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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...
Silibinin: a natural flavonoid with multifaceted anticancer potential and therapeutic challenges
Silibinin: a natural flavonoid with multifaceted anticancer potential and therapeutic challenges
Silibinin, the principal bioactive flavonolignan of Silybum marianum (milk thistle), has emerged as a promising natural ag...
Plant-derived pyroptosis inducers as a therapeutic strategy in drug-resistant cancers
Plant-derived pyroptosis inducers as a therapeutic strategy in drug-resistant cancers
Drug resistance in cancer therapy, often due to the evasion of apoptosis, highlights the need for alternative treatments. ...
Discovery of novel and potent URAT1 inhibitors bearing sulfamide scaffold for the treatment of gout
Discovery of novel and potent URAT1 inhibitors bearing sulfamide scaffold for the treatment of gout
The urate transporter 1 (URAT1) plays an important role in the reabsorption of uric acid, so URAT1 inhibitors are consider...
Exploring antidiabetic potential of plant diterpenes: from mechanisms to clinical insights
Exploring antidiabetic potential of plant diterpenes: from mechanisms to clinical insights
Type 2 diabetes mellitus (DM) is a heterogeneous metabolic disorder characterized by chronic hyperglycemia and glucose int...
Targeting west nile virus replication by xanthine inhibitors
Targeting west nile virus replication by xanthine inhibitors
West Nile Virus (WNV) is a mosquito-borne emerging virus, which can result in the development of meningitis or encephaliti...
Metabolism of 2,2′,5,5′-tetrachlorobiphenyl (PCB52) by a fish cytochrome P450 (CYP2Y) orthologous to the human CYP2ABFGST gene cluster
Metabolism of 2,2′,5,5′-tetrachlorobiphenyl (PCB52) by a fish cytochrome P450 (CYP2Y) orthologous to the human CYP2ABFGST gene cluster
Polychlorinated biphenyls (PCBs) are globally distributed pollutants that continue to pose health risks for humans and wil...
Synthesis and in vitro anti-trypanosomal evaluation of quinolone hydrazide analogues
Synthesis and in vitro anti-trypanosomal evaluation of quinolone hydrazide analogues
African trypanosomiasis is a major health threat to humans and animals in 36 countries within sub-Saharan Africa. We previ...
Increased plasma concentrations of 6-oxo-methylphenidate in carriers following a single oral dose of methylphenidate
Increased plasma concentrations of 6-oxo-methylphenidate in carriers following a single oral dose of methylphenidate
Attention-deficit/hyperactivity disorder (ADHD) is a neurodevelopmental disorder, with methylphenidate used as a first-lin...
Research progress on extraction and purification, pharmacological activity, pharmacokinetics and content determination of platycodin D
Research progress on extraction and purification, pharmacological activity, pharmacokinetics and content determination of platycodin D
Platycodin D (PD), a unique oleane-type triterpene saponin found in the roots of Platycodon grandiflorum (Jacq.) A. DC. (P...
Estrogen sulfotransferase inhibitors, triclosan and beyond
Estrogen sulfotransferase inhibitors, triclosan and beyond
The estrogen sulfotransferase (EST), also called sulfotransferase 1E1 (SULT1E1), plays an important role in estrogen homeo...
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