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 2021-09-01 to 2025-09-01.)
ArticleCitations
Editorial Board453
Graphical abstract contents continued207
Discovery of novel dual tubulin and MMPs inhibitors for the treatment of lung cancer and overcoming drug resistance184
Ligand-based design and synthesis of new trityl histamine and trityl cysteamine derivatives as SIRT2 inhibitors for cancer therapy172
[18F]R91150: Improved radiosynthesis and in vivo evaluation as imaging probe for 5-HT2A receptors152
Contents continued151
Corrigendum to “Structure-based development of N-Arylindole derivatives as Pks13 inhibitors against Mycobacterium tuberculosis” [Europ. J. Med. Chem. 283 (2025) 117148]151
Graphical abstract TOC149
Discovery and biological evaluation of phthalazines as novel non-kinase TGFβ pathway inhibitors148
Non-nucleoside structured compounds with antiviral activity—past 10 years (2010–2020)141
Design, synthesis, and biological evaluation of piperazine derivatives as pan-PPARs agonists for the treatment of liver fibrosis141
Discovery of N-(5-amido-2-methylphenyl)-5-methylisoxazole-3-carboxamide as dual CSF-1R/c-Kit Inhibitors with improved stability and BBB permeability132
Structure-based discovery of a 4,5-Dihydropyrazole-cored PET ligand for imaging of receptor-interacting serine/threonine-protein kinase 1 (RIPK1) in the brain118
Synthesis of 8-aminomorphans with high KOR affinity117
Graphical abstract TOC114
1,2,4-Triazolo[1,5-a]pyrimidines: Efficient one-step synthesis and functionalization as influenza polymerase PA-PB1 interaction disruptors112
Synthesis, anti-allergic rhinitis evaluation and mechanism investigation of novel 1,2,4-triazole-enamides as CB1 R antagonist109
H2dpa derivatives containing pentadentate ligands: An acyclic adjuvant potentiates meropenem activity in vitro and in vivo against metallo-β-lactamase-producing Enterobacterales107
Discovery of ML210-Based glutathione peroxidase 4 (GPX4) degrader inducing ferroptosis of human cancer cells105
Antitumor activity and transcriptome sequencing (RNA-seq) analyses of hepatocellular carcinoma cells in response to exposure triterpene-nucleoside conjugates100
Novel 6-hydroxybenzothiazol-2-carboxamides as potent and selective monoamine oxidase B inhibitors endowed with neuroprotective activity98
Small-molecule MDM2 inhibitors in clinical trials for cancer therapy95
6-Regioisomeric 5,8-quinolinediones as potent CDC25 inhibitors against colorectal cancers95
Bestatin analogs-4-quinolinone hybrids as antileishmanial hits: Design, repurposing rational, synthesis, in vitro and in silico studies94
Antibacterial sulfonimidamide-based oligopeptides as type I signal peptidase inhibitors: Synthesis and biological evaluation94
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 93
Design and synthesis of forsythin derivatives as anti-inflammatory agents for acute lung injury91
Discovery of the novel Benzo[b]thiophene 1,1-dioxide derivatives as a potent STAT3 inhibitor against idiopathic pulmonary fibrosis91
Coumarin–benzimidazole hybrids: A review of developments in medicinal chemistry91
Exploration of P1 and P4 modifications of nirmatrelvir: Design, synthesis, biological evaluation, and X-ray structural studies of SARS-CoV-2 Mpro inhibitors90
Synthesis of cinnamoyl tethered indoline derivatives with anti-inflammatory and antioxidant activities86
Straightforward access to novel mitochondriotropics derived from 2-arylethanol as potent and selective antiproliferative agents85
Design, synthesis and bioevaluation of PI3Kα-selective inhibitors as potential colorectal cancer drugs85
A brain-targeting dl-3-n-butylphthalide prodrug to treat ischemic stroke82
Exploring Si-phthalocyanines with different valency for PSMA-targeted photodynamic therapy: Synthesis and preclinical validation81
Novel nitrogen mustard-artemisinin hybrids with potent anti-leukemia action through DNA damage and activation of GPx79
Synthesis and evaluation of a new class of MIF-inhibitors in activated macrophage cells and in experimental septic shock in mice79
Discovery of novel Thieno[2,3-d]imidazole derivatives as agonists of human STING for antitumor immunotherapy using systemic administration78
Discovery of 3H-pyrrolo[2,3-c]quinolines with activity against Mycobacterium tuberculosis by allosteric inhibition of the glutamate-5-kinase enzyme78
Identification of novel diarylpyrimidine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against wild-type and K103N mutant viruses78
Discovery, structural optimization, and anti-tumor bioactivity evaluations of betulinic acid derivatives as a new type of RORγ antagonists76
Discovery and biological evaluation of 6-aryl-4-(3,4,5-trimethoxyphenyl)quinoline derivatives with promising antitumor activities as novel colchicine-binding site inhibitors76
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 therapy76
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 cytotoxicity76
Design, synthesis and biological evaluation of N-benzylaryl cinnamide derivatives as tubulin polymerization inhibitors capable of promoting YAP degradation with potent anti-gastric cancer activities76
Peptide inhibitors targeting Ras and Ras-associated protein–protein interactions75
EGCG-like non-competitive inhibitor of DYRK1A rescues cognitive defect in a down syndrome model74
Discovery of novel fluorine-containing parthenolide analogues as potential antitumor agents74
Synthesis and evaluation of (E)-4-hydroxy-3-methyl-but-2-enyl diphosphate analogs as competitive partial agonists of butyrophilin 3A173
Arginine and tryptophan-rich dendritic antimicrobial peptides that disrupt membranes for bacterial infection in vivo72
Rational drug design to explore the structure-activity relationship (SAR) of TRK inhibitors with 2,4-diaminopyrimidine scaffold72
Fluorinated sulfonamide-flavonoid derivatives as novel Keap1-Nrf2 inhibitors: Potent induction of cytoprotective gene HO-1 in vivo71
Synthesis and biological evaluation of novel pyrazole amides as potent mitochondrial complex I inhibitors71
Insight on pyrimido[5,4-g]indolizine and pyrimido[4,5-c]pyrrolo[1,2-a]azepine systems as promising photosensitizers on malignant cells70
Discovery of novel fused-heterocycle-bearing diarypyrimidine derivatives as HIV-1 potent NNRTIs targeting tolerant region I for enhanced antiviral activity and resistance profile70
Synthesis of tropane-based σ1 receptor antagonists with antiallodynic activity70
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. 70
New β-arylchalcogeno amines with procognitive properties targeting Carbonic Anhydrases and Monoamine Oxidases68
Discovery and optimization of 4-pyrazolyl-2-aminopyrimidine derivatives as potent spleen tyrosine kinase (SYK) inhibitors67
A pro-death autophagy-based nanoplatform for enhancing antitumour efficacy with improved immune responses66
Cinnamic acid derivatives linked to arylpiperazines as novel potent inhibitors of tyrosinase activity and melanin synthesis66
A glycyrrhetinic acid-iridium(III) conjugate as a theranostic NIR probe for hepatocellular carcinoma with mitochondrial-targeting ability66
Novel 1,3,4-oxadiazole chalcogen analogues: Synthesis and cytotoxic activity63
Platinum(IV) complexes as inhibitors of CD47-SIRPα axis for chemoimmunotherapy of cancer63
Design and syntheses of a bimolecular STING agonist based on the covalent STING antagonist63
Design, synthesis and promising anti-tumor efficacy of novel imidazo[1,2-a]pyridine derivatives as potent autotaxin allosteric inhibitors62
Exploring the modulatory influence on the antimalarial activity of amodiaquine using scaffold hybridisation with ferrocene integration62
Pyrazolopyrimidines as anticancer agents: A review on structural and target-based approaches61
The mechanism of UNC-51-like kinase 1 and the applications of small molecule modulators in cancer treatment61
Design and synthesis of benzothiazole aryl urea derivatives as potent anti-staphylococcal agents targeting autolysin-mediated peptidoglycan hydrolases59
Exploration of 2-phenylquinoline-4-carboxamide linked benzene sulfonamide derivatives as isoform selective inhibitors of transmembrane human carbonic anhydrases58
Rational molecular design converting fascaplysin derivatives to potent broad-spectrum inhibitors against bacterial pathogens via targeting FtsZ57
Rational design, synthesis and biological evaluation of dual PARP-1/2 and TNKS1/2 inhibitors for cancer therapy57
Oleanolic acid derivatives against drug-resistant bacteria and fungi by multi-targets to avoid drug resistance57
Inhibition of Histone Deacetylase 6 (HDAC6) as a therapeutic strategy for Alzheimer's disease: A review (2010–2020)56
Synthesis and evaluation of 3,4,5-trisubstituted triazoles as G protein-biased kappa opioid receptor agonists56
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 arthritis56
Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis56
Antioxidant, anti-inflammatory and immunomodulatory roles of vitamins in COVID-19 therapy55
Synthesis and antibacterial medicinal evaluation of carbothioamido hydrazonyl thiazolylquinolone with multitargeting antimicrobial potential to combat increasingly global resistance55
Monoamine oxidase inhibitors: A concise review with special emphasis on structure activity relationship studies55
Identification of novel tetrahydroquinoxaline derived phenyl ureas as modulators of the hepatitis B virus nucleocapsid assembly55
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
Anthraquinone derivatives as ADP-competitive inhibitors of liver pyruvate kinase55
Novel bifluorescent Zn(II)–cryptolepine–cyclen complexes trigger apoptosis induced by nuclear and mitochondrial DNA damage in cisplatin-resistant lung tumor cells55
Engineering a biomimicking strategy for discovering nonivamide-based quorum-sensing inhibitors for controlling bacterial infection55
Structure-based approaches for the design of 6-aryl-1-(3,4,5-trimethoxyphenyl)-1H-benzo[d][1,2,3]triazoles as tubulin polymerization inhibitors55
Applications of oxetanes in drug discovery and medicinal chemistry54
Nature-inspired new isoindole-based Passerini adducts as efficient tumor-selective apoptotic inducers via caspase-3/7 activation54
Design, synthesis and in vitro evaluation of novel SARS-CoV-2 3CLpro covalent inhibitors54
Histone deacetylases (HDACs) as the promising immunotherapeutic targets for hematologic cancer treatment53
From tryptophan-based amides to tertiary amines: Optimization of a butyrylcholinesterase inhibitor series53
An update on small molecule compounds targeting synthetic lethality for cancer therapy53
Discovery of small molecules for autophagy-lysosome degradation of immune checkpoint proteins52
Novel pterostilbene derivatives ameliorate heart failure by reducing oxidative stress and inflammation through regulating Nrf2/NF-κB signaling pathway52
Estrogen receptor β-targeted hypoxia-responsive near-infrared fluorescence probes for prostate cancer study52
A decade of USFDA-approved small molecules as anti-inflammatory agents: Recent trends and Commentaries on the “industrial” perspective52
Application of deuterium in research and development of drugs52
The first ADC bearing the ferroptosis inducer RSL3 as a payload with conservation of the fragile electrophilic warhead52
Identification of “dual-site”-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase52
Current trends in computer aided drug design and a highlight of drugs discovered via computational techniques: A review52
Graphical abstract TOC51
Graphical abstract TOC51
Graphical abstract TOC51
Discovery of a potent, selective and cell active inhibitor of m6A demethylase ALKBH551
Contents continued51
Structure-based development of potent Plasmodium falciparum M1 and M17 aminopeptidase selective and dual inhibitors via S1′-region optimisation50
Design, synthesis, and antitumor evaluation of triazolopyridine derivatives as novel inhibitors for BRD450
Nonsteroidal anti-inflammatory drugs (NSAIDs) and nucleotide analog GS-441524 conjugates with potent in vivo efficacy against coronaviruses50
Contents continued50
Design, synthesis, and biological activity evaluation of novel HDAC3 selective inhibitors for combination with Venetoclax against acute myeloid leukemia50
Bioisosteric replacement of 1H-1,2,3-triazole with 1H-tetrazole ring enhances anti-leukemic activity of (5-benzylthiazol-2-yl)benzamides49
Monofunctional dimetallic Ru(η6-arene) complexes inhibit NOTCH1 signaling pathway and synergistically enhance anticancer effect in combination with cisplatin or vitamin C49
Synthesis, design, and optimization of a potent and selective series of pyridylpiperazines as promising antimalarial agents48
O-derivatization of natural tropolone and β-thujaplicin leading to effective inhibitors of human carbonic anhydrases IX and XII48
Targeted vancomycin delivery via in situ albumin conjugation and acid-triggered drug release for reduced nephrotoxicity48
Covalent fragment mapping of KRasG12C revealed novel chemotypes with in vivo potency48
A deep learning model for structure-based bioactivity optimization and its application in the bioactivity optimization of a SARS-CoV-2 main protease inhibitor48
Immunosuppressive effects of new thiophene-based KV1.3 inhibitors47
Briarane-type diterpenoids, the inhibitors of osteoclast formation by interrupting Keap1-Nrf2 interaction and activating Nrf2 pathway47
Rational design and appraisal of selective Cdc2-Like kinase 1 (Clk1) inhibitors as novel autophagy inducers for the treatment of acute liver injury (ALI)47
Novel antimalarial 3-substituted quinolones isosteres with improved pharmacokinetic properties47
Benzimidazole analogues active against adult Schistosoma mansoni: SAR analyses, In vivo efficacy in mice, and preliminary mechanistic studies as potential inhibitors of hemozoin formation47
Discovery of novel diaryl substituted isoquinolin-1(2H)-one derivatives as hypoxia-inducible factor-1 signaling inhibitors for the treatment of rheumatoid arthritis46
Multicomponent syntheses enable the discovery of novel quisinostat-derived chemotypes as histone deacetylase inhibitors46
Mitochondrial targeted hierarchical drug delivery system based on HA-modified liposomes for cancer therapy46
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 pathway46
2-Phenoxy-3, 4′-bipyridine derivatives inhibit AURKB-dependent mitotic processes by disrupting its localization46
Discovery of novel β-carboline derivatives as selective AChE inhibitors with GSK-3β inhibitory property for the treatment of Alzheimer's disease45
Development of fibroblast activation protein-α radiopharmaceuticals: Recent advances and perspectives45
Design, synthesis, in vitro – In vivo biological evaluation of novel thiazolopyrimidine compounds as antileishmanial agent with PTR1 inhibition45
Recent developments in antimalarial activities of 4-aminoquinoline derivatives45
Synthesis and application of small molecules approved for the treatment of lymphoma45
Design and synthesis of harmiquins, harmine and chloroquine hybrids as potent antiplasmodial agents45
Discovery of 4-(N-dithiobenzyl piperazine)-1,8-naphthalimide as a potent multi-target antitumor agent with good efficacy, limited toxicity, and low resistance45
Discovery and optimization of isoliquiritigenin as a death-associated protein kinase 1 inhibitor44
Tandem construction of biological relevant aliphatic 5-membered N-heterocycles44
Advancing Src kinase inhibition: From structural design to therapeutic innovation - A comprehensive review44
Development of a next-generation endogenous OCT4 inducer and its anti-aging effect in vivo43
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 n43
Progress of NIR-II fluorescence imaging technology applied to disease diagnosis and treatment43
Novel dual-target FAAH and TRPV1 ligands as potential pharmacotherapeutics for pain management43
Antibody-drug conjugates for targeted cancer therapy: Recent advances in potential payloads43
Promises of anionic calix[n]arenes in life science: State of the art in 202342
Amphiphilic small molecule antimicrobials: From cationic antimicrobial peptides (CAMPs) to mechanism-related, structurally-diverse antimicrobials42
Targeting transthyretin in Alzheimer's disease: Drug discovery of small-molecule chaperones as disease-modifying drug candidates for Alzheimer's disease42
Design, synthesis and bioactivity evaluation of novel evodiamine derivatives with excellent potency against gastric cancer42
Microbial-derived peptides with anti-mycobacterial potential42
From garden to lab: C-3 chemical modifications of tomatidine unveil broad-spectrum ATP synthase inhibitors to combat bacterial resistance42
Antimicrobial activity of natural and semi-synthetic carbazole alkaloids42
Structure-activity relationship studies and design of a PTPN22 inhibitor with enhanced isozyme selectivity and cellular efficacy41
Graphical abstract TOC41
Editorial Board41
Graphical abstract TOC41
Development of novel S-N3-DABO derivatives as potent non-nucleoside reverse transcriptase inhibitors with improved potency and selectivity41
Discovery of novel triazine derivatives as potent retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists41
Synthesis and evaluation of novel ebselen derivatives as urease inhibitors for combating Helicobacter pylori infections41
Recent advances in triazoles as tyrosinase inhibitors40
Recent progress toward developing axial chirality bioactive compounds40
Synthesis of 10,10′-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro40
Discovery, enantioselective synthesis of myrtucommulone E analogues as tyrosyl-DNA phosphodiesterase 2 inhibitors and their biological activities39
SAR and lead optimization of (Z)-5-(4-hydroxy-3-methoxybenzylidene)-3-(2-morpholinoacetyl)thiazolidine-2,4-dione as a potential multi-target antidiabetic agent39
Macrocyclic-based strategy in drug design: From lab to the clinic39
Synthesis and evaluation of chemical linchpins for highly selective CK2α targeting39
Novel angiogenesis inhibitors with superoxide anion radical amplification effect: Surmounting the Achilles’ heels of angiogenesis inhibitors and photosensitizers39
Synthesis and biological evaluation of tyrosine derivatives as peripheral 5HT2A receptor antagonists for nonalcoholic fatty liver disease39
Recent advances on the development of NO-releasing molecules (NORMs) for biomedical applications39
Structure-directed identification of pyridine-2-methylamine derivatives as MmpL3 inhibitors for use as antitubercular agents39
Design, synthesis, and biological evaluation of diphenyl ether substituted quinazolin-4-amine derivatives as potent EGFRL858R/T790M/C797S inhibitors38
Design, synthesis and biological evaluation of new parbendazole derivatives for the treatment of HNSCC38
Corrigendum to “Discovery of novel tetrahydroquinoline derivatives as potent, selective, and orally Available AR antagonists” [Eur. J. Med. Chem. 291 (2025) 117566]38
Structure-based discovery of potent USP28 inhibitors derived from Vismodegib38
Design, development and evaluation of a prodrug-type TrkA-selective inhibitor with antinociceptive effects in vivo38
Reversal of subtype-selectivity and function by the introduction of a para-benzamidyl substituent to N-cyclopropylmethyl nornepenthone38
Amidoxime prodrugs convert to potent cell-active multimodal inhibitors of the dengue virus protease38
Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo38
Aporphines: A privileged scaffold in CNS drug discovery37
Hydrazinecarboxamides: Comprehensive review of their anticancer, anticonvulsive, anti-inflammatory, enzyme inhibition, antioxidant and other activities37
New broad-spectrum and potent antibacterial agents with dual-targeting mechanism: Promoting FtsZ polymerization and disrupting bacterial membranes37
Discovery of a novel dual-target inhibitor of CDK12 and PARP1 that induces synthetic lethality for treatment of triple-negative breast cancer37
Inhibitors of ABCG2-mediated multidrug resistance: Lead generation through computer-aided drug design37
Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models37
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
Design and synthesis of new 1,2,3-triazoles derived from eugenol and analogues with in vitro and in vivo activity against Trypanosoma cruzi36
Design, synthesis and anticancer evaluation of novel Se-NSAID hybrid molecules: Identification of a Se-indomethacin analog as a potential therapeutic for breast cancer36
Discovery of novel hybrids containing clioquinol−1-benzyl-1,2,3,6-tetrahydropyridine as multi-target-directed ligands (MTDLs) against Alzheimer's disease36
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 neuroprotection36
Contents continued36
Novel neuroprotective 5,6-dihydropyrido[2′,1':2,3]imidazo[4,5-c]quinoline derivatives acting through cholinesterase inhibition and CB2 signaling modulation36
Exploring the potential of histone demethylase inhibition in multi-therapeutic approaches for cancer treatment36
Design, synthesis and biological evaluation of pleuromutilin-Schiff base hybrids as potent anti-MRSA agents in vitro and in vivo36
Graphical abstract TOC36
3-Hydroxy-pyridin-4(1H)-ones as siderophores mediated delivery of isobavachalcone enhances antibacterial activity against pathogenic Pseudomonas aeruginosa36
Mucormycosis: A hidden mystery of fungal infection, possible diagnosis, treatment and development of new therapeutic agents36
Synthesis and evaluation of small molecule inhibitors of LSD1 for use against MYCN-expressing neuroblastoma36
Aurora kinase inhibitors as potential anticancer agents: Recent advances36
An overview on Estrogen receptors signaling and its ligands in breast cancer36
Graphical abstract TOC36
The journey of p38 MAP kinase inhibitors: From bench to bedside in treating inflammatory diseases36
Graphical abstract TOC35
An oleanic acid decorated gold nanorod for highly efficient inhibition of hemagglutinin and visible rapid detection of the influenza virus35
How many organic small molecules might be used to treat COVID-19? From natural products to synthetic agents35
Expanding the utilization of binding pockets proves to be effective for noncovalent small molecule inhibitors against SARS-CoV-2 Mpro35
Graphical abstract TOC35
Identification of thiophene-benzenesulfonamide derivatives for the treatment of multidrug-resistant tuberculosis35
Identification of a dual acting SARS-CoV-2 proteases inhibitor through in silico design and step-by-step biological characterization35
Editorial Board35
Sensitive quantification of fibroblast activation protein and high-throughput screening for inhibition by FDA-approved compounds35
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
Editorial Board34
The antibacterial properties of branched peptides based on poly(l-arginine): In vitro antibacterial evaluation and molecular dynamic simulations34
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
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 cancer34
Novel spiro[chromanone-2,4′-piperidine]-4-one derivatives as potential inhibitors of fatty acid synthesis in pathogens: Design, synthesis, and biological evaluation34
A novel viscosity sensitive hemicyanine fluorescent dye for real-time imaging of amyloid-β aggregation34
Synthesis and evaluation of N-sulfonylpiperidine-3-carboxamide derivatives as capsid assembly modulators inhibiting HBV in vitro and in HBV-transgenic mice34
New N-aryl-N′-aryl-/(thio)ureido-/sulfamoylamino-derivatives of alkyl/alkylcarbamoyl piperazines: Effect of structural modifications on selectivity over 5-HT1A receptor34
A novel Al18F-labelled NOTA-modified ubiquicidin 29-41 derivative as a bacterial infection PET imaging agent34
Design, synthesis and biological evaluation of conformationnally-restricted analogues of E7010 as inhibitors of tubulin assembly (ITA) and vascular disrupting agents (VDA)34
Structure-based discovery of potent myosin inhibitors to guide antiparasite drug development34
Discovery of novel polyheterocyclic neuraminidase inhibitors with 1,3,4-oxadiazole thioetheramide as core backbone34
PITB: A high affinity transthyretin aggregation inhibitor with optimal pharmacokinetic properties34
Editorial Board34
A novel antimicrobial peptide with broad-spectrum and exceptional stability derived from the natural peptide Brevicidine33
Structure-activity relationship study of new carbazole sulfonamide derivatives as anticancer agents with dual-target mechanism33
Defining the structure-activity relationship for a novel class of allosteric MKP5 inhibitors33
Identification and immunological evaluation of novel TLR2 agonists through structural optimization of Diprovocim33
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) inhibitors33
Graphical abstract TOC33
Hit-to-lead optimization of 4,5-dihydrofuran-3-sulfonyl scaffold against Leishmania amazonensis. Effect of an aliphatic moiety33
Design, synthesis and biological evaluation of biaryl amide derivatives against SARS-CoV-2 with dual-target mechanism33
Comprehensive coverage on anti-mycobacterial endeavour reported during 202233
Quaternary ammonium cations conjugated 5,15-diaryltetranaphtho[2,3]porphyrins as photosensitizers for photodynamic therapy33
Synthesis and structure-activity relationships of novel 14-membered 2-fluoro ketolides with structural modification at the C11 position33
Carbamoylation at C-8 position of natural 3-arylcoumarin scaffold for the discovery of novel PARP-1 inhibitors with potent anticancer activity33
Insight into small-molecule inhibitors targeting extracellular nucleotide pyrophosphatase/phosphodiesterase1 for potential multiple human diseases32
Covalent inhibitors meet epigenetics: New opportunities32
SAR investigation and optimization of benzimidazole-based derivatives as antimicrobial agents against Gram-negative bacteria32
Prominent supramolecular systems for cancer Therapy: From structural design to tailored applications32
Discovery of Artesunate (ARS) PROTACs as GPX4 protein degraders for the treatment of bladder cancer32
2-(Phenylamino)-7,8-dihydroquinazolin-5(6H)-one, a promising scaffold for MAO-B inhibitors with potential GSK3β targeting32
Design, synthesis and activity evaluation of benzene sulfonamide derivatives as novel androgen receptor antagonist32
2-Substituted quinazolines: Partial agonistic and antagonistic ligands of the constitutive androstane receptor (CAR)32
Emerging roles of fatty acid metabolism in cancer and their targeted drug development32
FLT3-PROTACs for combating AML resistance: Analytical overview on chimeric agents developed, challenges, and future perspectives32
Acyclic purine and pyrimidine nucleotide analogs as ecto-5′-nucleotidase (CD73) inhibitors32
Bicyclic 2-aminopyrimidine derivatives as potent VEGFR-2 inhibitors and apoptosis Inducers: Structure-Guided design, synthesis, anticancer assessment, and in-silico exploration32
Discovery and development of a novel N-(3-bromophenyl)-{[(phenylcarbamoyl)amino]methyl}-N-hydroxythiophene-2-carboximidamide indoleamine 2,3-dioxygenase inhibitor using knowledge-based drug design31
Development of high-affinity fluorinated ligands for cannabinoid subtype 2 receptor, and in vitro evaluation of a radioactive tracer for imaging31
Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections31
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