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 2022-05-01 to 2026-05-01.)
ArticleCitations
Contents continued269
Graphical abstract TOC229
Graphical abstract TOC188
A brain-targeting dl-3-n-butylphthalide prodrug to treat ischemic stroke183
Structure-based approaches for the design of 6-aryl-1-(3,4,5-trimethoxyphenyl)-1H-benzo[d][1,2,3]triazoles as tubulin polymerization inhibitors167
[18F]R91150: Improved radiosynthesis and in vivo evaluation as imaging probe for 5-HT2A receptors153
Synthesis of cinnamoyl tethered indoline derivatives with anti-inflammatory and antioxidant activities141
Design, synthesis and biological evaluation of N-benzylaryl cinnamide derivatives as tubulin polymerization inhibitors capable of promoting YAP degradation with potent anti-gastric cancer activities116
Corrigendum to “Structure-based development of N-Arylindole derivatives as Pks13 inhibitors against Mycobacterium tuberculosis” [Europ. J. Med. Chem. 283 (2025) 117148]112
Estrogen receptor β-targeted hypoxia-responsive near-infrared fluorescence probes for prostate cancer study109
Novel pterostilbene derivatives ameliorate heart failure by reducing oxidative stress and inflammation through regulating Nrf2/NF-κB signaling pathway108
Exploring Si-phthalocyanines with different valency for PSMA-targeted photodynamic therapy: Synthesis and preclinical validation107
Synthesis and evaluation of (E)-4-hydroxy-3-methyl-but-2-enyl diphosphate analogs as competitive partial agonists of butyrophilin 3A1104
Identification of novel tetrahydroquinoxaline derived phenyl ureas as modulators of the hepatitis B virus nucleocapsid assembly104
Editorial Board102
Discovery of novel fluorine-containing parthenolide analogues as potential antitumor agents102
Discovery of novel fused-heterocycle-bearing diarypyrimidine derivatives as HIV-1 potent NNRTIs targeting tolerant region I for enhanced antiviral activity and resistance profile97
Fluorinated sulfonamide-flavonoid derivatives as novel Keap1-Nrf2 inhibitors: Potent induction of cytoprotective gene HO-1 in vivo91
Structure-based discovery of a 4,5-Dihydropyrazole-cored PET ligand for imaging of receptor-interacting serine/threonine-protein kinase 1 (RIPK1) in the brain91
Inhibitors of membrane associated serine proteases block replication of coronavirus SARS-CoV-2 and influenza virus H1N189
Discovery of p300 histone acetyltransferase inhibitors bearing an imidazo[4,5-b]pyridine-2-one scaffold for the treatment of multiple myeloma89
Design and syntheses of a bimolecular STING agonist based on the covalent STING antagonist88
Water molecules in the cannabinoid receptor 2 binding site crucially impact the discovery of novel ligands87
Rational molecular design converting fascaplysin derivatives to potent broad-spectrum inhibitors against bacterial pathogens via targeting FtsZ87
Identification of “dual-site”-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase87
Design and synthesis of benzothiazole aryl urea derivatives as potent anti-staphylococcal agents targeting autolysin-mediated peptidoglycan hydrolases84
Novel bifluorescent Zn(II)–cryptolepine–cyclen complexes trigger apoptosis induced by nuclear and mitochondrial DNA damage in cisplatin-resistant lung tumor cells83
Design, synthesis, and biological evaluation of piperazine derivatives as pan-PPARs agonists for the treatment of liver fibrosis82
Discovery and optimization of 4-pyrazolyl-2-aminopyrimidine derivatives as potent spleen tyrosine kinase (SYK) inhibitors80
Synthesis, anti-allergic rhinitis evaluation and mechanism investigation of novel 1,2,4-triazole-enamides as CB1 R antagonist80
Antitumor activity and transcriptome sequencing (RNA-seq) analyses of hepatocellular carcinoma cells in response to exposure triterpene-nucleoside conjugates79
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
A pro-death autophagy-based nanoplatform for enhancing antitumour efficacy with improved immune responses79
Design, synthesis and promising anti-tumor efficacy of novel imidazo[1,2-a]pyridine derivatives as potent autotaxin allosteric inhibitors77
Discovery, structural optimization, and anti-tumor bioactivity evaluations of betulinic acid derivatives as a new type of RORγ antagonists75
An update on small molecule compounds targeting synthetic lethality for cancer therapy74
Rational design, synthesis and biological evaluation of dual PARP-1/2 and TNKS1/2 inhibitors for cancer therapy74
Structure-activity relationship of N-cyclopropylmethyl-7α-(m-methylaminophenyl)-6,14-endoethano-northebaine derivatives as G-protein-biased KOR-selective agonists73
Design, synthesis, and biological evaluation of hybrids from both nitrones with eNOS-mimicking activity and selective iNOS inhibitors for the treatment of ischemic stroke73
Discovery of tetrahydrothiazolopyridine-incorporated curcumol derivatives as novel and highly potent anti-cancer agents72
A medicinal chemistry perspective on disruptor of telomeric silencing 1-like: Its mechanisms and modulators in cancer treatment71
Engineering a biomimicking strategy for discovering nonivamide-based quorum-sensing inhibitors for controlling bacterial infection71
6-Regioisomeric 5,8-quinolinediones as potent CDC25 inhibitors against colorectal cancers70
Exploring the modulatory influence on the antimalarial activity of amodiaquine using scaffold hybridisation with ferrocene integration70
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 inhibitor69
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 arthritis68
Novel nitrogen mustard-artemisinin hybrids with potent anti-leukemia action through DNA damage and activation of GPx68
Identification of novel diarylpyrimidine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against wild-type and K103N mutant viruses67
Trimethyl Lock-2Cl (TML-2Cl): A self-cyclizing adapter for molecular release in antibody-drug conjugates66
Oleanolic acid derivatives against drug-resistant bacteria and fungi by multi-targets to avoid drug resistance65
The mechanism of UNC-51-like kinase 1 and the applications of small molecule modulators in cancer treatment65
Design and synthesis of forsythin derivatives as anti-inflammatory agents for acute lung injury65
Nature-inspired new isoindole-based Passerini adducts as efficient tumor-selective apoptotic inducers via caspase-3/7 activation64
Discovery of novel dual tubulin and MMPs inhibitors for the treatment of lung cancer and overcoming drug resistance64
Bestatin analogs-4-quinolinone hybrids as antileishmanial hits: Design, repurposing rational, synthesis, in vitro and in silico studies62
Discovery of novel Thieno[2,3-d]imidazole derivatives as agonists of human STING for antitumor immunotherapy using systemic administration62
Applications of oxetanes in drug discovery and medicinal chemistry62
Novel 1,3,4-oxadiazole chalcogen analogues: Synthesis and cytotoxic activity61
Design, synthesis and bioevaluation of PI3Kα-selective inhibitors as potential colorectal cancer drugs60
Editorial Board60
A decade of USFDA-approved small molecules as anti-inflammatory agents: Recent trends and Commentaries on the “industrial” perspective59
Multitarget-directed carbamate and carbamothioate derivatives: Cholinesterase and monoamine oxidase inhibition, anti-β-amyloid (Aβ) aggregation, antioxidant and blood–brain barrier permeation properti59
Synthesis of diarylpentane derivatives as novel α-glucosidase inhibitors: Their inhibitory mechanism and hypoglycemic effects59
The first ADC bearing the ferroptosis inducer RSL3 as a payload with conservation of the fragile electrophilic warhead58
Histone deacetylases (HDACs) as the promising immunotherapeutic targets for hematologic cancer treatment58
Synthesis and evaluation of 3,4,5-trisubstituted triazoles as G protein-biased kappa opioid receptor agonists57
Synthesis and biological evaluation of α-D-tocopherol derivatives as anticancer agents targeting mitochondrial metabolism56
Novel β-carboline derivatives show promise as dual-target inhibitors of DNA and TOP2A for the treatment of triple negative breast cancer56
Synthesis and biological evaluation of novel pyrazole amides as potent mitochondrial complex I inhibitors56
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
Discovery of the novel Benzo[b]thiophene 1,1-dioxide derivatives as a potent STAT3 inhibitor against idiopathic pulmonary fibrosis55
Peptide inhibitors targeting Ras and Ras-associated protein–protein interactions54
Discovery of anti-tumor targets based on photo-affinity labeling54
Ligand-based design and synthesis of new trityl histamine and trityl cysteamine derivatives as SIRT2 inhibitors for cancer therapy54
Arginine and tryptophan-rich dendritic antimicrobial peptides that disrupt membranes for bacterial infection in vivo54
Discovery of small molecules for autophagy-lysosome degradation of immune checkpoint proteins53
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 therapy53
Small-molecule MDM2 inhibitors in clinical trials for cancer therapy52
Discovery and biological evaluation of 6-aryl-4-(3,4,5-trimethoxyphenyl)quinoline derivatives with promising antitumor activities as novel colchicine-binding site inhibitors52
Functional quinoline-malononitriles for enhanced wound repair and monitoring52
Exploration of P1 and P4 modifications of nirmatrelvir: Design, synthesis, biological evaluation, and X-ray structural studies of SARS-CoV-2 Mpro inhibitors52
Synthesis and evaluation of a novel class of spiro[chromene-2,2′-indoline] derivatives as potent inhibitors of peptidylarginine deiminase IV to treat rheumatoid arthritis52
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 model52
Application of deuterium in research and development of drugs51
Insight on pyrimido[5,4-g]indolizine and pyrimido[4,5-c]pyrrolo[1,2-a]azepine systems as promising photosensitizers on malignant cells51
Discovery of N-(5-amido-2-methylphenyl)-5-methylisoxazole-3-carboxamide as dual CSF-1R/c-Kit Inhibitors with improved stability and BBB permeability51
Amino acid–modified chalcone derivatives with in vitro and in vivo efficacy against colon cancer50
A glycyrrhetinic acid-iridium(III) conjugate as a theranostic NIR probe for hepatocellular carcinoma with mitochondrial-targeting ability50
New β-arylchalcogeno amines with procognitive properties targeting Carbonic Anhydrases and Monoamine Oxidases50
Highly potent dipeptidyl peptidase 8/9 (DPP8/9) inhibitors designed via relative binding free energy calculations50
Recent developments in the synthesis of indolizines and their derivatives as compounds of interest in medicinal chemistry: a review49
Discovery of a potent, selective and cell active inhibitor of m6A demethylase ALKBH549
Design, synthesis, evaluation and X-ray structural studies of potent HIV-1 protease inhibitors containing substituted oxaspirocyclic carbamates as the P2 ligands49
1,3-Thiazole nucleus as promising molecular platform against antimicrobial resistance: a recent overview in drug discovery49
Poly(ADP-ribose) polymerase-1 (PARP1)-based dual inhibitors targeting cancer synthetic lethality (2022-present): advances and perspectives49
Novel 6-hydroxybenzothiazol-2-carboxamides as potent and selective monoamine oxidase B inhibitors endowed with neuroprotective activity48
Discovery of ML210-Based glutathione peroxidase 4 (GPX4) degrader inducing ferroptosis of human cancer cells48
Synthesis and antibacterial medicinal evaluation of carbothioamido hydrazonyl thiazolylquinolone with multitargeting antimicrobial potential to combat increasingly global resistance48
EGCG-like non-competitive inhibitor of DYRK1A rescues cognitive defect in a down syndrome model48
Monoamine oxidase inhibitors: A concise review with special emphasis on structure activity relationship studies48
Graphical abstract TOC47
Synthesis and evaluation of a new class of MIF-inhibitors in activated macrophage cells and in experimental septic shock in mice47
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 47
Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis47
Design, synthesis, in vitro – In vivo biological evaluation of novel thiazolopyrimidine compounds as antileishmanial agent with PTR1 inhibition46
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 neuroprotection46
Novel angiogenesis inhibitors with superoxide anion radical amplification effect: Surmounting the Achilles’ heels of angiogenesis inhibitors and photosensitizers46
Synthesis and biological evaluation of C-28-modified pyrazole-fused betulinic acid derivatives as potent antiosteoporosis agents45
Recent developments in antimalarial activities of 4-aminoquinoline derivatives45
Design, development and evaluation of a prodrug-type TrkA-selective inhibitor with antinociceptive effects in vivo45
Design, synthesis, and biological evaluation of diphenyl ether substituted quinazolin-4-amine derivatives as potent EGFRL858R/T790M/C797S inhibitors45
Design and synthesis of novel cyclin-dependent kinase 4/6(CDK4/6) and histone deacetylase (HDAC) dual inhibitors: In vitro and in vivo anticancer activity45
Antimicrobial activity of natural and semi-synthetic carbazole alkaloids44
Benzimidazole analogues active against adult Schistosoma mansoni: SAR analyses, In vivo efficacy in mice, and preliminary mechanistic studies as potential inhibitors of hemozoin formation44
Novel neuroprotective 5,6-dihydropyrido[2′,1':2,3]imidazo[4,5-c]quinoline derivatives acting through cholinesterase inhibition and CB2 signaling modulation44
From garden to lab: C-3 chemical modifications of tomatidine unveil broad-spectrum ATP synthase inhibitors to combat bacterial resistance44
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 of44
Natural alkaloids with therapeutic potential against Alzheimer's disease through cholinesterase inhibition44
Synthesis and evaluation of small molecule inhibitors of LSD1 for use against MYCN-expressing neuroblastoma44
Fenbendazole–amino acid derivatives as novel anthelmintic candidates: Synthesis, activity against Haemonchus contortus, and in silico profiling44
Amphiphilic small molecule antimicrobials: From cationic antimicrobial peptides (CAMPs) to mechanism-related, structurally-diverse antimicrobials44
Editorial Board44
Covalent fragment mapping of KRasG12C revealed novel chemotypes with in vivo potency43
Ketoconazole-carbonic anhydrase inhibitors as potential anticancer agents43
Inhibitors of ABCG2-mediated multidrug resistance: Lead generation through computer-aided drug design43
Bioisosteric replacement of 1H-1,2,3-triazole with 1H-tetrazole ring enhances anti-leukemic activity of (5-benzylthiazol-2-yl)benzamides43
Promises of anionic calix[n]arenes in life science: State of the art in 202343
Structure-based development of potent Plasmodium falciparum M1 and M17 aminopeptidase selective and dual inhibitors via S1′-region optimisation43
Synthesis and application of small molecules approved for the treatment of lymphoma43
Hydrazinecarboxamides: Comprehensive review of their anticancer, anticonvulsive, anti-inflammatory, enzyme inhibition, antioxidant and other activities43
Design, synthesis and anticancer evaluation of novel Se-NSAID hybrid molecules: Identification of a Se-indomethacin analog as a potential therapeutic for breast cancer43
Nonsteroidal anti-inflammatory drugs (NSAIDs) and nucleotide analog GS-441524 conjugates with potent in vivo efficacy against coronaviruses43
Briarane-type diterpenoids, the inhibitors of osteoclast formation by interrupting Keap1-Nrf2 interaction and activating Nrf2 pathway42
Synthesis and evaluation of novel ebselen derivatives as urease inhibitors for combating Helicobacter pylori infections42
Contents continued42
Immunosuppressive effects of new thiophene-based KV1.3 inhibitors42
Reversal of subtype-selectivity and function by the introduction of a para-benzamidyl substituent to N-cyclopropylmethyl nornepenthone42
N-acylated aminoguanidine-benzenesulfonamides: rational design, synthesis, and dual apoptotic mechanisms of anticancer activity involving VEGFR-2 inhibition and VEGFR-2–independent pathways42
A deep learning model for structure-based bioactivity optimization and its application in the bioactivity optimization of a SARS-CoV-2 main protease inhibitor42
Graphical abstract TOC42
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 pathway41
Monofunctional dimetallic Ru(η6-arene) complexes inhibit NOTCH1 signaling pathway and synergistically enhance anticancer effect in combination with cisplatin or vitamin C41
Structure-activity relationship studies and design of a PTPN22 inhibitor with enhanced isozyme selectivity and cellular efficacy41
Targeted vancomycin delivery via in situ albumin conjugation and acid-triggered drug release for reduced nephrotoxicity41
Discovery of 4-(N-dithiobenzyl piperazine)-1,8-naphthalimide as a potent multi-target antitumor agent with good efficacy, limited toxicity, and low resistance41
Corrigendum to “Discovery of novel tetrahydroquinoline derivatives as potent, selective, and orally Available AR antagonists” [Eur. J. Med. Chem. 291 (2025) 117566]41
Discovery of novel diaryl substituted isoquinolin-1(2H)-one derivatives as hypoxia-inducible factor-1 signaling inhibitors for the treatment of rheumatoid arthritis40
Synthesis and biological evaluation of tyrosine derivatives as peripheral 5HT2A receptor antagonists for nonalcoholic fatty liver disease40
Design, synthesis and biological evaluation of new parbendazole derivatives for the treatment of HNSCC40
Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models40
Mucormycosis: A hidden mystery of fungal infection, possible diagnosis, treatment and development of new therapeutic agents40
Graphical abstract TOC40
Research and development of natural product Salidroside: Pharmacology, total synthesis and structural modifications39
Discovery of novel triazine derivatives as potent retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists39
Discovery, enantioselective synthesis of myrtucommulone E analogues as tyrosyl-DNA phosphodiesterase 2 inhibitors and their biological activities39
The roles of fused-cyclopropanes in medicinal chemistry: Insights from the past decade39
Targeting p53 activation: Recent therapeutic advances in cancer and diabetic macular edema39
Synthesis and evaluation of chemical linchpins for highly selective CK2α targeting39
Small molecular inhibitors targeting Janus kinases (JAKs) for the treatment of psoriasis39
Design and synthesis of new 1,2,3-triazoles derived from eugenol and analogues with in vitro and in vivo activity against Trypanosoma cruzi39
Multicomponent syntheses enable the discovery of novel quisinostat-derived chemotypes as histone deacetylase inhibitors39
Novel boron-modified aza-BODIPY photosensitizers for low-dose light-dependent anti-cancer photodynamic therapy39
Structure-based discovery of potent USP28 inhibitors derived from Vismodegib39
Anti-cancer efficacy of novel lonidamine derivatives: Design, synthesis, in vitro, in vivo, and computational studies targeting hexokinase-239
Antibody-drug conjugates for targeted cancer therapy: Recent advances in potential payloads38
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 n38
Synthesis of 10,10′-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro38
The novel SIRT2-targeted PROTAC degraders as the efficient agents for the treatment of ovarian cancer38
Integration of computational and experimental techniques for the discovery of PLpro covalent inhibitors. When large virtual screening and rational design meet38
3-Hydroxy-pyridin-4(1H)-ones as siderophores mediated delivery of isobavachalcone enhances antibacterial activity against pathogenic Pseudomonas aeruginosa38
An overview on Estrogen receptors signaling and its ligands in breast cancer38
Novel dual-target FAAH and TRPV1 ligands as potential pharmacotherapeutics for pain management37
Progress of NIR-II fluorescence imaging technology applied to disease diagnosis and treatment37
Structure-guided expansion strategy unveils potent allosteric SHP2 inhibitors with synergistic efficacy against AML through MCL-1 co-targeting37
Aporphines: A privileged scaffold in CNS drug discovery37
Development of novel S-N3-DABO derivatives as potent non-nucleoside reverse transcriptase inhibitors with improved potency and selectivity37
Design and synthesis of harmiquins, harmine and chloroquine hybrids as potent antiplasmodial agents37
Assessing the anti-leukemic efficacy of a curcuminoid in cellular and animal models37
Recent progress toward developing axial chirality bioactive compounds37
Exploring the potential of histone demethylase inhibition in multi-therapeutic approaches for cancer treatment37
Rational design of next-generation FLT3 inhibitors in acute myeloid leukemia: From laboratory to clinics37
Development of a next-generation endogenous OCT4 inducer and its anti-aging effect in vivo37
Development of fibroblast activation protein-α radiopharmaceuticals: Recent advances and perspectives37
Mitochondrial targeted hierarchical drug delivery system based on HA-modified liposomes for cancer therapy37
Expanding the antiviral arsenal: N-arylated 1,2,4-oxadiazol-5(4H)-ones show high activity against orthopoxviruses37
Discovery and optimization of isoliquiritigenin as a death-associated protein kinase 1 inhibitor37
2-Phenoxy-3, 4′-bipyridine derivatives inhibit AURKB-dependent mitotic processes by disrupting its localization36
Synthetic α-glucosidase inhibitory peptides designed by molecular docking: In vitro screening and anti-hyperglycemic efficacy in diabetic mice36
Design, synthesis, and antitumor evaluation of triazolopyridine derivatives as novel inhibitors for BRD436
Recent advances on the development of NO-releasing molecules (NORMs) for biomedical applications36
Rational design and appraisal of selective Cdc2-Like kinase 1 (Clk1) inhibitors as novel autophagy inducers for the treatment of acute liver injury (ALI)36
O-derivatization of natural tropolone and β-thujaplicin leading to effective inhibitors of human carbonic anhydrases IX and XII36
Design, synthesis and evaluation of novel oxadiazole-based compounds as potential Rac1 inhibitors against breast cancer36
Accelerated de novo design of xanthine oxidase-inhibitory peptides via physics-informed computational approaches36
Synthesis of amide-linked panaxadiol-indolinedione derivatives: A novel NSD2/H3K36me2 epigenetic modulator with significant antitumor efficacy36
Synthesis, design, and optimization of a potent and selective series of pyridylpiperazines as promising antimalarial agents36
Tandem construction of biological relevant aliphatic 5-membered N-heterocycles35
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
Microbial-derived peptides with anti-mycobacterial potential35
Discovery of indolinone-based covalent ULK1 inhibitors that suppressed autophagy and induced apoptosis against colorectal carcinoma35
Large-Scale Structure-Based Virtual Screening Identifies Diverse KNa1.1 (KCNT1) Potassium Channel Inhibitors35
The application prospects of amino acid deprivation for cancer therapy35
Structure-directed identification of pyridine-2-methylamine derivatives as MmpL3 inhibitors for use as antitubercular agents35
Advancing Src kinase inhibition: From structural design to therapeutic innovation - A comprehensive review35
Discovery of novel hybrids containing clioquinol−1-benzyl-1,2,3,6-tetrahydropyridine as multi-target-directed ligands (MTDLs) against Alzheimer's disease35
Novel antimalarial 3-substituted quinolones isosteres with improved pharmacokinetic properties35
Discovery of a novel dual-target inhibitor of CDK12 and PARP1 that induces synthetic lethality for treatment of triple-negative breast cancer35
The journey of p38 MAP kinase inhibitors: From bench to bedside in treating inflammatory diseases35
Macrocyclic-based strategy in drug design: From lab to the clinic35
New broad-spectrum and potent antibacterial agents with dual-targeting mechanism: Promoting FtsZ polymerization and disrupting bacterial membranes35
Recent advances in triazoles as tyrosinase inhibitors34
Synthesis and evaluation of N-sulfonylpiperidine-3-carboxamide derivatives as capsid assembly modulators inhibiting HBV in vitro and in HBV-transgenic mice34
Graphical abstract TOC34
Graphical abstract TOC34
Discovery of antileishmanial hits in the 3-nitroimidazo[1,2-a]pyridine series via newly optimized tetrakis(dimethylamino)ethylene (TDAE) methodology at position 234
Graphical abstract TOC34
Emerging roles of fatty acid metabolism in cancer and their targeted drug development34
Contents continued34
Design, synthesis, and biological activity evaluation of novel HDAC3 selective inhibitors for combination with Venetoclax against acute myeloid leukemia34
Chiral pool synthesis of enantiomerically pure morphan derivatives with κ receptor affinity from (S)-perillaldehyde34
Design, synthesis and biological evaluation of conformationnally-restricted analogues of E7010 as inhibitors of tubulin assembly (ITA) and vascular disrupting agents (VDA)34
SILAC-based chemoproteomics reveals a neoligan analogue as an anti-inflammatory agent targeting IRGM to ameliorate cytokine storm33
Synthesis and structure-activity relationships of novel 14-membered 2-fluoro ketolides with structural modification at the C11 position33
Design, synthesis and biological evaluation of biaryl amide derivatives against SARS-CoV-2 with dual-target mechanism33
Research progress and challenges of TRPV1 channel modulators as a prospective therapy for diabetic neuropathic pain33
Acyclic purine and pyrimidine nucleotide analogs as ecto-5′-nucleotidase (CD73) inhibitors33
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 cancer33
How many organic small molecules might be used to treat COVID-19? From natural products to synthetic agents33
Graphical abstract TOC33
Expanding the utilization of binding pockets proves to be effective for noncovalent small molecule inhibitors against SARS-CoV-2 Mpro33
Editorial Board33
Design, synthesis and activity evaluation of benzene sulfonamide derivatives as novel androgen receptor antagonist33
Plant-derived strategies to fight against severe acute respiratory syndrome coronavirus 233
Editorial Board33
New N-aryl-N′-aryl-/(thio)ureido-/sulfamoylamino-derivatives of alkyl/alkylcarbamoyl piperazines: Effect of structural modifications on selectivity over 5-HT1A receptor33
Synthesis, molecular modeling, biological and pharmacokinetic evaluation of hydroxy pyrimidinones and pyrimidinediones as novel LDHA inhibitors32
Structural basis for specific inhibition of salicylate synthase from Mycobacterium abscessus32
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 mice32
Quaternary ammonium cations conjugated 5,15-diaryltetranaphtho[2,3]porphyrins as photosensitizers for photodynamic therapy32
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) inhibitors32
Biotin-conjugated Ru(II) complexes with AIE characteristics as mitochondria-targeted photosensitizers for enhancing photodynamic therapy by disrupting cellular redox balance32
PITB: A high affinity transthyretin aggregation inhibitor with optimal pharmacokinetic properties32
Design, synthesis and anti-ovarian cancer activities of thieno[2,3-d]pyrimidine based chimeric BRD4 inhibitor/nitric oxide-donator32
Carbamoylation at C-8 position of natural 3-arylcoumarin scaffold for the discovery of novel PARP-1 inhibitors with potent anticancer activity32
An oleanic acid decorated gold nanorod for highly efficient inhibition of hemagglutinin and visible rapid detection of the influenza virus32
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) 11532
Bicyclic 2-aminopyrimidine derivatives as potent VEGFR-2 inhibitors and apoptosis Inducers: Structure-Guided design, synthesis, anticancer assessment, and in-silico exploration32
Graphical abstract TOC32
Discovery of novel pyrrolidine-2,5-dione scaffold PICK1 PDZ inhibitors as anti-ischemic stroke agents32
AR-A014418-based dual Glycogen Synthase Kinase 3β/Histone Deacetylase inhibitors as potential therapeutics for Alzheimer's disease32
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