European Journal of Medicinal Chemistry

Papers
(The median citation count of European Journal of Medicinal Chemistry is 5. The table below lists those papers that are above that threshold based on CrossRef citation counts [max. 250 papers]. The publications cover those that have been published in the past four years, i.e., from 2022-01-01 to 2026-01-01.)
ArticleCitations
Contents continued242
Graphical abstract TOC203
Graphical abstract TOC202
Nature-inspired new isoindole-based Passerini adducts as efficient tumor-selective apoptotic inducers via caspase-3/7 activation176
Synthesis and evaluation of (E)-4-hydroxy-3-methyl-but-2-enyl diphosphate analogs as competitive partial agonists of butyrophilin 3A1172
Synthesis of tropane-based σ1 receptor antagonists with antiallodynic activity163
Graphical abstract contents continued163
Design and synthesis of forsythin derivatives as anti-inflammatory agents for acute lung injury134
Identification of novel tetrahydroquinoxaline derived phenyl ureas as modulators of the hepatitis B virus nucleocapsid assembly134
Editorial Board121
Discovery of N-(5-amido-2-methylphenyl)-5-methylisoxazole-3-carboxamide as dual CSF-1R/c-Kit Inhibitors with improved stability and BBB permeability113
Synthesis and biological evaluation of novel pyrazole amides as potent mitochondrial complex I inhibitors105
Rational drug design to explore the structure-activity relationship (SAR) of TRK inhibitors with 2,4-diaminopyrimidine scaffold104
Recent developments in the synthesis of indolizines and their derivatives as compounds of interest in medicinal chemistry: a review102
Corrigendum to “Structure-based development of N-Arylindole derivatives as Pks13 inhibitors against Mycobacterium tuberculosis” [Europ. J. Med. Chem. 283 (2025) 117148]101
Novel nitrogen mustard-artemisinin hybrids with potent anti-leukemia action through DNA damage and activation of GPx100
A brain-targeting dl-3-n-butylphthalide prodrug to treat ischemic stroke99
Design, synthesis, evaluation and X-ray structural studies of potent HIV-1 protease inhibitors containing substituted oxaspirocyclic carbamates as the P2 ligands96
Fluorinated sulfonamide-flavonoid derivatives as novel Keap1-Nrf2 inhibitors: Potent induction of cytoprotective gene HO-1 in vivo95
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. 94
Peptide inhibitors targeting Ras and Ras-associated protein–protein interactions90
Structure-based approaches for the design of 6-aryl-1-(3,4,5-trimethoxyphenyl)-1H-benzo[d][1,2,3]triazoles as tubulin polymerization inhibitors90
Synthesis, anti-allergic rhinitis evaluation and mechanism investigation of novel 1,2,4-triazole-enamides as CB1 R antagonist89
Bestatin analogs-4-quinolinone hybrids as antileishmanial hits: Design, repurposing rational, synthesis, in vitro and in silico studies87
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 arthritis85
Novel 1,3,4-oxadiazole chalcogen analogues: Synthesis and cytotoxic activity84
[18F]R91150: Improved radiosynthesis and in vivo evaluation as imaging probe for 5-HT2A receptors84
Anthraquinone derivatives as ADP-competitive inhibitors of liver pyruvate kinase84
Amino acid–modified chalcone derivatives with in vitro and in vivo efficacy against colon cancer83
Arginine and tryptophan-rich dendritic antimicrobial peptides that disrupt membranes for bacterial infection in vivo82
Non-nucleoside structured compounds with antiviral activity—past 10 years (2010–2020)81
Synthesis and evaluation of a new class of MIF-inhibitors in activated macrophage cells and in experimental septic shock in mice81
Water molecules in the cannabinoid receptor 2 binding site crucially impact the discovery of novel ligands81
Discovery of novel Thieno[2,3-d]imidazole derivatives as agonists of human STING for antitumor immunotherapy using systemic administration80
Novel β-carboline derivatives show promise as dual-target inhibitors of DNA and TOP2A for the treatment of triple negative breast cancer77
Design, synthesis and bioevaluation of PI3Kα-selective inhibitors as potential colorectal cancer drugs75
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 model75
Synthesis and biological evaluation of α-D-tocopherol derivatives as anticancer agents targeting mitochondrial metabolism74
Discovery of small molecules for autophagy-lysosome degradation of immune checkpoint proteins73
6-Regioisomeric 5,8-quinolinediones as potent CDC25 inhibitors against colorectal cancers72
Design, synthesis and biological evaluation of N-benzylaryl cinnamide derivatives as tubulin polymerization inhibitors capable of promoting YAP degradation with potent anti-gastric cancer activities72
Discovery of novel fluorine-containing parthenolide analogues as potential antitumor agents72
Synthesis of diarylpentane derivatives as novel α-glucosidase inhibitors: Their inhibitory mechanism and hypoglycemic effects72
Exploring the modulatory influence on the antimalarial activity of amodiaquine using scaffold hybridisation with ferrocene integration71
Estrogen receptor β-targeted hypoxia-responsive near-infrared fluorescence probes for prostate cancer study70
Synthesis and evaluation of 3,4,5-trisubstituted triazoles as G protein-biased kappa opioid receptor agonists70
Exploring Si-phthalocyanines with different valency for PSMA-targeted photodynamic therapy: Synthesis and preclinical validation70
Discovery of 3H-pyrrolo[2,3-c]quinolines with activity against Mycobacterium tuberculosis by allosteric inhibition of the glutamate-5-kinase enzyme67
Synthesis of 8-aminomorphans with high KOR affinity67
A glycyrrhetinic acid-iridium(III) conjugate as a theranostic NIR probe for hepatocellular carcinoma with mitochondrial-targeting ability66
Synthesis and evaluation of a novel class of spiro[chromene-2,2′-indoline] derivatives as potent inhibitors of peptidylarginine deiminase IV to treat rheumatoid arthritis66
1,3-Thiazole nucleus as promising molecular platform against antimicrobial resistance: a recent overview in drug discovery65
Design and synthesis of benzothiazole aryl urea derivatives as potent anti-staphylococcal agents targeting autolysin-mediated peptidoglycan hydrolases64
Identification of “dual-site”-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase64
Identification of novel diarylpyrimidine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against wild-type and K103N mutant viruses63
Discovery of novel fused-heterocycle-bearing diarypyrimidine derivatives as HIV-1 potent NNRTIs targeting tolerant region I for enhanced antiviral activity and resistance profile63
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 cytotoxicity62
Structure-based discovery of a 4,5-Dihydropyrazole-cored PET ligand for imaging of receptor-interacting serine/threonine-protein kinase 1 (RIPK1) in the brain61
Discovery of the novel Benzo[b]thiophene 1,1-dioxide derivatives as a potent STAT3 inhibitor against idiopathic pulmonary fibrosis61
Insight on pyrimido[5,4-g]indolizine and pyrimido[4,5-c]pyrrolo[1,2-a]azepine systems as promising photosensitizers on malignant cells61
Exploration of P1 and P4 modifications of nirmatrelvir: Design, synthesis, biological evaluation, and X-ray structural studies of SARS-CoV-2 Mpro inhibitors60
Discovery of anti-tumor targets based on photo-affinity labeling60
Ligand-based design and synthesis of new trityl histamine and trityl cysteamine derivatives as SIRT2 inhibitors for cancer therapy60
Design, synthesis, and biological evaluation of piperazine derivatives as pan-PPARs agonists for the treatment of liver fibrosis60
Novel pterostilbene derivatives ameliorate heart failure by reducing oxidative stress and inflammation through regulating Nrf2/NF-κB signaling pathway59
Design and syntheses of a bimolecular STING agonist based on the covalent STING antagonist59
Novel 6-hydroxybenzothiazol-2-carboxamides as potent and selective monoamine oxidase B inhibitors endowed with neuroprotective activity59
Inhibitors of membrane associated serine proteases block replication of coronavirus SARS-CoV-2 and influenza virus H1N158
Multitarget-directed carbamate and carbamothioate derivatives: Cholinesterase and monoamine oxidase inhibition, anti-β-amyloid (Aβ) aggregation, antioxidant and blood–brain barrier permeation properti57
A decade of USFDA-approved small molecules as anti-inflammatory agents: Recent trends and Commentaries on the “industrial” perspective57
Discovery, structural optimization, and anti-tumor bioactivity evaluations of betulinic acid derivatives as a new type of RORγ antagonists57
Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis57
Discovery of novel dual tubulin and MMPs inhibitors for the treatment of lung cancer and overcoming drug resistance56
EGCG-like non-competitive inhibitor of DYRK1A rescues cognitive defect in a down syndrome model56
Poly(ADP-ribose) polymerase-1 (PARP1)-based dual inhibitors targeting cancer synthetic lethality (2022-present): advances and perspectives56
New β-arylchalcogeno amines with procognitive properties targeting Carbonic Anhydrases and Monoamine Oxidases56
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 therapy56
Rational design, synthesis and biological evaluation of dual PARP-1/2 and TNKS1/2 inhibitors for cancer therapy56
Small-molecule MDM2 inhibitors in clinical trials for cancer therapy56
The mechanism of UNC-51-like kinase 1 and the applications of small molecule modulators in cancer treatment56
From tryptophan-based amides to tertiary amines: Optimization of a butyrylcholinesterase inhibitor series55
Applications of oxetanes in drug discovery and medicinal chemistry55
Antitumor activity and transcriptome sequencing (RNA-seq) analyses of hepatocellular carcinoma cells in response to exposure triterpene-nucleoside conjugates55
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 inhibitor55
Monoamine oxidase inhibitors: A concise review with special emphasis on structure activity relationship studies54
Antioxidant, anti-inflammatory and immunomodulatory roles of vitamins in COVID-19 therapy53
Discovery and biological evaluation of 6-aryl-4-(3,4,5-trimethoxyphenyl)quinoline derivatives with promising antitumor activities as novel colchicine-binding site inhibitors53
Design, synthesis and in vitro evaluation of novel SARS-CoV-2 3CLpro covalent inhibitors52
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 52
Exploration of 2-phenylquinoline-4-carboxamide linked benzene sulfonamide derivatives as isoform selective inhibitors of transmembrane human carbonic anhydrases52
Synthesis of cinnamoyl tethered indoline derivatives with anti-inflammatory and antioxidant activities51
Oleanolic acid derivatives against drug-resistant bacteria and fungi by multi-targets to avoid drug resistance51
Cinnamic acid derivatives linked to arylpiperazines as novel potent inhibitors of tyrosinase activity and melanin synthesis51
Engineering a biomimicking strategy for discovering nonivamide-based quorum-sensing inhibitors for controlling bacterial infection51
Discovery and optimization of 4-pyrazolyl-2-aminopyrimidine derivatives as potent spleen tyrosine kinase (SYK) inhibitors50
The first ADC bearing the ferroptosis inducer RSL3 as a payload with conservation of the fragile electrophilic warhead50
Novel bifluorescent Zn(II)–cryptolepine–cyclen complexes trigger apoptosis induced by nuclear and mitochondrial DNA damage in cisplatin-resistant lung tumor cells50
Straightforward access to novel mitochondriotropics derived from 2-arylethanol as potent and selective antiproliferative agents50
An update on small molecule compounds targeting synthetic lethality for cancer therapy49
Design, synthesis and promising anti-tumor efficacy of novel imidazo[1,2-a]pyridine derivatives as potent autotaxin allosteric inhibitors49
Coumarin–benzimidazole hybrids: A review of developments in medicinal chemistry49
Platinum(IV) complexes as inhibitors of CD47-SIRPα axis for chemoimmunotherapy of cancer49
Discovery of ML210-Based glutathione peroxidase 4 (GPX4) degrader inducing ferroptosis of human cancer cells49
Histone deacetylases (HDACs) as the promising immunotherapeutic targets for hematologic cancer treatment49
Synthesis and antibacterial medicinal evaluation of carbothioamido hydrazonyl thiazolylquinolone with multitargeting antimicrobial potential to combat increasingly global resistance49
Discovery of a potent, selective and cell active inhibitor of m6A demethylase ALKBH549
Application of deuterium in research and development of drugs49
Rational molecular design converting fascaplysin derivatives to potent broad-spectrum inhibitors against bacterial pathogens via targeting FtsZ48
Highly potent dipeptidyl peptidase 8/9 (DPP8/9) inhibitors designed via relative binding free energy calculations48
A pro-death autophagy-based nanoplatform for enhancing antitumour efficacy with improved immune responses48
Structure-activity relationship studies and design of a PTPN22 inhibitor with enhanced isozyme selectivity and cellular efficacy47
Corrigendum to “Discovery of novel tetrahydroquinoline derivatives as potent, selective, and orally Available AR antagonists” [Eur. J. Med. Chem. 291 (2025) 117566]47
Graphical abstract TOC47
The roles of fused-cyclopropanes in medicinal chemistry: Insights from the past decade46
Natural alkaloids with therapeutic potential against Alzheimer's disease through cholinesterase inhibition46
Novel angiogenesis inhibitors with superoxide anion radical amplification effect: Surmounting the Achilles’ heels of angiogenesis inhibitors and photosensitizers46
Structure-based development of potent Plasmodium falciparum M1 and M17 aminopeptidase selective and dual inhibitors via S1′-region optimisation46
Design, synthesis, and biological activity evaluation of novel HDAC3 selective inhibitors for combination with Venetoclax against acute myeloid leukemia45
Design and synthesis of new 1,2,3-triazoles derived from eugenol and analogues with in vitro and in vivo activity against Trypanosoma cruzi45
Design, synthesis and biological evaluation of new parbendazole derivatives for the treatment of HNSCC44
Macrocyclic-based strategy in drug design: From lab to the clinic44
Advancing Src kinase inhibition: From structural design to therapeutic innovation - A comprehensive review44
Briarane-type diterpenoids, the inhibitors of osteoclast formation by interrupting Keap1-Nrf2 interaction and activating Nrf2 pathway44
Aporphines: A privileged scaffold in CNS drug discovery44
Recent advances on the development of NO-releasing molecules (NORMs) for biomedical applications44
Microbial-derived peptides with anti-mycobacterial potential43
Design, synthesis, and antitumor evaluation of triazolopyridine derivatives as novel inhibitors for BRD443
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 of43
From garden to lab: C-3 chemical modifications of tomatidine unveil broad-spectrum ATP synthase inhibitors to combat bacterial resistance43
Promises of anionic calix[n]arenes in life science: State of the art in 202343
Development of a next-generation endogenous OCT4 inducer and its anti-aging effect in vivo43
The journey of p38 MAP kinase inhibitors: From bench to bedside in treating inflammatory diseases43
Synthesis and evaluation of small molecule inhibitors of LSD1 for use against MYCN-expressing neuroblastoma43
Design, synthesis, and biological evaluation of diphenyl ether substituted quinazolin-4-amine derivatives as potent EGFRL858R/T790M/C797S inhibitors43
Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models43
Benzimidazole analogues active against adult Schistosoma mansoni: SAR analyses, In vivo efficacy in mice, and preliminary mechanistic studies as potential inhibitors of hemozoin formation43
Synthesis and biological evaluation of tyrosine derivatives as peripheral 5HT2A receptor antagonists for nonalcoholic fatty liver disease43
Discovery, enantioselective synthesis of myrtucommulone E analogues as tyrosyl-DNA phosphodiesterase 2 inhibitors and their biological activities42
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 pathway42
Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo42
Synthesis, design, and optimization of a potent and selective series of pyridylpiperazines as promising antimalarial agents42
Discovery of novel β-carboline derivatives as selective AChE inhibitors with GSK-3β inhibitory property for the treatment of Alzheimer's disease42
Targeted vancomycin delivery via in situ albumin conjugation and acid-triggered drug release for reduced nephrotoxicity41
Structure-directed identification of pyridine-2-methylamine derivatives as MmpL3 inhibitors for use as antitubercular agents41
Rational design and appraisal of selective Cdc2-Like kinase 1 (Clk1) inhibitors as novel autophagy inducers for the treatment of acute liver injury (ALI)41
Novel antimalarial 3-substituted quinolones isosteres with improved pharmacokinetic properties41
Design, synthesis and bioactivity evaluation of novel evodiamine derivatives with excellent potency against gastric cancer41
Novel boron-modified aza-BODIPY photosensitizers for low-dose light-dependent anti-cancer photodynamic therapy41
Editorial Board41
Reversal of subtype-selectivity and function by the introduction of a para-benzamidyl substituent to N-cyclopropylmethyl nornepenthone41
Immunosuppressive effects of new thiophene-based KV1.3 inhibitors41
2-Phenoxy-3, 4′-bipyridine derivatives inhibit AURKB-dependent mitotic processes by disrupting its localization40
Contents continued40
Graphical abstract TOC40
Discovery of novel triazine derivatives as potent retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists40
Inhibitors of ABCG2-mediated multidrug resistance: Lead generation through computer-aided drug design40
Structure-based discovery of potent USP28 inhibitors derived from Vismodegib40
Graphical abstract TOC40
Contents continued40
Anti-cancer efficacy of novel lonidamine derivatives: Design, synthesis, in vitro, in vivo, and computational studies targeting hexokinase-239
Synthesis and biological evaluation of C-28-modified pyrazole-fused betulinic acid derivatives as potent antiosteoporosis agents39
Discovery and optimization of isoliquiritigenin as a death-associated protein kinase 1 inhibitor39
Development of novel S-N3-DABO derivatives as potent non-nucleoside reverse transcriptase inhibitors with improved potency and selectivity39
Design, synthesis, in vitro – In vivo biological evaluation of novel thiazolopyrimidine compounds as antileishmanial agent with PTR1 inhibition39
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 neuroprotection39
Expanding the antiviral arsenal: N-arylated 1,2,4-oxadiazol-5(4H)-ones show high activity against orthopoxviruses39
Design, development and evaluation of a prodrug-type TrkA-selective inhibitor with antinociceptive effects in vivo39
Exploring the potential of histone demethylase inhibition in multi-therapeutic approaches for cancer treatment39
Rational design of next-generation FLT3 inhibitors in acute myeloid leukemia: From laboratory to clinics39
Novel dual-target FAAH and TRPV1 ligands as potential pharmacotherapeutics for pain management38
Bioisosteric replacement of 1H-1,2,3-triazole with 1H-tetrazole ring enhances anti-leukemic activity of (5-benzylthiazol-2-yl)benzamides38
Structure-guided expansion strategy unveils potent allosteric SHP2 inhibitors with synergistic efficacy against AML through MCL-1 co-targeting38
Synthesis and application of small molecules approved for the treatment of lymphoma38
Synthesis and evaluation of chemical linchpins for highly selective CK2α targeting38
Synthesis and evaluation of novel ebselen derivatives as urease inhibitors for combating Helicobacter pylori infections38
Research and development of natural product Salidroside: Pharmacology, total synthesis and structural modifications38
Small molecular inhibitors targeting Janus kinases (JAKs) for the treatment of psoriasis38
Nonsteroidal anti-inflammatory drugs (NSAIDs) and nucleotide analog GS-441524 conjugates with potent in vivo efficacy against coronaviruses38
Assessing the anti-leukemic efficacy of a curcuminoid in cellular and animal models38
Synthesis of 10,10′-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro37
Novel neuroprotective 5,6-dihydropyrido[2′,1':2,3]imidazo[4,5-c]quinoline derivatives acting through cholinesterase inhibition and CB2 signaling modulation37
Fenbendazole–amino acid derivatives as novel anthelmintic candidates: Synthesis, activity against Haemonchus contortus, and in silico profiling37
Targeting p53 activation: Recent therapeutic advances in cancer and diabetic macular edema37
Design and synthesis of novel cyclin-dependent kinase 4/6(CDK4/6) and histone deacetylase (HDAC) dual inhibitors: In vitro and in vivo anticancer activity37
Synthesis of amide-linked panaxadiol-indolinedione derivatives: A novel NSD2/H3K36me2 epigenetic modulator with significant antitumor efficacy37
Mucormycosis: A hidden mystery of fungal infection, possible diagnosis, treatment and development of new therapeutic agents37
Covalent fragment mapping of KRasG12C revealed novel chemotypes with in vivo potency37
Multicomponent syntheses enable the discovery of novel quisinostat-derived chemotypes as histone deacetylase inhibitors37
Discovery of novel diaryl substituted isoquinolin-1(2H)-one derivatives as hypoxia-inducible factor-1 signaling inhibitors for the treatment of rheumatoid arthritis37
Progress of NIR-II fluorescence imaging technology applied to disease diagnosis and treatment37
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 n37
Discovery of a novel dual-target inhibitor of CDK12 and PARP1 that induces synthetic lethality for treatment of triple-negative breast cancer37
Synthetic α-glucosidase inhibitory peptides designed by molecular docking: In vitro screening and anti-hyperglycemic efficacy in diabetic mice36
Tandem construction of biological relevant aliphatic 5-membered N-heterocycles36
Development of fibroblast activation protein-α radiopharmaceuticals: Recent advances and perspectives36
The novel SIRT2-targeted PROTAC degraders as the efficient agents for the treatment of ovarian cancer36
Recent advances in triazoles as tyrosinase inhibitors36
New broad-spectrum and potent antibacterial agents with dual-targeting mechanism: Promoting FtsZ polymerization and disrupting bacterial membranes36
O-derivatization of natural tropolone and β-thujaplicin leading to effective inhibitors of human carbonic anhydrases IX and XII36
Accelerated de novo design of xanthine oxidase-inhibitory peptides via physics-informed computational approaches36
Antimicrobial activity of natural and semi-synthetic carbazole alkaloids36
Recent developments in antimalarial activities of 4-aminoquinoline derivatives35
SAR and lead optimization of (Z)-5-(4-hydroxy-3-methoxybenzylidene)-3-(2-morpholinoacetyl)thiazolidine-2,4-dione as a potential multi-target antidiabetic agent35
Antibody-drug conjugates for targeted cancer therapy: Recent advances in potential payloads35
Design, synthesis and anticancer evaluation of novel Se-NSAID hybrid molecules: Identification of a Se-indomethacin analog as a potential therapeutic for breast cancer35
Discovery of 4-(N-dithiobenzyl piperazine)-1,8-naphthalimide as a potent multi-target antitumor agent with good efficacy, limited toxicity, and low resistance35
3-Hydroxy-pyridin-4(1H)-ones as siderophores mediated delivery of isobavachalcone enhances antibacterial activity against pathogenic Pseudomonas aeruginosa35
Monofunctional dimetallic Ru(η6-arene) complexes inhibit NOTCH1 signaling pathway and synergistically enhance anticancer effect in combination with cisplatin or vitamin C35
A deep learning model for structure-based bioactivity optimization and its application in the bioactivity optimization of a SARS-CoV-2 main protease inhibitor34
Contents continued34
Graphical abstract TOC34
Recent progress toward developing axial chirality bioactive compounds34
Hydrazinecarboxamides: Comprehensive review of their anticancer, anticonvulsive, anti-inflammatory, enzyme inhibition, antioxidant and other activities34
An overview on Estrogen receptors signaling and its ligands in breast cancer34
Structure-based discovery of potent myosin inhibitors to guide antiparasite drug development34
Graphical abstract TOC34
Mitochondrial targeted hierarchical drug delivery system based on HA-modified liposomes for cancer therapy34
Design and synthesis of harmiquins, harmine and chloroquine hybrids as potent antiplasmodial agents34
Synthesis and evaluation of N-sulfonylpiperidine-3-carboxamide derivatives as capsid assembly modulators inhibiting HBV in vitro and in HBV-transgenic mice34
2-Substituted quinazolines: Partial agonistic and antagonistic ligands of the constitutive androstane receptor (CAR)34
An oleanic acid decorated gold nanorod for highly efficient inhibition of hemagglutinin and visible rapid detection of the influenza virus34
Discovery of novel hybrids containing clioquinol−1-benzyl-1,2,3,6-tetrahydropyridine as multi-target-directed ligands (MTDLs) against Alzheimer's disease34
Amphiphilic small molecule antimicrobials: From cationic antimicrobial peptides (CAMPs) to mechanism-related, structurally-diverse antimicrobials34
Graphical abstract TOC33
Discovery of novel polyheterocyclic neuraminidase inhibitors with 1,3,4-oxadiazole thioetheramide as core backbone33
Editorial Board33
SILAC-based chemoproteomics reveals a neoligan analogue as an anti-inflammatory agent targeting IRGM to ameliorate cytokine storm33
Editorial Board33
Chiral pool synthesis of enantiomerically pure morphan derivatives with κ receptor affinity from (S)-perillaldehyde33
Discovery of a tricyclic farnesoid X receptor agonist HEC96719, a clinical candidate for treatment of non-alcoholic steatohepatitis33
Discovery and validation of LAGi-DEL: A nanomolar LAG-3 inhibitor that reverses immune suppression in tumor-immune co-culture models33
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 i33
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) 11533
Design, synthesis, and evaluation of novel matrine derivatives as topoisomerase I inhibitors for anticancer agents33
Recent advances in the development of inhibitors targeting KRAS-G12C and its related pathways33
Defining the structure-activity relationship for a novel class of allosteric MKP5 inhibitors33
Unveiling ortho-phenolic Mannich ciprofloxacin-chalcone conjugates with potential antineoplastic activity: synthesis, mechanistic study, in silico docking and molecular dynamic simulation33
Plant-derived strategies to fight against severe acute respiratory syndrome coronavirus 233
Design, synthesis and biological evaluation of biaryl amide derivatives against SARS-CoV-2 with dual-target mechanism33
Graphical abstract TOC32
Design, synthesis, and biological evaluation of N-(3-cyano-1H-indol-5/6-yl)-6-oxo-1,6-dihydropyrimidine-4-carboxamides and 5-(6-oxo-1,6-dihydropyrimidin-2-yl)-1H-indole-3-carbonitriles as novel xanthi32
Optimization of an Hsp90β-selective inhibitor via exploration of the Hsp90 N-terminal ATP-binding pocket32
Synthesis and structure-activity relationships of novel 14-membered 2-fluoro ketolides with structural modification at the C11 position32
Synthesis, molecular modeling, biological and pharmacokinetic evaluation of hydroxy pyrimidinones and pyrimidinediones as novel LDHA inhibitors32
Bicyclic 2-aminopyrimidine derivatives as potent VEGFR-2 inhibitors and apoptosis Inducers: Structure-Guided design, synthesis, anticancer assessment, and in-silico exploration32
Hit-to-lead optimization of 4,5-dihydrofuran-3-sulfonyl scaffold against Leishmania amazonensis. Effect of an aliphatic moiety32
Graphical abstract TOC32
Positive allosteric modulators of purinergic P2X4 receptors: design, synthesis and therapeutic potential of “click” ligands for multiple sclerosis32
Synthesis and biological evaluation of novel hybrids of phenylsulfonyl furoxan and phenstatin derivatives as potent anti-tumor agents31
Novel thieno[2,3-b]pyridine derivatives protect islet through DRAK2 kinase inhibition31
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