity study of tubulin/HDAC6 dual targeting inhibitor
Cancer combination therapy is a novel strategy to circumvent drug resistance in highly metastatic and advanced malignancie...
Pharmacological significance of palbociclib and its derivatives in cancer treatment and prevention: an update
Pharmacological significance of palbociclib and its derivatives in cancer treatment and prevention: an update
Palbociclib is a selective cyclin-dependent kinases 4 and 6 (CDK4/6) inhibitor that emerged as a significant therapeutic a...
Exploring putative histone deacetylase inhibitors with antiproliferative activity of chrysin derivatives
Exploring putative histone deacetylase inhibitors with antiproliferative activity of chrysin derivatives
Thirty-three derivatives of chrysin were designed and synthesized to evaluate biological activities. All compounds were ch...
Design and synthesis of novel 1-1,2,3-triazolecarbohydrazides and 1,2,4-triazoloazines based on them for anticancer drug discovery
Design and synthesis of novel 1-1,2,3-triazolecarbohydrazides and 1,2,4-triazoloazines based on them for anticancer drug discovery
The synthesis of (1H-1,2,3-triazol-4-yl)-1,2,4-triazolazine derivatives was achieved via a multi-step synthesis starting f...
Discovery of a novel selenamide derivative as potent activator of aldehyde dehydrogenase 2 for cardioprotective applications
Discovery of a novel selenamide derivative as potent activator of aldehyde dehydrogenase 2 for cardioprotective applications
Aldehyde dehydrogenase 2 (ALDH2), a mitochondrial enzyme, plays a pivotal role in the metabolism of endogenous reactive al...
Benzoxa-[2,1,3]-diazole substituted amino acid hydrazides as therapeutics for drug-resistant
Benzoxa-[2,1,3]-diazole substituted amino acid hydrazides as therapeutics for drug-resistant
The global burden of tuberculosis is on the rise and continues to be alarmingly high, with a notable prevalence of multidr...
Development of novel caffeic acid derivatives as multifunctional agents for the treatment of AD
Development of novel caffeic acid derivatives as multifunctional agents for the treatment of AD
Alzheimer’s disease (AD) is a progressive neurodegenerative disorder for which the multi-target-directed ligand (MTD...
Design and discovery of POLQ helicase domain inhibitors by virtual screening and machine learning
Design and discovery of POLQ helicase domain inhibitors by virtual screening and machine learning
DNA polymerase theta (Polθ or POLQ) is an attractive target for treating BRCA-deficient cancers. In the present work,...
Nanosensing doxorubicin: a new frontier in medicinal chemistry
Nanosensing doxorubicin: a new frontier in medicinal chemistry
The advent of nanosensing technologies marks a significant advancement in medicinal chemistry, particularly in the detecti...
The inhibition of monoamine oxidase by 2-methylbenzo[]oxazole derivatives
The inhibition of monoamine oxidase by 2-methylbenzo[]oxazole derivatives
The monoamine oxidase (MAO) enzymes metabolise neurotransmitter amines and are drug targets for the treatment of neuropsyc...
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