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8-Fluorotryptanthrin, an immunomodulatory IDO-1 inhibitor enhances the efficacy of artemether-lumefantrine in the treatment of malaria
Malaria is a lethal disease caused by Plasmodium parasites, transmitted through the bites of infected Anopheles mosquitoes...
3H-pyrazolo[4,3-f]quinoline hinge binder, a tunable scaffold for development of novel kinase inhibitors against FLT3-driven leukemia
The 3H-pyrazolo[4,3-f]quinoline moiety, synthesized via a Doebner or Povarov multi-component reaction, has been described ...
Radiosynthesis and PET evaluation of [18F]Fuzuloparib as a PARP-targeted imaging agent in breast cancer
The global burden of breast cancer has risen markedly in recent years. In 2020, breast cancer surpassed lung cancer to bec...
Coixol derivatives induce DNA damage by targeting PARP1
Poly(ADP-ribose)polymerases (PARPs) family consists of 18 members that play pivotal roles in many cellular processes, incl...
Pyrrolopyrimidines: A promising scaffold for the development of novel cathepsin K inhibitors
Osteoporosis is a prevalent condition characterized by a reduction in bone mass and a high risk of fracture, particularly ...
Discovery of highly selective and potent HPK1 inhibitors for cancer immunotherapy
Hematopoietic progenitor kinase 1 (HPK1, also known as MAP4K1), a member of the Ste20-related serine/threonine kinase fami...
An adamantylureido-benzylamide aniline as FLAP/sEH dual inhibitor: Rational design, in vitro and in vivo lipidomic profiling
Inflammation is a host response to various noxious stimuli, including thermal, mechanical, chemical injuries, as well as p...
Structural insights into frog skin-derived cyclic peptides as selective matriptase inhibitors
Matriptase and TMPRSS6 (also known as matriptase 2) are type II transmembrane serine proteases (TTSPs) that share signific...
Advancing the antituberculosis activity of nitropicolinic acids and amides
WHOWorld Health OrganisationDprE1decaprenylphosphoryl-β-d-ribose 2′-oxidaseDprE2decaprenylphosphoryl-2-keto-β-d-erythropen...
Functionalized nitrogen- and chalcogen-containing heterocyclic compounds as aromatase inhibitors: Design, synthesis and biological evaluation
Aromatase inhibition remains a key therapeutic strategy for hormone-dependent breast cancer (HDBC). Among non-steroidal ar...
Design, synthesis and structural development of nonsecosteroidal VDR ligands based on the C,C′-diphenyl-m-carborane scaffold
Vitamin D receptor (VDR) is a nuclear receptor that acts as a ligand-dependent transcription factor in response to 1α,25-d...
FXR-targeted drug discovery: Recent advances and therapeutic perspectives
Farnesoid X receptor (FXR), a core member of the nuclear receptor (NR) superfamily, is a bile acid-activated nuclear trans...
Discovery of XRF-1021, a 2,4-disubstituted-5-fluoropyrimidine derivative as a homeodomain-interacting protein kinase 2 inhibitor for the treatment of chronic kidney disease
Chronic kidney disease (CKD) affects 10–13 % of the global population and is characterized by persistent inflammation and ...
Design, synthesis and preliminary biological evaluation of novel carbamoyl pyridone derivatives as potent inhibitors of Crimean-Congo hemorrhagic fever virus
Crimean-Congo hemorrhagic fever virus (CCHFV) is an enveloped negative-sense RNA virus that belongs to the order Hareavira...
Fabrication and analysis of polydatin-loaded gelatin-coated Polycaprolactone nanoparticles for targeting radioresistant lung cancer cells
Advancements in phytochemistry have led to the development of phytochemicals as promising agents for cancer treatment and ...
Novel imidazo[1,2-a]pyridine-based tubulin polymerization inhibitors: Structure-activity relationships and anti-tumor immune potentiation
Microtubules composed of α-tubulin and β-tubulin heterodimers are an organelle widely present in cells, with multiple biol...
From tetrazole to isoquinolinone: Structure-based optimization and late-stage diversification of AR-C118925-derived P2Y2 receptor antagonists
The P2Y2 receptor is a G protein-coupled receptor activated by extracellular nucleotides, is implicated in various patholo...
Discovery of a novel napabucasin derivative B16 as a potent STAT3 inhibitor for the treatment of triple-negative breast cancer
Breast cancers are malignant tumors that originate from the excessive proliferation of breast epithelial cells. Among them...
Exploring the influence of the glycone space on the therapeutic potential of sp2-iminoglycolipids
Extensive structure-activity relationship studies performed on sp2-iminoglycolipids revealed the fundamental role played b...
Synthesis of β-boswellic acid-amino acid conjugates for targeting KRASG13D mutant colon cancer
Boswellic acids, a class of pentacyclic triterpenes derived from the resin of Boswellia species, have garnered considerabl...
Discovery of novel rigid STING PROTAC degraders as potential therapeutics for acute kidney injury
Acute Kidney Injury (AKI) refers to a disease of rapid deterioration of renal function characterized by acute inflammation...
Discovery of novel azetidine-based imidazopyridines as selective and orally bioavailable inhibitors of phosphodiesterase 10A for the treatment of pulmonary arterial hypertension
Pulmonary arterial hypertension (PAH), a progressive and life-threatening disease classified as a subtype of pulmonary hyp...
Structural simplification of quaternary benzophenanthridine alkaloids generating a candidate for the treatment of non-small cell lung cancer
Natural products and their derivatives represent a significant source of therapeutic agents, playing a crucial role in the...
Tetracationic tetraaryltetranaphtho[2,3]porphyrins for photodynamic inactivation against Staphylococcus aureus biofilm
Infectious diseases continue to pose one of the most significant challenges to global healthcare. Traditionally, antibioti...
Discovery of ultra short β-peptoids with selective activity against drug-resistant Mycobacterium tuberculosis
The search for new antibiotics against drug-resistant microbes has led to renewed focus on antimicrobial peptides (AMPs) a...
Exploring Si-phthalocyanines with different valency for PSMA-targeted photodynamic therapy: Synthesis and preclinical validation
Prostate cancer remains a significant health concern, with existing treatments often proving invasive or inadequate in pre...
A highly active angiotensin I-converting enzyme inhibitory peptide KAKW designed based on the role of C-terminal residue, and its antihypertensive effects on spontaneously hypertensive rats
Bioactive peptides are formed by linking two or more proteinogenic amino acids via peptide bonds, typically ranging in len...
Design, synthesis, and antitumor activity of stapled peptide inhibitors targeting the RAS–RAF interactions
The RAS genes (KRAS, HRAS, and NRAS) are well-known oncogenes, and mutations in these genes can lead to uncontrolled cell ...
Synthesis of Benzo[h]quinoline derivatives and evaluation of their insecticidal activity against Culex pipiens L. larvae
Benzo[h]quinoline derivatives are valuable scaffolds found in pharmaceuticals and natural products, known for their divers...
Discovery of phenylisoxazolidine analogs targeting receptor interacting protein kinase 1 with anti-inflammatory activity
Necroptosis is a type of programmed cell death that was first proposed in 2005 and is associated with a variety of inflamm...
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