European Journal of Medicinal Chemistry

Article	Citations
Contents continued	259
Graphical abstract TOC	204
Graphical abstract TOC	201
A brain-targeting dl-3-n-butylphthalide prodrug to treat ischemic stroke	192
[18F]R91150: Improved radiosynthesis and in vivo evaluation as imaging probe for 5-HT2A receptors	166
Synthesis of cinnamoyl tethered indoline derivatives with anti-inflammatory and antioxidant activities	158
Corrigendum to “Structure-based development of N-Arylindole derivatives as Pks13 inhibitors against Mycobacterium tuberculosis” [Europ. J. Med. Chem. 283 (2025) 117148]	127
Identification of novel tetrahydroquinoxaline derived phenyl ureas as modulators of the hepatitis B virus nucleocapsid assembly	126
Synthesis and evaluation of (E)-4-hydroxy-3-methyl-but-2-enyl diphosphate analogs as competitive partial agonists of butyrophilin 3A1	119
Inhibitors of membrane associated serine proteases block replication of coronavirus SARS-CoV-2 and influenza virus H1N1	113
Design and syntheses of a bimolecular STING agonist based on the covalent STING antagonist	112
Discovery of tetrahydrothiazolopyridine-incorporated curcumol derivatives as novel and highly potent anti-cancer agents	110
Rational molecular design converting fascaplysin derivatives to potent broad-spectrum inhibitors against bacterial pathogens via targeting FtsZ	110
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	110
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	104
Identification of novel diarylpyrimidine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against wild-type and K103N mutant viruses	100
A glycyrrhetinic acid-iridium(III) conjugate as a theranostic NIR probe for hepatocellular carcinoma with mitochondrial-targeting ability	96
Design, synthesis, evaluation and X-ray structural studies of potent HIV-1 protease inhibitors containing substituted oxaspirocyclic carbamates as the P2 ligands	94
Peptide inhibitors targeting Ras and Ras-associated protein–protein interactions	94
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	94
Discovery, structural optimization, and anti-tumor bioactivity evaluations of betulinic acid derivatives as a new type of RORγ antagonists	93
Estrogen receptor β-targeted hypoxia-responsive near-infrared fluorescence probes for prostate cancer study	93
Vitamin K-Trolox synergism realized in hybrid neuroprotectant with potent anti-ferroptosi/oxytosis activity, reduced toxicity, and in vivo efficacy in Alzheimer's disease mouse model	92
Discovery of p300 histone acetyltransferase inhibitors bearing an imidazo[4,5-b]pyridine-2-one scaffold for the treatment of multiple myeloma	91
Graphical abstract TOC	90

Discovery of novel fused-heterocycle-bearing diarypyrimidine derivatives as HIV-1 potent NNRTIs targeting tolerant region I for enhanced antiviral activity and resistance profile	89
Synthesis and biological evaluation of novel pyrazole amides as potent mitochondrial complex I inhibitors	88
Trimethyl Lock-2Cl (TML-2Cl): A self-cyclizing adapter for molecular release in antibody-drug conjugates	85
Editorial Board	84
Novel 1,3,4-oxadiazole chalcogen analogues: Synthesis and cytotoxic activity	84
Discovery of the novel Benzo[b]thiophene 1,1-dioxide derivatives as a potent STAT3 inhibitor against idiopathic pulmonary fibrosis	84
Discovery and optimization of 4-pyrazolyl-2-aminopyrimidine derivatives as potent spleen tyrosine kinase (SYK) inhibitors	82
Discovery of anti-tumor targets based on photo-affinity labeling	82
Ligand-based design and synthesis of new trityl histamine and trityl cysteamine derivatives as SIRT2 inhibitors for cancer therapy	80
Novel nitrogen mustard-artemisinin hybrids with potent anti-leukemia action through DNA damage and activation of GPx	80
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.	79
Design, synthesis and bioevaluation of PI3Kα-selective inhibitors as potential colorectal cancer drugs	77
Exploring Si-phthalocyanines with different valency for PSMA-targeted photodynamic therapy: Synthesis and preclinical validation	76
Structure-activity relationship of N-cyclopropylmethyl-7α-(m-methylaminophenyl)-6,14-endoethano-northebaine derivatives as G-protein-biased KOR-selective agonists	75
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	74
Synthesis, anti-allergic rhinitis evaluation and mechanism investigation of novel 1,2,4-triazole-enamides as CB1 R antagonist	74
Synthesis and antibacterial medicinal evaluation of carbothioamido hydrazonyl thiazolylquinolone with multitargeting antimicrobial potential to combat increasingly global resistance	73
Highly potent dipeptidyl peptidase 8/9 (DPP8/9) inhibitors designed via relative binding free energy calculations	73
Synthesis and evaluation of a new class of MIF-inhibitors in activated macrophage cells and in experimental septic shock in mice	71
An update on small molecule compounds targeting synthetic lethality for cancer therapy	71
The mechanism of UNC-51-like kinase 1 and the applications of small molecule modulators in cancer treatment	70
Active fragment assembly strategy enabling fast discovery of KRAS inhibitors against pancreatic cancer cells	70
Discovery of novel fluorine-containing parthenolide analogues as potential antitumor agents	68
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	67
A bivalent anti-CTGF aptamer modulates multiple signaling pathways to attenuate liver fibrosis	67
Design and synthesis of benzothiazole aryl urea derivatives as potent anti-staphylococcal agents targeting autolysin-mediated peptidoglycan hydrolases	67
Nature-inspired new isoindole-based Passerini adducts as efficient tumor-selective apoptotic inducers via caspase-3/7 activation	66
Novel 6-hydroxybenzothiazol-2-carboxamides as potent and selective monoamine oxidase B inhibitors endowed with neuroprotective activity	66
6-Regioisomeric 5,8-quinolinediones as potent CDC25 inhibitors against colorectal cancers	66
A medicinal chemistry perspective on disruptor of telomeric silencing 1-like: Its mechanisms and modulators in cancer treatment	65
Design, synthesis, and biological evaluation of hybrids from both nitrones with eNOS-mimicking activity and selective iNOS inhibitors for the treatment of ischemic stroke	64
A pro-death autophagy-based nanoplatform for enhancing antitumour efficacy with improved immune responses	64
Exploring the modulatory influence on the antimalarial activity of amodiaquine using scaffold hybridisation with ferrocene integration	63
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	63
Histone deacetylases (HDACs) as the promising immunotherapeutic targets for hematologic cancer treatment	63
A decade of USFDA-approved small molecules as anti-inflammatory agents: Recent trends and Commentaries on the “industrial” perspective	63
New β-arylchalcogeno amines with procognitive properties targeting Carbonic Anhydrases and Monoamine Oxidases	62
Exploration of P1 and P4 modifications of nirmatrelvir: Design, synthesis, biological evaluation, and X-ray structural studies of SARS-CoV-2 Mpro inhibitors	62
Discovery of novel dual tubulin and MMPs inhibitors for the treatment of lung cancer and overcoming drug resistance	61
Discovery of N-(5-amido-2-methylphenyl)-5-methylisoxazole-3-carboxamide as dual CSF-1R/c-Kit Inhibitors with improved stability and BBB permeability	60
Discovery and biological evaluation of 6-aryl-4-(3,4,5-trimethoxyphenyl)quinoline derivatives with promising antitumor activities as novel colchicine-binding site inhibitors	60
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	60
Novel pterostilbene derivatives ameliorate heart failure by reducing oxidative stress and inflammation through regulating Nrf2/NF-κB signaling pathway	60
Synthesis of diarylpentane derivatives as novel α-glucosidase inhibitors: Their inhibitory mechanism and hypoglycemic effects	60
Water molecules in the cannabinoid receptor 2 binding site crucially impact the discovery of novel ligands	58
Fluorinated sulfonamide-flavonoid derivatives as novel Keap1-Nrf2 inhibitors: Potent induction of cytoprotective gene HO-1 in vivo	58
Oleanolic acid derivatives against drug-resistant bacteria and fungi by multi-targets to avoid drug resistance	57
Multitarget-directed carbamate and carbamothioate derivatives: Cholinesterase and monoamine oxidase inhibition, anti-β-amyloid (Aβ) aggregation, antioxidant and blood–brain barrier permeation properti	57
Poly(ADP-ribose) polymerase-1 (PARP1)-based dual inhibitors targeting cancer synthetic lethality (2022-present): advances and perspectives	57
Recent developments in the synthesis of indolizines and their derivatives as compounds of interest in medicinal chemistry: a review	57

Monoamine oxidase inhibitors: A concise review with special emphasis on structure activity relationship studies	57
Functional quinoline-malononitriles for enhanced wound repair and monitoring	56
Engineering a biomimicking strategy for discovering nonivamide-based quorum-sensing inhibitors for controlling bacterial infection	56
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	56
Discovery of a potent, selective and cell active inhibitor of m6A demethylase ALKBH5	56
The first ADC bearing the ferroptosis inducer RSL3 as a payload with conservation of the fragile electrophilic warhead	56
Arginine and tryptophan-rich dendritic antimicrobial peptides that disrupt membranes for bacterial infection in vivo	56
Amino acid–modified chalcone derivatives with in vitro and in vivo efficacy against colon cancer	55
Discovery of novel Thieno[2,3-d]imidazole derivatives as agonists of human STING for antitumor immunotherapy using systemic administration	55
Design, synthesis, and biological evaluation of piperazine derivatives as pan-PPARs agonists for the treatment of liver fibrosis	55
Discovery of small molecules for autophagy-lysosome degradation of immune checkpoint proteins	55
EGCG-like non-competitive inhibitor of DYRK1A rescues cognitive defect in a down syndrome model	55
Synthesis and evaluation of 3,4,5-trisubstituted triazoles as G protein-biased kappa opioid receptor agonists	54
1,3-Thiazole nucleus as promising molecular platform against antimicrobial resistance: a recent overview in drug discovery	54
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	54
Antitumor activity and transcriptome sequencing (RNA-seq) analyses of hepatocellular carcinoma cells in response to exposure triterpene-nucleoside conjugates	54
Novel β-carboline derivatives show promise as dual-target inhibitors of DNA and TOP2A for the treatment of triple negative breast cancer	53
Bestatin analogs-4-quinolinone hybrids as antileishmanial hits: Design, repurposing rational, synthesis, in vitro and in silico studies	53
Synthesis and biological evaluation of α-D-tocopherol derivatives as anticancer agents targeting mitochondrial metabolism	52
Application of deuterium in research and development of drugs	52
Novel bifluorescent Zn(II)–cryptolepine–cyclen complexes trigger apoptosis induced by nuclear and mitochondrial DNA damage in cisplatin-resistant lung tumor cells	52
Identification of “dual-site”-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase	52
Design and synthesis of forsythin derivatives as anti-inflammatory agents for acute lung injury	52
Applications of oxetanes in drug discovery and medicinal chemistry	52
Graphical abstract TOC	51
Discovery of ML210-Based glutathione peroxidase 4 (GPX4) degrader inducing ferroptosis of human cancer cells	51
Graphical abstract TOC	50
Development of a next-generation endogenous OCT4 inducer and its anti-aging effect in vivo	50
Novel angiogenesis inhibitors with superoxide anion radical amplification effect: Surmounting the Achilles’ heels of angiogenesis inhibitors and photosensitizers	50
Hydrazinecarboxamides: Comprehensive review of their anticancer, anticonvulsive, anti-inflammatory, enzyme inhibition, antioxidant and other activities	49
Editorial Board	49
Graphical abstract TOC	49
Benzimidazole analogues active against adult Schistosoma mansoni: SAR analyses, In vivo efficacy in mice, and preliminary mechanistic studies as potential inhibitors of hemozoin formation	49
Development of novel S-N3-DABO derivatives as potent non-nucleoside reverse transcriptase inhibitors with improved potency and selectivity	49
Synthesis and biological evaluation of N–O heterobicyclic ring systems derived from 1,2-dihydropyridines as novel TRPA1 activators: implication in GLP-1 release and neuroprotection	49
Novel dual-target FAAH and TRPV1 ligands as potential pharmacotherapeutics for pain management	48
Discovery of 4-(N-dithiobenzyl piperazine)-1,8-naphthalimide as a potent multi-target antitumor agent with good efficacy, limited toxicity, and low resistance	48
Synthesis and evaluation of chemical linchpins for highly selective CK2α targeting	48
Amphiphilic small molecule antimicrobials: From cationic antimicrobial peptides (CAMPs) to mechanism-related, structurally-diverse antimicrobials	48
Design, synthesis, in vitro – In vivo biological evaluation of novel thiazolopyrimidine compounds as antileishmanial agent with PTR1 inhibition	47
Discovery, enantioselective synthesis of myrtucommulone E analogues as tyrosyl-DNA phosphodiesterase 2 inhibitors and their biological activities	47
Targeted vancomycin delivery via in situ albumin conjugation and acid-triggered drug release for reduced nephrotoxicity	47
Immunosuppressive effects of new thiophene-based KV1.3 inhibitors	47
Contents continued	47
Structure-guided expansion strategy unveils potent allosteric SHP2 inhibitors with synergistic efficacy against AML through MCL-1 co-targeting	47
Discovery of indolinone-based covalent ULK1 inhibitors that suppressed autophagy and induced apoptosis against colorectal carcinoma	47
Inhibitors of ABCG2-mediated multidrug resistance: Lead generation through computer-aided drug design	47
Graphical abstract TOC	47
Reversal of subtype-selectivity and function by the introduction of a para-benzamidyl substituent to N-cyclopropylmethyl nornepenthone	46
O-derivatization of natural tropolone and β-thujaplicin leading to effective inhibitors of human carbonic anhydrases IX and XII	46
Synthesis of amide-linked panaxadiol-indolinedione derivatives: A novel NSD2/H3K36me2 epigenetic modulator with significant antitumor efficacy	46
Microbial-derived peptides with anti-mycobacterial potential	46
Discovery and optimization of isoliquiritigenin as a death-associated protein kinase 1 inhibitor	46
Accelerated de novo design of xanthine oxidase-inhibitory peptides via physics-informed computational approaches	46
Fenbendazole–amino acid derivatives as novel anthelmintic candidates: Synthesis, activity against Haemonchus contortus, and in silico profiling	46
The novel SIRT2-targeted PROTAC degraders as the efficient agents for the treatment of ovarian cancer	46
Discovery of novel hybrids containing clioquinol−1-benzyl-1,2,3,6-tetrahydropyridine as multi-target-directed ligands (MTDLs) against Alzheimer's disease	46
2-Phenoxy-3, 4′-bipyridine derivatives inhibit AURKB-dependent mitotic processes by disrupting its localization	46
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
Bioisosteric replacement of 1H-1,2,3-triazole with 1H-tetrazole ring enhances anti-leukemic activity of (5-benzylthiazol-2-yl)benzamides	45
Corrigendum to “Discovery of novel tetrahydroquinoline derivatives as potent, selective, and orally Available AR antagonists” [Eur. J. Med. Chem. 291 (2025) 117566]	45
Briarane-type diterpenoids, the inhibitors of osteoclast formation by interrupting Keap1-Nrf2 interaction and activating Nrf2 pathway	45
Synthesis and biological evaluation of tyrosine derivatives as peripheral 5HT2A receptor antagonists for nonalcoholic fatty liver disease	45
Monofunctional dimetallic Ru(η6-arene) complexes inhibit NOTCH1 signaling pathway and synergistically enhance anticancer effect in combination with cisplatin or vitamin C	45
Recent progress toward developing axial chirality bioactive compounds	44
From garden to lab: C-3 chemical modifications of tomatidine unveil broad-spectrum ATP synthase inhibitors to combat bacterial resistance	44
Recent advances in triazoles as tyrosinase inhibitors	44
Discovery of novel triazine derivatives as potent retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists	44
Novel boron-modified aza-BODIPY photosensitizers for low-dose light-dependent anti-cancer photodynamic therapy	44
Design, synthesis and biological evaluation of new parbendazole derivatives for the treatment of HNSCC	44
3-Hydroxy-pyridin-4(1H)-ones as siderophores mediated delivery of isobavachalcone enhances antibacterial activity against pathogenic Pseudomonas aeruginosa	43
Discovery of antileishmanial hits in the 3-nitroimidazo[1,2-a]pyridine series via newly optimized tetrakis(dimethylamino)ethylene (TDAE) methodology at position 2	43
Multicomponent syntheses enable the discovery of novel quisinostat-derived chemotypes as histone deacetylase inhibitors	43
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	43
Design, development and evaluation of a prodrug-type TrkA-selective inhibitor with antinociceptive effects in vivo	43
Design, synthesis, and biological evaluation of diphenyl ether substituted quinazolin-4-amine derivatives as potent EGFRL858R/T790M/C797S inhibitors	43
Synthesis of 10,10′-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro	43
Integration of computational and experimental techniques for the discovery of PLpro covalent inhibitors. When large virtual screening and rational design meet	42
Covalent fragment mapping of KRasG12C revealed novel chemotypes with in vivo potency	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

Targeting p53 activation: Recent therapeutic advances in cancer and diabetic macular edema	42
Macrocyclic-based strategy in drug design: From lab to the clinic	42
Recent developments in antimalarial activities of 4-aminoquinoline derivatives	41
Design and synthesis of novel cyclin-dependent kinase 4/6(CDK4/6) and histone deacetylase (HDAC) dual inhibitors: In vitro and in vivo anticancer activity	41
Small molecular inhibitors targeting Janus kinases (JAKs) for the treatment of psoriasis	41
Spiranic compounds as novel AMPK paradoxical inhibitors: can we derive new mechanistic insights?	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
Nonsteroidal anti-inflammatory drugs (NSAIDs) and nucleotide analog GS-441524 conjugates with potent in vivo efficacy against coronaviruses	41
N-acylated aminoguanidine-benzenesulfonamides: rational design, synthesis, and dual apoptotic mechanisms of anticancer activity involving VEGFR-2 inhibition and VEGFR-2–independent pathways	41
Synthesis and evaluation of small molecule inhibitors of LSD1 for use against MYCN-expressing neuroblastoma	41
Design, synthesis and evaluation of novel oxadiazole-based compounds as potential Rac1 inhibitors against breast cancer	41
Recent advances on the development of NO-releasing molecules (NORMs) for biomedical applications	41
Discovery of novel diaryl substituted isoquinolin-1(2H)-one derivatives as hypoxia-inducible factor-1 signaling inhibitors for the treatment of rheumatoid arthritis	41
Aporphines: A privileged scaffold in CNS drug discovery	41
The application prospects of amino acid deprivation for cancer therapy	41
Structure-activity relationship studies and design of a PTPN22 inhibitor with enhanced isozyme selectivity and cellular efficacy	40
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	40
Discovery of a novel dual-target inhibitor of CDK12 and PARP1 that induces synthetic lethality for treatment of triple-negative breast cancer	40
Synthesis and biological evaluation of C-28-modified pyrazole-fused betulinic acid derivatives as potent antiosteoporosis agents	40
Structure-directed identification of pyridine-2-methylamine derivatives as MmpL3 inhibitors for use as antitubercular agents	40
Antibody-drug conjugates for targeted cancer therapy: Recent advances in potential payloads	40
Design, synthesis and anticancer evaluation of novel Se-NSAID hybrid molecules: Identification of a Se-indomethacin analog as a potential therapeutic for breast cancer	40
A deep learning model for structure-based bioactivity optimization and its application in the bioactivity optimization of a SARS-CoV-2 main protease inhibitor	40
Design, synthesis, and antitumor evaluation of triazolopyridine derivatives as novel inhibitors for BRD4	40
Research and development of natural product Salidroside: Pharmacology, total synthesis and structural modifications	40
Design and synthesis of harmiquins, harmine and chloroquine hybrids as potent antiplasmodial agents	40
Rational design of next-generation FLT3 inhibitors in acute myeloid leukemia: From laboratory to clinics	40
An overview on Estrogen receptors signaling and its ligands in breast cancer	39
Promises of anionic calix[n]arenes in life science: State of the art in 2023	39
Ketoconazole-carbonic anhydrase inhibitors as potential anticancer agents	39
Synthesis and evaluation of novel ebselen derivatives as urease inhibitors for combating Helicobacter pylori infections	39
Mitochondrial targeted hierarchical drug delivery system based on HA-modified liposomes for cancer therapy	39
Mucormycosis: A hidden mystery of fungal infection, possible diagnosis, treatment and development of new therapeutic agents	39
New broad-spectrum and potent antibacterial agents with dual-targeting mechanism: Promoting FtsZ polymerization and disrupting bacterial membranes	38
Expanding the antiviral arsenal: N-arylated 1,2,4-oxadiazol-5(4H)-ones show high activity against orthopoxviruses	38
Synthesis, design, and optimization of a potent and selective series of pyridylpiperazines as promising antimalarial agents	38
Anti-cancer efficacy of novel lonidamine derivatives: Design, synthesis, in vitro, in vivo, and computational studies targeting hexokinase-2	38
Novel antimalarial 3-substituted quinolones isosteres with improved pharmacokinetic properties	38
The journey of p38 MAP kinase inhibitors: From bench to bedside in treating inflammatory diseases	38
Development of fibroblast activation protein-α radiopharmaceuticals: Recent advances and perspectives	38
Synthesis and application of small molecules approved for the treatment of lymphoma	38
Novel neuroprotective 5,6-dihydropyrido[2′,1':2,3]imidazo[4,5-c]quinoline derivatives acting through cholinesterase inhibition and CB2 signaling modulation	38
Exploring the potential of histone demethylase inhibition in multi-therapeutic approaches for cancer treatment	38
Design, synthesis, and biological activity evaluation of novel HDAC3 selective inhibitors for combination with Venetoclax against acute myeloid leukemia	38
Advancing Src kinase inhibition: From structural design to therapeutic innovation - A comprehensive review	38
Design and synthesis of new 1,2,3-triazoles derived from eugenol and analogues with in vitro and in vivo activity against Trypanosoma cruzi	38
Structure-based development of potent Plasmodium falciparum M1 and M17 aminopeptidase selective and dual inhibitors via S1′-region optimisation	38
Natural alkaloids with therapeutic potential against Alzheimer's disease through cholinesterase inhibition	37
Corrigendum to “Designing anticancer copper(II) complexes by optimizing 2-pyridine-thiosemicarbazone ligands” [Eur. J. Med. Chem. 158 (2018) 442–452]	37
Discovery, Synthesis, and Biological Evaluation of N,N′-Diacyl-m-Phenylenediamine Derivatives as Novel PCSK9 Small-Molecule Inhibitors	37
Research progress and challenges of TRPV1 channel modulators as a prospective therapy for diabetic neuropathic pain	37
Progress of NIR-II fluorescence imaging technology applied to disease diagnosis and treatment	37
Structure-based discovery of potent USP28 inhibitors derived from Vismodegib	37
The roles of fused-cyclopropanes in medicinal chemistry: Insights from the past decade	37
Structure-activity relationship study of new carbazole sulfonamide derivatives as anticancer agents with dual-target mechanism	37
Synthetic α-glucosidase inhibitory peptides designed by molecular docking: In vitro screening and anti-hyperglycemic efficacy in diabetic mice	37
Antimicrobial activity of natural and semi-synthetic carbazole alkaloids	37
Assessing the anti-leukemic efficacy of a curcuminoid in cellular and animal models	37
Contents continued	37
Rational design and optimization of novel 4-methyl quinazoline derivatives as PI3K/HDAC dual inhibitors with benzamide as zinc binding moiety for the treatment of acute myeloid leukemia	36
Novel dihydropyrimidines as promising EGFR & HER2 inhibitors: Insights from experimental and computational studies	36
Graphical abstract TOC	36
AR-A014418-based dual Glycogen Synthase Kinase 3β/Histone Deacetylase inhibitors as potential therapeutics for Alzheimer's disease	36
Unveiling ortho-phenolic Mannich ciprofloxacin-chalcone conjugates with potential antineoplastic activity: synthesis, mechanistic study, in silico docking and molecular dynamic simulation	36
Corrigendum to “Aromatic π-stacking stabilizes an α-helical SARS-CoV-2 MPER peptide that mimics the post-fusion spike and enables potent antiviral activity” [Eur. J. Med. Chem. 317 (2026) 119122]	36
Design, synthesis and biological evaluation of conformationnally-restricted analogues of E7010 as inhibitors of tubulin assembly (ITA) and vascular disrupting agents (VDA)	36
How generative Artificial Intelligence can transform drug discovery?	36
Synthesis and mitochondria-localized iridium (III) complexes induce cell death through pyroptosis and ferroptosis pathways	36
Graphical abstract TOC	36
Design, synthesis and activity evaluation of benzene sulfonamide derivatives as novel androgen receptor antagonist	36
New antitubercular pretomanid analogues as potent payloads in polymeric micelles: Leveraging zebrafish assays to accelerate lead optimisation	35
Discovery of potent and selective c-Met inhibitors for MET-amplified hepatocellular carcinoma treatment	35
Structure-based discovery of potent myosin inhibitors to guide antiparasite drug development	35
Editorial Board	35
Expanding the utilization of binding pockets proves to be effective for noncovalent small molecule inhibitors against SARS-CoV-2 Mpro	35
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	35
Design, synthesis, and biological evaluation of novel 7-substituted 10,11-methylenedioxy-camptothecin derivatives against drug-resistant small-cell lung cancer in vitro and in vivo	35
Plant-derived strategies to fight against severe acute respiratory syndrome coronavirus 2	35
Editorial Board	35
Acyclic purine and pyrimidine nucleotide analogs as ecto-5′-nucleotidase (CD73) inhibitors	35
Synthesis and structure-activity relationships of novel 14-membered 2-fluoro ketolides with structural modification at the C11 position	35
Sensitive quantification of fibroblast activation protein and high-throughput screening for inhibition by FDA-approved compounds	35
2-(Phenylamino)-7,8-dihydroquinazolin-5(6H)-one, a promising scaffold for MAO-B inhibitors with potential GSK3β targeting	35
Design, synthesis and biological evaluation of biaryl amide derivatives against SARS-CoV-2 with dual-target mechanism	35
Graphical abstract TOC	35
An overview of RAF kinases and their inhibitors (2019–2023)	34
Unlocking the potential of TNF: From biologic agents to small-molecule inhibitors	34
Comprehensive coverage on anti-mycobacterial endeavour reported during 2022	34
Bicyclic 2-aminopyrimidine derivatives as potent VEGFR-2 inhibitors and apoptosis Inducers: Structure-Guided design, synthesis, anticancer assessment, and in-silico exploration	34
Covalent inhibitors meet epigenetics: New opportunities	34
Design, synthesis and anti-ovarian cancer activities of thieno[2,3-d]pyrimidine based chimeric BRD4 inhibitor/nitric oxide-donator	34
Designed and synthesized novel tripeptides targeting diabetes and its related pathologies	34
Discovery of 4-amino-1,6-dihydro-7H-pyrrolo[2,3-d]pyridazin-7-one derivatives as potential receptor-interacting serine/threonine-protein kinase 1 (RIPK1) inhibitors	34
Positive allosteric modulators of purinergic P2X4 receptors: design, synthesis and therapeutic potential of “click” ligands for multiple sclerosis	34
Corrigendum to “Design, synthesis, and biological evaluation of 1,6-naphthyridine-2-one derivatives as novel FGFR4 inhibitors for the treatment of colorectal cancer” [Eur. J. Med. Chem. 259 (2023) 115	34