European Journal of Medicinal Chemistry

Papers
(The TQCC of European Journal of Medicinal Chemistry is 13. 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 2021-12-01 to 2025-12-01.)
ArticleCitations
Contents continued235
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 arthritis195
Graphical abstract TOC194
Graphical abstract TOC172
Exploration of 2-phenylquinoline-4-carboxamide linked benzene sulfonamide derivatives as isoform selective inhibitors of transmembrane human carbonic anhydrases169
Nature-inspired new isoindole-based Passerini adducts as efficient tumor-selective apoptotic inducers via caspase-3/7 activation161
Synthesis and evaluation of (E)-4-hydroxy-3-methyl-but-2-enyl diphosphate analogs as competitive partial agonists of butyrophilin 3A1159
Novel 1,3,4-oxadiazole chalcogen analogues: Synthesis and cytotoxic activity157
Graphical abstract contents continued156
Synthesis of tropane-based σ1 receptor antagonists with antiallodynic activity128
Identification of novel tetrahydroquinoxaline derived phenyl ureas as modulators of the hepatitis B virus nucleocapsid assembly126
Design and synthesis of forsythin derivatives as anti-inflammatory agents for acute lung injury117
Editorial Board116
A pro-death autophagy-based nanoplatform for enhancing antitumour efficacy with improved immune responses108
Discovery of N-(5-amido-2-methylphenyl)-5-methylisoxazole-3-carboxamide as dual CSF-1R/c-Kit Inhibitors with improved stability and BBB permeability106
Synthesis and biological evaluation of novel pyrazole amides as potent mitochondrial complex I inhibitors102
Rational drug design to explore the structure-activity relationship (SAR) of TRK inhibitors with 2,4-diaminopyrimidine scaffold101
Corrigendum to “Structure-based development of N-Arylindole derivatives as Pks13 inhibitors against Mycobacterium tuberculosis” [Europ. J. Med. Chem. 283 (2025) 117148]100
Recent developments in the synthesis of indolizines and their derivatives as compounds of interest in medicinal chemistry: a review100
Exploration of P1 and P4 modifications of nirmatrelvir: Design, synthesis, biological evaluation, and X-ray structural studies of SARS-CoV-2 Mpro inhibitors98
Straightforward access to novel mitochondriotropics derived from 2-arylethanol as potent and selective antiproliferative agents95
Novel nitrogen mustard-artemisinin hybrids with potent anti-leukemia action through DNA damage and activation of GPx94
Rational design, synthesis and biological evaluation of dual PARP-1/2 and TNKS1/2 inhibitors for cancer therapy91
Highly potent dipeptidyl peptidase 8/9 (DPP8/9) inhibitors designed via relative binding free energy calculations89
A brain-targeting dl-3-n-butylphthalide prodrug to treat ischemic stroke89
Design, synthesis, evaluation and X-ray structural studies of potent HIV-1 protease inhibitors containing substituted oxaspirocyclic carbamates as the P2 ligands86
Fluorinated sulfonamide-flavonoid derivatives as novel Keap1-Nrf2 inhibitors: Potent induction of cytoprotective gene HO-1 in vivo85
Poly(ADP-ribose) polymerase-1 (PARP1)-based dual inhibitors targeting cancer synthetic lethality (2022-present): advances and perspectives85
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. 84
Structure-based approaches for the design of 6-aryl-1-(3,4,5-trimethoxyphenyl)-1H-benzo[d][1,2,3]triazoles as tubulin polymerization inhibitors83
Peptide inhibitors targeting Ras and Ras-associated protein–protein interactions83
Antitumor activity and transcriptome sequencing (RNA-seq) analyses of hepatocellular carcinoma cells in response to exposure triterpene-nucleoside conjugates82
Non-nucleoside structured compounds with antiviral activity—past 10 years (2010–2020)81
Discovery and optimization of 4-pyrazolyl-2-aminopyrimidine derivatives as potent spleen tyrosine kinase (SYK) inhibitors81
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 ligands80
Platinum(IV) complexes as inhibitors of CD47-SIRPα axis for chemoimmunotherapy of cancer78
Discovery of novel Thieno[2,3-d]imidazole derivatives as agonists of human STING for antitumor immunotherapy using systemic administration77
Novel β-carboline derivatives show promise as dual-target inhibitors of DNA and TOP2A for the treatment of triple negative breast cancer76
Engineering a biomimicking strategy for discovering nonivamide-based quorum-sensing inhibitors for controlling bacterial infection76
Design, synthesis and bioevaluation of PI3Kα-selective inhibitors as potential colorectal cancer drugs75
Synthesis and antibacterial medicinal evaluation of carbothioamido hydrazonyl thiazolylquinolone with multitargeting antimicrobial potential to combat increasingly global resistance73
Design, synthesis and in vitro evaluation of novel SARS-CoV-2 3CLpro covalent inhibitors73
Discovery of a potent, selective and cell active inhibitor of m6A demethylase ALKBH572
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 model72
Anthraquinone derivatives as ADP-competitive inhibitors of liver pyruvate kinase70
Design and syntheses of a bimolecular STING agonist based on the covalent STING antagonist70
Discovery of small molecules for autophagy-lysosome degradation of immune checkpoint proteins70
Synthesis and biological evaluation of α-D-tocopherol derivatives as anticancer agents targeting mitochondrial metabolism70
Novel pterostilbene derivatives ameliorate heart failure by reducing oxidative stress and inflammation through regulating Nrf2/NF-κB signaling pathway70
Synthesis of diarylpentane derivatives as novel α-glucosidase inhibitors: Their inhibitory mechanism and hypoglycemic effects69
Design, synthesis and biological evaluation of N-benzylaryl cinnamide derivatives as tubulin polymerization inhibitors capable of promoting YAP degradation with potent anti-gastric cancer activities67
6-Regioisomeric 5,8-quinolinediones as potent CDC25 inhibitors against colorectal cancers66
Discovery of novel fluorine-containing parthenolide analogues as potential antitumor agents66
Exploring the modulatory influence on the antimalarial activity of amodiaquine using scaffold hybridisation with ferrocene integration65
Design, synthesis, and biological evaluation of piperazine derivatives as pan-PPARs agonists for the treatment of liver fibrosis65
Estrogen receptor β-targeted hypoxia-responsive near-infrared fluorescence probes for prostate cancer study64
Synthesis and evaluation of 3,4,5-trisubstituted triazoles as G protein-biased kappa opioid receptor agonists63
Exploring Si-phthalocyanines with different valency for PSMA-targeted photodynamic therapy: Synthesis and preclinical validation63
Synthesis of 8-aminomorphans with high KOR affinity63
Coumarin–benzimidazole hybrids: A review of developments in medicinal chemistry62
[18F]R91150: Improved radiosynthesis and in vivo evaluation as imaging probe for 5-HT2A receptors62
Discovery of 3H-pyrrolo[2,3-c]quinolines with activity against Mycobacterium tuberculosis by allosteric inhibition of the glutamate-5-kinase enzyme61
Design, synthesis and promising anti-tumor efficacy of novel imidazo[1,2-a]pyridine derivatives as potent autotaxin allosteric inhibitors60
A decade of USFDA-approved small molecules as anti-inflammatory agents: Recent trends and Commentaries on the “industrial” perspective59
Synthesis and evaluation of a novel class of spiro[chromene-2,2′-indoline] derivatives as potent inhibitors of peptidylarginine deiminase IV to treat rheumatoid arthritis59
Discovery of the novel Benzo[b]thiophene 1,1-dioxide derivatives as a potent STAT3 inhibitor against idiopathic pulmonary fibrosis59
A glycyrrhetinic acid-iridium(III) conjugate as a theranostic NIR probe for hepatocellular carcinoma with mitochondrial-targeting ability59
The mechanism of UNC-51-like kinase 1 and the applications of small molecule modulators in cancer treatment59
Structure-based discovery of a 4,5-Dihydropyrazole-cored PET ligand for imaging of receptor-interacting serine/threonine-protein kinase 1 (RIPK1) in the brain58
1,3-Thiazole nucleus as promising molecular platform against antimicrobial resistance: a recent overview in drug discovery58
Discovery of novel dual tubulin and MMPs inhibitors for the treatment of lung cancer and overcoming drug resistance57
Design and synthesis of benzothiazole aryl urea derivatives as potent anti-staphylococcal agents targeting autolysin-mediated peptidoglycan hydrolases57
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 therapy57
Identification of novel diarylpyrimidine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against wild-type and K103N mutant viruses56
Histone deacetylases (HDACs) as the promising immunotherapeutic targets for hematologic cancer treatment56
Insight on pyrimido[5,4-g]indolizine and pyrimido[4,5-c]pyrrolo[1,2-a]azepine systems as promising photosensitizers on malignant cells56
Arginine and tryptophan-rich dendritic antimicrobial peptides that disrupt membranes for bacterial infection in vivo56
Identification of “dual-site”-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase56
Discovery of novel fused-heterocycle-bearing diarypyrimidine derivatives as HIV-1 potent NNRTIs targeting tolerant region I for enhanced antiviral activity and resistance profile56
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 cytotoxicity56
Cinnamic acid derivatives linked to arylpiperazines as novel potent inhibitors of tyrosinase activity and melanin synthesis55
EGCG-like non-competitive inhibitor of DYRK1A rescues cognitive defect in a down syndrome model55
Monoamine oxidase inhibitors: A concise review with special emphasis on structure activity relationship studies55
Discovery, structural optimization, and anti-tumor bioactivity evaluations of betulinic acid derivatives as a new type of RORγ antagonists55
Synthesis of cinnamoyl tethered indoline derivatives with anti-inflammatory and antioxidant activities54
Synthesis, anti-allergic rhinitis evaluation and mechanism investigation of novel 1,2,4-triazole-enamides as CB1 R antagonist54
Novel 6-hydroxybenzothiazol-2-carboxamides as potent and selective monoamine oxidase B inhibitors endowed with neuroprotective activity54
Ligand-based design and synthesis of new trityl histamine and trityl cysteamine derivatives as SIRT2 inhibitors for cancer therapy53
Discovery of ML210-Based glutathione peroxidase 4 (GPX4) degrader inducing ferroptosis of human cancer cells53
Small-molecule MDM2 inhibitors in clinical trials for cancer therapy53
The first ADC bearing the ferroptosis inducer RSL3 as a payload with conservation of the fragile electrophilic warhead53
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 inhibitor52
From tryptophan-based amides to tertiary amines: Optimization of a butyrylcholinesterase inhibitor series52
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 51
Novel bifluorescent Zn(II)–cryptolepine–cyclen complexes trigger apoptosis induced by nuclear and mitochondrial DNA damage in cisplatin-resistant lung tumor cells51
Multitarget-directed carbamate and carbamothioate derivatives: Cholinesterase and monoamine oxidase inhibition, anti-β-amyloid (Aβ) aggregation, antioxidant and blood–brain barrier permeation properti51
Bestatin analogs-4-quinolinone hybrids as antileishmanial hits: Design, repurposing rational, synthesis, in vitro and in silico studies51
New β-arylchalcogeno amines with procognitive properties targeting Carbonic Anhydrases and Monoamine Oxidases50
Application of deuterium in research and development of drugs50
An update on small molecule compounds targeting synthetic lethality for cancer therapy50
Inhibition of Histone Deacetylase 6 (HDAC6) as a therapeutic strategy for Alzheimer's disease: A review (2010–2020)50
Applications of oxetanes in drug discovery and medicinal chemistry49
Oleanolic acid derivatives against drug-resistant bacteria and fungi by multi-targets to avoid drug resistance49
Pyrazolopyrimidines as anticancer agents: A review on structural and target-based approaches49
Rational molecular design converting fascaplysin derivatives to potent broad-spectrum inhibitors against bacterial pathogens via targeting FtsZ49
Amino acid–modified chalcone derivatives with in vitro and in vivo efficacy against colon cancer49
Antioxidant, anti-inflammatory and immunomodulatory roles of vitamins in COVID-19 therapy49
Graphical abstract TOC48
Corrigendum to “Discovery of novel tetrahydroquinoline derivatives as potent, selective, and orally Available AR antagonists” [Eur. J. Med. Chem. 291 (2025) 117566]48
Discovery and biological evaluation of 6-aryl-4-(3,4,5-trimethoxyphenyl)quinoline derivatives with promising antitumor activities as novel colchicine-binding site inhibitors48
Structure-activity relationship studies and design of a PTPN22 inhibitor with enhanced isozyme selectivity and cellular efficacy48
Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis48
Synthesis, design, and optimization of a potent and selective series of pyridylpiperazines as promising antimalarial agents47
Novel angiogenesis inhibitors with superoxide anion radical amplification effect: Surmounting the Achilles’ heels of angiogenesis inhibitors and photosensitizers47
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 pathway47
Editorial Board47
Discovery, enantioselective synthesis of myrtucommulone E analogues as tyrosyl-DNA phosphodiesterase 2 inhibitors and their biological activities47
Bioisosteric replacement of 1H-1,2,3-triazole with 1H-tetrazole ring enhances anti-leukemic activity of (5-benzylthiazol-2-yl)benzamides46
Novel antimalarial 3-substituted quinolones isosteres with improved pharmacokinetic properties46
Discovery of novel diaryl substituted isoquinolin-1(2H)-one derivatives as hypoxia-inducible factor-1 signaling inhibitors for the treatment of rheumatoid arthritis46
Nonsteroidal anti-inflammatory drugs (NSAIDs) and nucleotide analog GS-441524 conjugates with potent in vivo efficacy against coronaviruses46
Benzimidazole analogues active against adult Schistosoma mansoni: SAR analyses, In vivo efficacy in mice, and preliminary mechanistic studies as potential inhibitors of hemozoin formation46
Contents continued45
Exploring the potential of histone demethylase inhibition in multi-therapeutic approaches for cancer treatment45
Structure-based discovery of potent USP28 inhibitors derived from Vismodegib45
Inhibitors of ABCG2-mediated multidrug resistance: Lead generation through computer-aided drug design45
Macrocyclic-based strategy in drug design: From lab to the clinic45
Discovery of novel triazine derivatives as potent retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists45
Contents continued45
2-Phenoxy-3, 4′-bipyridine derivatives inhibit AURKB-dependent mitotic processes by disrupting its localization44
Design, development and evaluation of a prodrug-type TrkA-selective inhibitor with antinociceptive effects in vivo44
Graphical abstract TOC44
Rational design and appraisal of selective Cdc2-Like kinase 1 (Clk1) inhibitors as novel autophagy inducers for the treatment of acute liver injury (ALI)43
Immunosuppressive effects of new thiophene-based KV1.3 inhibitors43
Graphical abstract TOC43
Design, synthesis, in vitro – In vivo biological evaluation of novel thiazolopyrimidine compounds as antileishmanial agent with PTR1 inhibition43
Targeted vancomycin delivery via in situ albumin conjugation and acid-triggered drug release for reduced nephrotoxicity42
Structure-directed identification of pyridine-2-methylamine derivatives as MmpL3 inhibitors for use as antitubercular agents42
Synthesis and evaluation of small molecule inhibitors of LSD1 for use against MYCN-expressing neuroblastoma42
Design, synthesis and bioactivity evaluation of novel evodiamine derivatives with excellent potency against gastric cancer42
Novel boron-modified aza-BODIPY photosensitizers for low-dose light-dependent anti-cancer photodynamic therapy42
Synthesis and evaluation of novel ebselen derivatives as urease inhibitors for combating Helicobacter pylori infections42
Reversal of subtype-selectivity and function by the introduction of a para-benzamidyl substituent to N-cyclopropylmethyl nornepenthone42
Development of novel S-N3-DABO derivatives as potent non-nucleoside reverse transcriptase inhibitors with improved potency and selectivity42
Discovery of a novel dual-target inhibitor of CDK12 and PARP1 that induces synthetic lethality for treatment of triple-negative breast cancer41
Research and development of natural product Salidroside: Pharmacology, total synthesis and structural modifications41
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 neuroprotection41
Assessing the anti-leukemic efficacy of a curcuminoid in cellular and animal models41
Structure-guided expansion strategy unveils potent allosteric SHP2 inhibitors with synergistic efficacy against AML through MCL-1 co-targeting41
Expanding the antiviral arsenal: N-arylated 1,2,4-oxadiazol-5(4H)-ones show high activity against orthopoxviruses41
Synthesis and biological evaluation of C-28-modified pyrazole-fused betulinic acid derivatives as potent antiosteoporosis agents41
Synthesis and application of small molecules approved for the treatment of lymphoma41
Tandem construction of biological relevant aliphatic 5-membered N-heterocycles41
Design, synthesis and anticancer evaluation of novel Se-NSAID hybrid molecules: Identification of a Se-indomethacin analog as a potential therapeutic for breast cancer40
Novel dual-target FAAH and TRPV1 ligands as potential pharmacotherapeutics for pain management40
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 n40
Anti-cancer efficacy of novel lonidamine derivatives: Design, synthesis, in vitro, in vivo, and computational studies targeting hexokinase-240
Covalent fragment mapping of KRasG12C revealed novel chemotypes with in vivo potency40
Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo40
Development of a next-generation endogenous OCT4 inducer and its anti-aging effect in vivo40
Synthesis and evaluation of chemical linchpins for highly selective CK2α targeting39
Mucormycosis: A hidden mystery of fungal infection, possible diagnosis, treatment and development of new therapeutic agents39
Recent progress toward developing axial chirality bioactive compounds39
Multicomponent syntheses enable the discovery of novel quisinostat-derived chemotypes as histone deacetylase inhibitors39
Recent advances on the development of NO-releasing molecules (NORMs) for biomedical applications39
Progress of NIR-II fluorescence imaging technology applied to disease diagnosis and treatment39
Antimicrobial activity of natural and semi-synthetic carbazole alkaloids39
Discovery and optimization of isoliquiritigenin as a death-associated protein kinase 1 inhibitor39
O-derivatization of natural tropolone and β-thujaplicin leading to effective inhibitors of human carbonic anhydrases IX and XII38
Design, synthesis and evaluation of novel oxadiazole-based compounds as potential Rac1 inhibitors against breast cancer38
Small molecular inhibitors targeting Janus kinases (JAKs) for the treatment of psoriasis38
Design, synthesis, and biological evaluation of diphenyl ether substituted quinazolin-4-amine derivatives as potent EGFRL858R/T790M/C797S inhibitors38
Aporphines: A privileged scaffold in CNS drug discovery38
SAR and lead optimization of (Z)-5-(4-hydroxy-3-methoxybenzylidene)-3-(2-morpholinoacetyl)thiazolidine-2,4-dione as a potential multi-target antidiabetic agent38
3-Hydroxy-pyridin-4(1H)-ones as siderophores mediated delivery of isobavachalcone enhances antibacterial activity against pathogenic Pseudomonas aeruginosa38
Development of fibroblast activation protein-α radiopharmaceuticals: Recent advances and perspectives38
Synthesis of 10,10′-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro38
Design and synthesis of harmiquins, harmine and chloroquine hybrids as potent antiplasmodial agents38
An overview on Estrogen receptors signaling and its ligands in breast cancer38
Briarane-type diterpenoids, the inhibitors of osteoclast formation by interrupting Keap1-Nrf2 interaction and activating Nrf2 pathway38
Design, synthesis and biological evaluation of new parbendazole derivatives for the treatment of HNSCC38
Hydrazinecarboxamides: Comprehensive review of their anticancer, anticonvulsive, anti-inflammatory, enzyme inhibition, antioxidant and other activities38
Promises of anionic calix[n]arenes in life science: State of the art in 202338
Recent advances in triazoles as tyrosinase inhibitors38
Novel neuroprotective 5,6-dihydropyrido[2′,1':2,3]imidazo[4,5-c]quinoline derivatives acting through cholinesterase inhibition and CB2 signaling modulation37
Recent developments in antimalarial activities of 4-aminoquinoline derivatives37
Mitochondrial targeted hierarchical drug delivery system based on HA-modified liposomes for cancer therapy37
Microbial-derived peptides with anti-mycobacterial potential37
A deep learning model for structure-based bioactivity optimization and its application in the bioactivity optimization of a SARS-CoV-2 main protease inhibitor37
The roles of fused-cyclopropanes in medicinal chemistry: Insights from the past decade37
Synthesis and biological evaluation of tyrosine derivatives as peripheral 5HT2A receptor antagonists for nonalcoholic fatty liver disease37
Discovery of novel hybrids containing clioquinol−1-benzyl-1,2,3,6-tetrahydropyridine as multi-target-directed ligands (MTDLs) against Alzheimer's disease37
Design and synthesis of new 1,2,3-triazoles derived from eugenol and analogues with in vitro and in vivo activity against Trypanosoma cruzi37
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 of37
Targeting p53 activation: Recent therapeutic advances in cancer and diabetic macular edema37
Discovery of 4-(N-dithiobenzyl piperazine)-1,8-naphthalimide as a potent multi-target antitumor agent with good efficacy, limited toxicity, and low resistance37
Antibody-drug conjugates for targeted cancer therapy: Recent advances in potential payloads37
Amphiphilic small molecule antimicrobials: From cationic antimicrobial peptides (CAMPs) to mechanism-related, structurally-diverse antimicrobials37
Structure-based development of potent Plasmodium falciparum M1 and M17 aminopeptidase selective and dual inhibitors via S1′-region optimisation37
Targeting transthyretin in Alzheimer's disease: Drug discovery of small-molecule chaperones as disease-modifying drug candidates for Alzheimer's disease36
From garden to lab: C-3 chemical modifications of tomatidine unveil broad-spectrum ATP synthase inhibitors to combat bacterial resistance36
New broad-spectrum and potent antibacterial agents with dual-targeting mechanism: Promoting FtsZ polymerization and disrupting bacterial membranes36
Discovery of novel β-carboline derivatives as selective AChE inhibitors with GSK-3β inhibitory property for the treatment of Alzheimer's disease36
Monofunctional dimetallic Ru(η6-arene) complexes inhibit NOTCH1 signaling pathway and synergistically enhance anticancer effect in combination with cisplatin or vitamin C36
Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models36
Design, synthesis, and biological activity evaluation of novel HDAC3 selective inhibitors for combination with Venetoclax against acute myeloid leukemia36
Design, synthesis, and antitumor evaluation of triazolopyridine derivatives as novel inhibitors for BRD436
The journey of p38 MAP kinase inhibitors: From bench to bedside in treating inflammatory diseases36
Advancing Src kinase inhibition: From structural design to therapeutic innovation - A comprehensive review36
Synthesis and evaluation of N-sulfonylpiperidine-3-carboxamide derivatives as capsid assembly modulators inhibiting HBV in vitro and in HBV-transgenic mice35
Contents continued35
SILAC-based chemoproteomics reveals a neoligan analogue as an anti-inflammatory agent targeting IRGM to ameliorate cytokine storm35
An oleanic acid decorated gold nanorod for highly efficient inhibition of hemagglutinin and visible rapid detection of the influenza virus35
Mechanistic analysis of diverse click reactions along with their applications35
Plant-derived strategies to fight against severe acute respiratory syndrome coronavirus 235
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 i35
How many organic small molecules might be used to treat COVID-19? From natural products to synthetic agents35
Prominent supramolecular systems for cancer Therapy: From structural design to tailored applications35
Design, synthesis and biological evaluation of biaryl amide derivatives against SARS-CoV-2 with dual-target mechanism35
Graphical abstract TOC34
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) 11534
Graphical abstract TOC34
Recent advances in the development of inhibitors targeting KRAS-G12C and its related pathways34
Structure-based discovery of potent myosin inhibitors to guide antiparasite drug development34
Insight into small-molecule inhibitors targeting extracellular nucleotide pyrophosphatase/phosphodiesterase1 for potential multiple human diseases34
Discovery of a tricyclic farnesoid X receptor agonist HEC96719, a clinical candidate for treatment of non-alcoholic steatohepatitis34
2-Substituted quinazolines: Partial agonistic and antagonistic ligands of the constitutive androstane receptor (CAR)34
Graphical abstract TOC34
Discovery of a potential anti-ischemic stroke agent by suppressing ferroptosis through the ATF3/SLC7A11/GPX4 pathway33
Design, synthesis and biological evaluation of N-substituted nipecotamide derivatives as multifunctional agents for epilepsy treatment33
Discovery of SA-8 as a potent SHP2-AUTAC degrader in cancer therapy33
New N-aryl-N′-aryl-/(thio)ureido-/sulfamoylamino-derivatives of alkyl/alkylcarbamoyl piperazines: Effect of structural modifications on selectivity over 5-HT1A receptor33
Synthesis and structure-activity relationships of novel 14-membered 2-fluoro ketolides with structural modification at the C11 position33
Graphical abstract TOC33
Acyclic purine and pyrimidine nucleotide analogs as ecto-5′-nucleotidase (CD73) inhibitors33
Targeting RIPK1-mediated necroptosis, oxidative stress, and ferroptosis: A novel multitarget therapy for ischemic stroke33
Cathepsin C inhibitors as anti-inflammatory drug discovery: Challenges and opportunities33
Novel dihydropyrimidines as promising EGFR & HER2 inhibitors: Insights from experimental and computational studies33
Synthesis, structure-activity relationship and antiviral activity of indole-containing inhibitors of Flavivirus NS2B-NS3 protease33
Hit-to-lead optimization of 4,5-dihydrofuran-3-sulfonyl scaffold against Leishmania amazonensis. Effect of an aliphatic moiety33
Synthesis, molecular modeling, biological and pharmacokinetic evaluation of hydroxy pyrimidinones and pyrimidinediones as novel LDHA inhibitors33
2-(Phenylamino)-7,8-dihydroquinazolin-5(6H)-one, a promising scaffold for MAO-B inhibitors with potential GSK3β targeting33
Expanding the utilization of binding pockets proves to be effective for noncovalent small molecule inhibitors against SARS-CoV-2 Mpro33
A novel Al18F-labelled NOTA-modified ubiquicidin 29-41 derivative as a bacterial infection PET imaging agent33
AR-A014418-based dual Glycogen Synthase Kinase 3β/Histone Deacetylase inhibitors as potential therapeutics for Alzheimer's disease33
Editorial Board33
Graphical abstract TOC33
Design, synthesis and activity evaluation of benzene sulfonamide derivatives as novel androgen receptor antagonist33
Editorial Board33
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