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Selectively and efficiently eliciting a ROS-dependent energy crisis within cancer cells through a mitochondria-targeted catechol-based diphenylhextriene
Cancer is one of the most intractable diseases posing a threat to human health. Chemotherapy is one of the main methods fo...
TBP-TA exhibits potent antibacterial activity against vancomycin-resistant Enterococcus
Antimicrobial resistance (AMR) has emerged as a major global challenge for livestock production [1]. AMR not only exacerba...
Mucoadhesive lignin–liposome nanocarriers of coptisine: A multifunctional strategy against antibiotic-resistant Helicobacter pylori biofilms
Helicobacter pylori (H. pylori) is a widely spread pathogen that infects more than half of the world's population [1]. H. ...
Lometrexol targets MRPL2 to suppress NSCLC via dual regulation of mitochondrial ribosomal activity and nuclear PDCD11/ Ca2+ signaling
Lung cancer, classified into non-small cell lung carcinoma (NSCLC) and small cell lung carcinoma (SCLC), presents a signif...
Reconnecting new tetrahydrobenzothieno-4-pyrimidine amides as potent PIM-1 kinase inhibitors via an integrated ligand, machine learning model and structure based scaffold hopping: In vitro anti-tumor investigations
Cancer development and progression are based on the dysregulated function of the kinases namely tyrosine and serine/threon...
Cascade biocatalysis for pyridoxal 5′-phosphate synthesis with ATP autonomy via polyphosphate kinase
Pyridoxal 5′-phosphate (PLP), the active form of vitamin B6, stands as one of the most versatile enzymatic cofactors in na...
An insight into the anticancer potential of sulfonated styrylquinazolines as multifunctional agents targeting microtubules.
Developing new microtubule-targeting agents is extremely important for cancer treatment. One of the goals is to overcome d...
Comparative study of 47Sc and 177Lu-labeled albumin binder-conjugated FAPI radiopharmaceuticals
The tumor microenvironment (TME) plays a central role in cancer progression and therapeutic resistance. Among its non-mali...
Design, synthesis, and biological evaluation of hydrophobic-tagged poly (ADP-ribose) polymerase 1 (PARP1) degraders
The poly (ADP-ribose) polymerase (PARP) family comprises seventeen DNA-dependent nucleases that are primarily involved in ...
Construction of the chiral 24R-OH squalamine intermediate by an engineered ketoreductase from Rhodococcus sp.
Squalamine, chemically known as 3β-[[3-((4-aminobutyl)amino)propyl]amino]-5α-cholestan-7α,24R-diol-24-sulfonate, was initi...
Copper(II)-catalysed one-pot synthesis of thiazole/benzothiazole-based isoquinolin-1(2H)-ones as potential cytotoxic and VEGFR-2 inhibitors
Over the decades, copper-catalysed reactions have shown considerable synthetic utility in organic and medicinal chemistry ...
Discovery and mechanistic insights of novel Piperlongumine analogs as potent Bcr-Abl kinase inhibitors
Chronic myeloid leukemia (CML) is a clonal myeloproliferative neoplasm characterized by the uncontrolled proliferation of ...
4-[(Aryloylhydrazineylidene)methyl]-N-phenylbenzamides as a new class of antimycobacterial agents: design, synthesis and biological evaluation
A novel series of 4-[(aryloylhydrazineylidene)methyl]-N-phenylbenzamides was designed, synthesized, and evaluated as poten...
Ruthenium(II)-catalyzed asymmetric transfer hydrogenation for enantioselective synthesis of (S)-/(R)-4-ethyl-N-[(2-methyl-1,2,3,4-tetrahydroisoquinolin-1-yl)methyl]benzamide exhibiting differing antinociceptive effects
Isoquinoline-based compounds are among the most significant naturally occurring alkaloids and constitute a substantial gro...
Novel 5,7-Diazaindole-based ERK5 inhibitor induces endoplasmic reticulum stress and mitochondrial apoptosis in non-small cell lung Cancer
Lung cancer remains the leading cause of cancer-related mortality worldwide, with non-small cell lung cancer (NSCLC) accou...
Design, synthesis and biological evaluation of novel isoalantolactone-benzylamine derivatives leading to the discovery of a PARP1 inhibitor with selective cytotoxicity against MCF-7 breast cancer cells
Breast cancer (BC) stands as the most prevalent malignancy among women worldwide, and approximately 15%–20% of breast canc...
Design and evaluation of glycyrrhetinic acid-Pt(IV) hybrids for targeted therapy of liver cancer with reduced systemic toxicity
Cancer remains a leading cause of mortality worldwide, accounting for nearly 10 million deaths in 2020 [1], [2]. The World...
Phenylpiperazine/dithioates as novel H2S donors: design, synthesis, H2S release, formulation as PEG-niosomes and antifungal activity against Candida albicans
Candida yeasts are the primary cause of invasive fungal infections, which are among the most severe fungal diseases since ...
Current landscape and recent developments of PI3K/AKT/mTOR targeted inhibitors for breast carcinoma
Cancer is a fatal illness, accounting for millions of deaths worldwide annually. Recent statistics from the International ...
Harnessing marine bacteria-derived compounds as anti-quorum sensing agents: a spotlight on sources, mechanisms and emerging technologies
Infectious diseases have posed the greatest threat to human existence throughout history. The National Institute of Health...
Development of novel seleno-ciprofloxacin derivatives: an X in the antibiotic treasure map
The growing emergence of pathogens resistant to the currently available antibacterial agents is an increasing and troubles...
Antiplasmodial effect of benzimidazole-pyrazole derivative against Plasmodium berghei infection in mice model
Malaria-associated morbidity and mortality pose a major threat to public health globally, contributing to 245 million case...
Dual cholinesterase inhibition by lactam-1,2,3-triazole hybrids: A click chemistry approach for drug discovery
Alzheimer's disease (AD) is a devastating neurodegenerative disorder that affects millions of people worldwide [1,2]. The ...
A natural flavagline derivative A2073 inhibits the proliferation of erythroleukemia cells by targeting the MAPK, PI3K, NF-κB, and cell cycle pathways
BackgroundAcute Erythroid Leukemia (AEL) is a distinct subtype of Acute Myeloid Leukemia (AML), which is characterised by ...
Discovery of novel imidazo[2,1-b][1,3,4]thiadiazole analogs as fluorescent SHP2 inhibitors
Protein tyrosine phosphatase SHP2, encoded by the PTPN11 gene, represents a nonreceptor PTP containing two tandem N-termin...
Potent soluble epoxide hydrolase inhibitors based on thiazole-5-carboxamide structure with imidazolidinone moiety as a secondary pharmacophore
Eicosanoids are metabolites derived from arachidonic acid (AA), generated through three enzymatic routes, namely cyclooxyg...
The influence of halogen-substituted anisaldehyde and aminophenol precursors on the solid-state molecular conformation and antiproliferative activity of resulting Schiff bases
Herein, we report the synthesis of (E)-2-(4-methoxybenzylidene) aminophenol (3a) and its mono/dihalo substituted aryl anal...
Development of 9-cinnamyl-9H-purine derivatives as potent anticancer agents through inactivation of NF-κb/p65 and p-STAT1 signaling pathways: Discovery of a new template for adenosine receptor
Cancer remains one of the leading causes of death worldwide, and despite significant advances in cancer research, discover...
Exploitation of novel pyrazolo[3,4-d]pyrimidine scaffold tethered to thiazole as potential EGFR/HER2 dual kinase inhibitor to overcome lapatinib resistant breast cancer: Design, synthesis, in silico docking and molecular dynamic simulation
Breast cancer (BC) is currently the most devastating condition in women globally. The American Cancer Society anticipated ...
Evolution of 8-esterified cycloberberines as a novel class of antibacterial agents against MDR gram-positive strains by targeting DNA polymerase IIIC
The constant evolution of methicillin-resistant Staphylococcus aureus (MRSA), a predominant pathogen in purulent skin and ...
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