European Journal of Medicinal Chemistry

Article	Citations
Contents continued	475
Scaffold hopping-based structural modification of tranilast led to the identification of HNW005 as a promising NLRP3 inflammasome and URAT1 dual inhibitor for the treatment of gouty arthritis	225
Design, synthesis, evaluation and X-ray structural studies of potent HIV-1 protease inhibitors containing substituted oxaspirocyclic carbamates as the P2 ligands	193
Amino acid–modified chalcone derivatives with in vitro and in vivo efficacy against colon cancer	188
Design and synthesis of benzothiazole aryl urea derivatives as potent anti-staphylococcal agents targeting autolysin-mediated peptidoglycan hydrolases	179
[18F]R91150: Improved radiosynthesis and in vivo evaluation as imaging probe for 5-HT2A receptors	168
Graphical abstract TOC	160
Graphical abstract TOC	158
Structure-based discovery of a 4,5-Dihydropyrazole-cored PET ligand for imaging of receptor-interacting serine/threonine-protein kinase 1 (RIPK1) in the brain	155
Exploring the modulatory influence on the antimalarial activity of amodiaquine using scaffold hybridisation with ferrocene integration	153
Rational molecular design converting fascaplysin derivatives to potent broad-spectrum inhibitors against bacterial pathogens via targeting FtsZ	153
Synthesis and evaluation of a novel class of spiro[chromene-2,2′-indoline] derivatives as potent inhibitors of peptidylarginine deiminase IV to treat rheumatoid arthritis	136
Graphical abstract contents continued	125
Synthesis of tropane-based σ1 receptor antagonists with antiallodynic activity	122
Bestatin analogs-4-quinolinone hybrids as antileishmanial hits: Design, repurposing rational, synthesis, in vitro and in silico studies	117
Identification of novel tetrahydroquinoxaline derived phenyl ureas as modulators of the hepatitis B virus nucleocapsid assembly	115
Design and synthesis of forsythin derivatives as anti-inflammatory agents for acute lung injury	114
Identification of “dual-site”-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase	112
Structure-based approaches for the design of 6-aryl-1-(3,4,5-trimethoxyphenyl)-1H-benzo[d][1,2,3]triazoles as tubulin polymerization inhibitors	108
Ligand-based design and synthesis of new trityl histamine and trityl cysteamine derivatives as SIRT2 inhibitors for cancer therapy	105
Editorial Board	103
A pro-death autophagy-based nanoplatform for enhancing antitumour efficacy with improved immune responses	101
Synthesis and biological evaluation of novel pyrazole amides as potent mitochondrial complex I inhibitors	98
Discovery of N-(5-amido-2-methylphenyl)-5-methylisoxazole-3-carboxamide as dual CSF-1R/c-Kit Inhibitors with improved stability and BBB permeability	98
Rational drug design to explore the structure-activity relationship (SAR) of TRK inhibitors with 2,4-diaminopyrimidine scaffold	97

Highly potent dipeptidyl peptidase 8/9 (DPP8/9) inhibitors designed via relative binding free energy calculations	95
Discovery of the novel Benzo[b]thiophene 1,1-dioxide derivatives as a potent STAT3 inhibitor against idiopathic pulmonary fibrosis	95
Synthesis and antibacterial medicinal evaluation of carbothioamido hydrazonyl thiazolylquinolone with multitargeting antimicrobial potential to combat increasingly global resistance	94
Antitumor activity and transcriptome sequencing (RNA-seq) analyses of hepatocellular carcinoma cells in response to exposure triterpene-nucleoside conjugates	92
Histone deacetylases (HDACs) as the promising immunotherapeutic targets for hematologic cancer treatment	90
Antibacterial sulfonimidamide-based oligopeptides as type I signal peptidase inhibitors: Synthesis and biological evaluation	90
Antioxidant, anti-inflammatory and immunomodulatory roles of vitamins in COVID-19 therapy	87
EGCG-like non-competitive inhibitor of DYRK1A rescues cognitive defect in a down syndrome model	86
Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis	86
Recent developments in the synthesis of indolizines and their derivatives as compounds of interest in medicinal chemistry: a review	84
Rational design, synthesis and biological evaluation of dual PARP-1/2 and TNKS1/2 inhibitors for cancer therapy	84
Monoamine oxidase inhibitors: A concise review with special emphasis on structure activity relationship studies	83
New β-arylchalcogeno amines with procognitive properties targeting Carbonic Anhydrases and Monoamine Oxidases	82
Synthesis of 8-aminomorphans with high KOR affinity	82
Design, synthesis and biological evaluation of N-benzylaryl cinnamide derivatives as tubulin polymerization inhibitors capable of promoting YAP degradation with potent anti-gastric cancer activities	81
Discovery of ML210-Based glutathione peroxidase 4 (GPX4) degrader inducing ferroptosis of human cancer cells	80
Novel pterostilbene derivatives ameliorate heart failure by reducing oxidative stress and inflammation through regulating Nrf2/NF-κB signaling pathway	79
Synthesis and evaluation of 3,4,5-trisubstituted triazoles as G protein-biased kappa opioid receptor agonists	79
6-Regioisomeric 5,8-quinolinediones as potent CDC25 inhibitors against colorectal cancers	79
Corrigendum to “Structure-based development of N-Arylindole derivatives as Pks13 inhibitors against Mycobacterium tuberculosis” [Europ. J. Med. Chem. 283 (2025) 117148]	78
The first ADC bearing the ferroptosis inducer RSL3 as a payload with conservation of the fragile electrophilic warhead	78
Exploration of P1 and P4 modifications of nirmatrelvir: Design, synthesis, biological evaluation, and X-ray structural studies of SARS-CoV-2 Mpro inhibitors	76
Poly(ADP-ribose) polymerase-1 (PARP1)-based dual inhibitors targeting cancer synthetic lethality (2022-present): advances and perspectives	75
Discovery and biological evaluation of 6-aryl-4-(3,4,5-trimethoxyphenyl)quinoline derivatives with promising antitumor activities as novel colchicine-binding site inhibitors	75
Peptide inhibitors targeting Ras and Ras-associated protein–protein interactions	74
Discovery of small molecules for autophagy-lysosome degradation of immune checkpoint proteins	74
Exploring Si-phthalocyanines with different valency for PSMA-targeted photodynamic therapy: Synthesis and preclinical validation	73
Arginine and tryptophan-rich dendritic antimicrobial peptides that disrupt membranes for bacterial infection in vivo	71
Design, synthesis and promising anti-tumor efficacy of novel imidazo[1,2-a]pyridine derivatives as potent autotaxin allosteric inhibitors	71
Discovery of a potent, selective and cell active inhibitor of m6A demethylase ALKBH5	70
Multitarget-directed carbamate and carbamothioate derivatives: Cholinesterase and monoamine oxidase inhibition, anti-β-amyloid (Aβ) aggregation, antioxidant and blood–brain barrier permeation properti	69
A brain-targeting dl-3-n-butylphthalide prodrug to treat ischemic stroke	69
Discovery of novel fused-heterocycle-bearing diarypyrimidine derivatives as HIV-1 potent NNRTIs targeting tolerant region I for enhanced antiviral activity and resistance profile	68
Fluorinated sulfonamide-flavonoid derivatives as novel Keap1-Nrf2 inhibitors: Potent induction of cytoprotective gene HO-1 in vivo	67
Corrigendum to “Design, synthesis and evaluation of carbamate-bridged amino acid prodrugs of cycloicaritin with improved antitumor activity, aqueous solubility and phase II metabolic stability” [Eur.	67
Identification of novel diarylpyrimidine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against wild-type and K103N mutant viruses	66
Discovery, structural optimization, and anti-tumor bioactivity evaluations of betulinic acid derivatives as a new type of RORγ antagonists	66
An update on small molecule compounds targeting synthetic lethality for cancer therapy	65
Application of deuterium in research and development of drugs	64
A decade of USFDA-approved small molecules as anti-inflammatory agents: Recent trends and Commentaries on the “industrial” perspective	64
Non-nucleoside structured compounds with antiviral activity—past 10 years (2010–2020)	64
Synthesis and evaluation of a new class of MIF-inhibitors in activated macrophage cells and in experimental septic shock in mice	63
Anthraquinone derivatives as ADP-competitive inhibitors of liver pyruvate kinase	62
Synthesis of cinnamoyl tethered indoline derivatives with anti-inflammatory and antioxidant activities	61
Discovery and optimization of 4-pyrazolyl-2-aminopyrimidine derivatives as potent spleen tyrosine kinase (SYK) inhibitors	61
Novel 6-hydroxybenzothiazol-2-carboxamides as potent and selective monoamine oxidase B inhibitors endowed with neuroprotective activity	60
Design and syntheses of a bimolecular STING agonist based on the covalent STING antagonist	60
Discovery and biological evaluation of phthalazines as novel non-kinase TGFβ pathway inhibitors	60
1,3-Thiazole nucleus as promising molecular platform against antimicrobial resistance: a recent overview in drug discovery	59
Synthesis, anti-allergic rhinitis evaluation and mechanism investigation of novel 1,2,4-triazole-enamides as CB1 R antagonist	59

Design, synthesis, and biological evaluation of piperazine derivatives as pan-PPARs agonists for the treatment of liver fibrosis	58
Design, synthesis, and biological evaluation of some 2-(3-oxo-5,6-diphenyl-1,2,4-triazin-2(3H)-yl)-N-phenylacetamide hybrids as MTDLs for Alzheimer's disease therapy	58
Novel 3-hydroxypyridin-4(1H)-One derivatives as ferroptosis inhibitors with iron-chelating and reactive oxygen species scavenging activities and therapeutic effect in cisplatin-induced cytotoxicity	58
Nature-inspired new isoindole-based Passerini adducts as efficient tumor-selective apoptotic inducers via caspase-3/7 activation	57
Exploration of 2-phenylquinoline-4-carboxamide linked benzene sulfonamide derivatives as isoform selective inhibitors of transmembrane human carbonic anhydrases	57
Cinnamic acid derivatives linked to arylpiperazines as novel potent inhibitors of tyrosinase activity and melanin synthesis	57
Discovery of novel Thieno[2,3-d]imidazole derivatives as agonists of human STING for antitumor immunotherapy using systemic administration	57
Platinum(IV) complexes as inhibitors of CD47-SIRPα axis for chemoimmunotherapy of cancer	56
Novel nitrogen mustard-artemisinin hybrids with potent anti-leukemia action through DNA damage and activation of GPx	56
Novel β-carboline derivatives show promise as dual-target inhibitors of DNA and TOP2A for the treatment of triple negative breast cancer	56
Discovery of N-(3-fluorophenyl)-2-(4-((7-(1-methyl-1H-pyrazol-4-yl)quinazolin-4-yl)amino)phenyl)acetamide as the first orally active selective aurora kinase B inhibitor	56
Applications of oxetanes in drug discovery and medicinal chemistry	56
Discovery of novel fluorine-containing parthenolide analogues as potential antitumor agents	56
Probing benzenesulfonamide–thiazolidinone hybrids as multitarget directed ligands for efficient control of type 2 diabetes mellitus through targeting the enzymes: α-glucosidase and carbonic anhydrase	55
H2dpa derivatives containing pentadentate ligands: An acyclic adjuvant potentiates meropenem activity in vitro and in vivo against metallo-β-lactamase-producing Enterobacterales	55
A glycyrrhetinic acid-iridium(III) conjugate as a theranostic NIR probe for hepatocellular carcinoma with mitochondrial-targeting ability	55
Estrogen receptor β-targeted hypoxia-responsive near-infrared fluorescence probes for prostate cancer study	55
Design, synthesis and bioevaluation of PI3Kα-selective inhibitors as potential colorectal cancer drugs	55
Engineering a biomimicking strategy for discovering nonivamide-based quorum-sensing inhibitors for controlling bacterial infection	54
Straightforward access to novel mitochondriotropics derived from 2-arylethanol as potent and selective antiproliferative agents	54
Synthesis and evaluation of (E)-4-hydroxy-3-methyl-but-2-enyl diphosphate analogs as competitive partial agonists of butyrophilin 3A1	54
Insight on pyrimido[5,4-g]indolizine and pyrimido[4,5-c]pyrrolo[1,2-a]azepine systems as promising photosensitizers on malignant cells	54
Novel 1,3,4-oxadiazole chalcogen analogues: Synthesis and cytotoxic activity	54
Design, synthesis and in vitro evaluation of novel SARS-CoV-2 3CLpro covalent inhibitors	53
Discovery of 3H-pyrrolo[2,3-c]quinolines with activity against Mycobacterium tuberculosis by allosteric inhibition of the glutamate-5-kinase enzyme	53
Coumarin–benzimidazole hybrids: A review of developments in medicinal chemistry	53
Current trends in computer aided drug design and a highlight of drugs discovered via computational techniques: A review	52
The mechanism of UNC-51-like kinase 1 and the applications of small molecule modulators in cancer treatment	52
Inhibition of Histone Deacetylase 6 (HDAC6) as a therapeutic strategy for Alzheimer's disease: A review (2010–2020)	52
From tryptophan-based amides to tertiary amines: Optimization of a butyrylcholinesterase inhibitor series	51
Novel bifluorescent Zn(II)–cryptolepine–cyclen complexes trigger apoptosis induced by nuclear and mitochondrial DNA damage in cisplatin-resistant lung tumor cells	51
Small-molecule MDM2 inhibitors in clinical trials for cancer therapy	51
Oleanolic acid derivatives against drug-resistant bacteria and fungi by multi-targets to avoid drug resistance	51
Pyrazolopyrimidines as anticancer agents: A review on structural and target-based approaches	51
Graphical abstract TOC	50
Corrigendum to “Discovery of novel tetrahydroquinoline derivatives as potent, selective, and orally Available AR antagonists” [Eur. J. Med. Chem. 291 (2025) 117566]	50
Discovery of novel dual tubulin and MMPs inhibitors for the treatment of lung cancer and overcoming drug resistance	50
Structure-activity relationship studies and design of a PTPN22 inhibitor with enhanced isozyme selectivity and cellular efficacy	50
Novel angiogenesis inhibitors with superoxide anion radical amplification effect: Surmounting the Achilles’ heels of angiogenesis inhibitors and photosensitizers	49
Design and synthesis of novel derivatives of bisepoxylignans as potent anti-inflammatory agents involves the modulation of the M1/M2 microglia phenotype via TLR4/NF-κB signaling pathway	49
Discovery, enantioselective synthesis of myrtucommulone E analogues as tyrosyl-DNA phosphodiesterase 2 inhibitors and their biological activities	49
Novel antimalarial 3-substituted quinolones isosteres with improved pharmacokinetic properties	48
Multicomponent syntheses enable the discovery of novel quisinostat-derived chemotypes as histone deacetylase inhibitors	48
Benzimidazole analogues active against adult Schistosoma mansoni: SAR analyses, In vivo efficacy in mice, and preliminary mechanistic studies as potential inhibitors of hemozoin formation	48
Targeted vancomycin delivery via in situ albumin conjugation and acid-triggered drug release for reduced nephrotoxicity	48
Structure-guided expansion strategy unveils potent allosteric SHP2 inhibitors with synergistic efficacy against AML through MCL-1 co-targeting	48
Synthesis, design, and optimization of a potent and selective series of pyridylpiperazines as promising antimalarial agents	47
Novel dual-target FAAH and TRPV1 ligands as potential pharmacotherapeutics for pain management	47
Nonsteroidal anti-inflammatory drugs (NSAIDs) and nucleotide analog GS-441524 conjugates with potent in vivo efficacy against coronaviruses	47
Small molecular inhibitors targeting Janus kinases (JAKs) for the treatment of psoriasis	47
Editorial Board	47
Synthesis, computational and experimental pharmacological studies for (thio)ether-triazine 5-HT6R ligands with noticeable action on AChE/BChE and chalcogen-dependent intrinsic activity in search for n	46
Discovery of novel diaryl substituted isoquinolin-1(2H)-one derivatives as hypoxia-inducible factor-1 signaling inhibitors for the treatment of rheumatoid arthritis	46
Inhibitors of ABCG2-mediated multidrug resistance: Lead generation through computer-aided drug design	46
Novel boron-modified aza-BODIPY photosensitizers for low-dose light-dependent anti-cancer photodynamic therapy	46
Contents continued	46
Targeting p53 activation: Recent therapeutic advances in cancer and diabetic macular edema	46
2-Phenoxy-3, 4′-bipyridine derivatives inhibit AURKB-dependent mitotic processes by disrupting its localization	45
Discovery of novel triazine derivatives as potent retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists	45
Covalent fragment mapping of KRasG12C revealed novel chemotypes with in vivo potency	45
Briarane-type diterpenoids, the inhibitors of osteoclast formation by interrupting Keap1-Nrf2 interaction and activating Nrf2 pathway	45
Exploring the potential of histone demethylase inhibition in multi-therapeutic approaches for cancer treatment	45
Structure-based discovery of potent USP28 inhibitors derived from Vismodegib	45
Contents continued	45
Reversal of subtype-selectivity and function by the introduction of a para-benzamidyl substituent to N-cyclopropylmethyl nornepenthone	44
Graphical abstract TOC	44
From garden to lab: C-3 chemical modifications of tomatidine unveil broad-spectrum ATP synthase inhibitors to combat bacterial resistance	44
Synthesis and application of small molecules approved for the treatment of lymphoma	43
Amidoxime prodrugs convert to potent cell-active multimodal inhibitors of the dengue virus protease	43
Graphical abstract TOC	43
Graphical abstract TOC	43
Design, development and evaluation of a prodrug-type TrkA-selective inhibitor with antinociceptive effects in vivo	43
Synthesis and biological evaluation of tyrosine derivatives as peripheral 5HT2A receptor antagonists for nonalcoholic fatty liver disease	43
Design, synthesis, in vitro – In vivo biological evaluation of novel thiazolopyrimidine compounds as antileishmanial agent with PTR1 inhibition	42
New broad-spectrum and potent antibacterial agents with dual-targeting mechanism: Promoting FtsZ polymerization and disrupting bacterial membranes	42
Rational design and appraisal of selective Cdc2-Like kinase 1 (Clk1) inhibitors as novel autophagy inducers for the treatment of acute liver injury (ALI)	42
The journey of p38 MAP kinase inhibitors: From bench to bedside in treating inflammatory diseases	42
Structure-directed identification of pyridine-2-methylamine derivatives as MmpL3 inhibitors for use as antitubercular agents	42
Anti-cancer efficacy of novel lonidamine derivatives: Design, synthesis, in vitro, in vivo, and computational studies targeting hexokinase-2	41
Design, synthesis and biological evaluation of new parbendazole derivatives for the treatment of HNSCC	41

Discovery of 2-((2-methylbenzyl)thio)-6-oxo-4-(3,4,5-trimethoxyphenyl)-1,6-dihydropyrimidine-5-carbonitrile as a novel and effective bromodomain and extra-terminal (BET) inhibitor for the treatment of	41
Discovery of novel hybrids containing clioquinol−1-benzyl-1,2,3,6-tetrahydropyridine as multi-target-directed ligands (MTDLs) against Alzheimer's disease	41
Bioisosteric replacement of 1H-1,2,3-triazole with 1H-tetrazole ring enhances anti-leukemic activity of (5-benzylthiazol-2-yl)benzamides	41
Tandem construction of biological relevant aliphatic 5-membered N-heterocycles	41
Aporphines: A privileged scaffold in CNS drug discovery	40
Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models	40
Hydrazinecarboxamides: Comprehensive review of their anticancer, anticonvulsive, anti-inflammatory, enzyme inhibition, antioxidant and other activities	40
An overview on Estrogen receptors signaling and its ligands in breast cancer	40
Discovery of a novel dual-target inhibitor of CDK12 and PARP1 that induces synthetic lethality for treatment of triple-negative breast cancer	40
Design, synthesis, and biological evaluation of diphenyl ether substituted quinazolin-4-amine derivatives as potent EGFRL858R/T790M/C797S inhibitors	40
Design, synthesis and biological evaluation of pleuromutilin-Schiff base hybrids as potent anti-MRSA agents in vitro and in vivo	40
Immunosuppressive effects of new thiophene-based KV1.3 inhibitors	40
Amphiphilic small molecule antimicrobials: From cationic antimicrobial peptides (CAMPs) to mechanism-related, structurally-diverse antimicrobials	39
Synthesis of 10,10′-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro	39
Advancing Src kinase inhibition: From structural design to therapeutic innovation - A comprehensive review	39
Antimicrobial activity of natural and semi-synthetic carbazole alkaloids	39
Structure-based development of potent Plasmodium falciparum M1 and M17 aminopeptidase selective and dual inhibitors via S1′-region optimisation	39
Synthesis and evaluation of small molecule inhibitors of LSD1 for use against MYCN-expressing neuroblastoma	39
Progress of NIR-II fluorescence imaging technology applied to disease diagnosis and treatment	39
Synthesis and evaluation of novel ebselen derivatives as urease inhibitors for combating Helicobacter pylori infections	39
Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo	39
Development of novel S-N3-DABO derivatives as potent non-nucleoside reverse transcriptase inhibitors with improved potency and selectivity	39
Design, synthesis and anticancer evaluation of novel Se-NSAID hybrid molecules: Identification of a Se-indomethacin analog as a potential therapeutic for breast cancer	39
The roles of fused-cyclopropanes in medicinal chemistry: Insights from the past decade	38
Development of fibroblast activation protein-α radiopharmaceuticals: Recent advances and perspectives	38
Mucormycosis: A hidden mystery of fungal infection, possible diagnosis, treatment and development of new therapeutic agents	38
Development of a next-generation endogenous OCT4 inducer and its anti-aging effect in vivo	38
Discovery and optimization of isoliquiritigenin as a death-associated protein kinase 1 inhibitor	38
Design, synthesis and bioactivity evaluation of novel evodiamine derivatives with excellent potency against gastric cancer	38
Promises of anionic calix[n]arenes in life science: State of the art in 2023	38
Synthesis and evaluation of chemical linchpins for highly selective CK2α targeting	38
Discovery of 4-(N-dithiobenzyl piperazine)-1,8-naphthalimide as a potent multi-target antitumor agent with good efficacy, limited toxicity, and low resistance	38
Targeting transthyretin in Alzheimer's disease: Drug discovery of small-molecule chaperones as disease-modifying drug candidates for Alzheimer's disease	37
Discovery of novel β-carboline derivatives as selective AChE inhibitors with GSK-3β inhibitory property for the treatment of Alzheimer's disease	37
Recent advances in triazoles as tyrosinase inhibitors	37
Macrocyclic-based strategy in drug design: From lab to the clinic	37
Antibody-drug conjugates for targeted cancer therapy: Recent advances in potential payloads	37
Microbial-derived peptides with anti-mycobacterial potential	37
3-Hydroxy-pyridin-4(1H)-ones as siderophores mediated delivery of isobavachalcone enhances antibacterial activity against pathogenic Pseudomonas aeruginosa	37
SAR and lead optimization of (Z)-5-(4-hydroxy-3-methoxybenzylidene)-3-(2-morpholinoacetyl)thiazolidine-2,4-dione as a potential multi-target antidiabetic agent	37
Design and synthesis of harmiquins, harmine and chloroquine hybrids as potent antiplasmodial agents	37
Recent progress toward developing axial chirality bioactive compounds	37
Mitochondrial targeted hierarchical drug delivery system based on HA-modified liposomes for cancer therapy	37
O-derivatization of natural tropolone and β-thujaplicin leading to effective inhibitors of human carbonic anhydrases IX and XII	37
Recent developments in antimalarial activities of 4-aminoquinoline derivatives	37
Novel neuroprotective 5,6-dihydropyrido[2′,1':2,3]imidazo[4,5-c]quinoline derivatives acting through cholinesterase inhibition and CB2 signaling modulation	37
Design, synthesis, and biological activity evaluation of novel HDAC3 selective inhibitors for combination with Venetoclax against acute myeloid leukemia	37
Recent advances on the development of NO-releasing molecules (NORMs) for biomedical applications	36
Sensitive quantification of fibroblast activation protein and high-throughput screening for inhibition by FDA-approved compounds	36
Synthesis and evaluation of N-sulfonylpiperidine-3-carboxamide derivatives as capsid assembly modulators inhibiting HBV in vitro and in HBV-transgenic mice	36
An oleanic acid decorated gold nanorod for highly efficient inhibition of hemagglutinin and visible rapid detection of the influenza virus	36
Design and synthesis of new 1,2,3-triazoles derived from eugenol and analogues with in vitro and in vivo activity against Trypanosoma cruzi	36
Design, synthesis, and antitumor evaluation of triazolopyridine derivatives as novel inhibitors for BRD4	36
Quaternary ammonium cations conjugated 5,15-diaryltetranaphtho[2,3]porphyrins as photosensitizers for photodynamic therapy	36
Design, synthesis and biological evaluation of N-substituted nipecotamide derivatives as multifunctional agents for epilepsy treatment	36
A deep learning model for structure-based bioactivity optimization and its application in the bioactivity optimization of a SARS-CoV-2 main protease inhibitor	36
Monofunctional dimetallic Ru(η6-arene) complexes inhibit NOTCH1 signaling pathway and synergistically enhance anticancer effect in combination with cisplatin or vitamin C	36
How many organic small molecules might be used to treat COVID-19? From natural products to synthetic agents	36
AR-A014418-based dual Glycogen Synthase Kinase 3β/Histone Deacetylase inhibitors as potential therapeutics for Alzheimer's disease	36
Mechanistic analysis of diverse click reactions along with their applications	35
Isoalantolactone/hydroxamic acid hybrids as potent dual STAT3/HDAC inhibitors and self-assembled nanoparticles for cancer therapy	35
Designed and synthesized novel tripeptides targeting diabetes and its related pathologies	35
Discovery of a potential anti-ischemic stroke agent by suppressing ferroptosis through the ATF3/SLC7A11/GPX4 pathway	35
Novel dihydropyrimidines as promising EGFR & HER2 inhibitors: Insights from experimental and computational studies	35
Contents continued	35
Positive allosteric modulators of purinergic P2X4 receptors: design, synthesis and therapeutic potential of “click” ligands for multiple sclerosis	35
Prominent supramolecular systems for cancer Therapy: From structural design to tailored applications	35
Discovery of SA-8 as a potent SHP2-AUTAC degrader in cancer therapy	35
Novel E-F ring derivatives of aconitine scaffold as potent Hsp90 inhibitors for the treatment of colorectal cancer	35
Design, synthesis and biological evaluation of dapsone derivatives with broad-spectrum antiviral activity	34
Design, synthesis and biological evaluation of 1,5-disubstituted α-amino tetrazole derivatives as non-covalent inflammasome-caspase-1 complex inhibitors with potential application against immune and i	34
Design, synthesis and biological evaluation of biaryl amide derivatives against SARS-CoV-2 with dual-target mechanism	34
SILAC-based chemoproteomics reveals a neoligan analogue as an anti-inflammatory agent targeting IRGM to ameliorate cytokine storm	34
Expanding the utilization of binding pockets proves to be effective for noncovalent small molecule inhibitors against SARS-CoV-2 Mpro	34
Discovery of 5-(3,4-dihydroxybenzylidene)-1,3-dimethylpyrimidine- 2,4,6(1H,3H,5H)-trione as a novel and effective cardioprotective agent via dual anti-inflammatory and anti-oxidative activities	34
Identification and immunological evaluation of novel TLR2 agonists through structural optimization of Diprovocim	34
Novel substituted 4-(Arylethynyl)-Pyrrolo[2,3-d]pyrimidines negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 5 (mGlu5) Treat depressive disorder in mice	34
New N-aryl-N′-aryl-/(thio)ureido-/sulfamoylamino-derivatives of alkyl/alkylcarbamoyl piperazines: Effect of structural modifications on selectivity over 5-HT1A receptor	34
A novel Al18F-labelled NOTA-modified ubiquicidin 29-41 derivative as a bacterial infection PET imaging agent	34
An 19F NMR fragment-based approach for the discovery and development of BRCA2-RAD51 inhibitors to pursuit synthetic lethality in combination with PARP inhibition in pancreatic cancer	34
Plant-derived strategies to fight against severe acute respiratory syndrome coronavirus 2	34
Graphical abstract TOC	34
Graphical abstract TOC	33
Discovery of a tricyclic farnesoid X receptor agonist HEC96719, a clinical candidate for treatment of non-alcoholic steatohepatitis	33
HDAC8 as a target in drug discovery: Function, structure and design	33
Synthesis and preliminary anticancer evaluation of photo-responsive prodrugs of hydroxymethylene bisphosphonate alendronate	33
Structure-based discovery of potent myosin inhibitors to guide antiparasite drug development	33
Design, synthesis and biological evaluation of conformationnally-restricted analogues of E7010 as inhibitors of tubulin assembly (ITA) and vascular disrupting agents (VDA)	33
Identification of thiophene-benzenesulfonamide derivatives for the treatment of multidrug-resistant tuberculosis	33
4,6-Disubstituted-1H-Indazole-4-Amine derivatives with immune-chemotherapy effect and in vivo antitumor activity	33
Recent advances in the development of inhibitors targeting KRAS-G12C and its related pathways	33
Discovery and development of a novel N-(3-bromophenyl)-{[(phenylcarbamoyl)amino]methyl}-N-hydroxythiophene-2-carboximidamide indoleamine 2,3-dioxygenase inhibitor using knowledge-based drug design	33
Discovery of styrylaniline derivatives as novel alpha-synuclein aggregates ligands	33
Targeting RIPK1-mediated necroptosis, oxidative stress, and ferroptosis: A novel multitarget therapy for ischemic stroke	33
Graphical abstract TOC	33