European Journal of Medicinal Chemistry

Papers
(The TQCC of European Journal of Medicinal Chemistry is 14. 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 2021-10-01 to 2025-10-01.)
ArticleCitations
Graphical abstract contents continued469
Design and synthesis of benzothiazole aryl urea derivatives as potent anti-staphylococcal agents targeting autolysin-mediated peptidoglycan hydrolases218
Oleanolic acid derivatives against drug-resistant bacteria and fungi by multi-targets to avoid drug resistance188
Rational molecular design converting fascaplysin derivatives to potent broad-spectrum inhibitors against bacterial pathogens via targeting FtsZ180
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 arthritis163
[18F]R91150: Improved radiosynthesis and in vivo evaluation as imaging probe for 5-HT2A receptors157
Contents continued156
Graphical abstract TOC155
Non-nucleoside structured compounds with antiviral activity—past 10 years (2010–2020)154
Design, synthesis, and biological evaluation of piperazine derivatives as pan-PPARs agonists for the treatment of liver fibrosis148
Structure-based discovery of a 4,5-Dihydropyrazole-cored PET ligand for imaging of receptor-interacting serine/threonine-protein kinase 1 (RIPK1) in the brain146
Graphical abstract TOC135
Synthesis, anti-allergic rhinitis evaluation and mechanism investigation of novel 1,2,4-triazole-enamides as CB1 R antagonist123
Antitumor activity and transcriptome sequencing (RNA-seq) analyses of hepatocellular carcinoma cells in response to exposure triterpene-nucleoside conjugates122
Exploring the modulatory influence on the antimalarial activity of amodiaquine using scaffold hybridisation with ferrocene integration119
Pyrazolopyrimidines as anticancer agents: A review on structural and target-based approaches118
Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis112
Corrigendum to “Structure-based development of N-Arylindole derivatives as Pks13 inhibitors against Mycobacterium tuberculosis” [Europ. J. Med. Chem. 283 (2025) 117148]109
Synthesis and evaluation of 3,4,5-trisubstituted triazoles as G protein-biased kappa opioid receptor agonists109
Design, synthesis and in vitro evaluation of novel SARS-CoV-2 3CLpro covalent inhibitors105
Design and syntheses of a bimolecular STING agonist based on the covalent STING antagonist105
Discovery of a potent, selective and cell active inhibitor of m6A demethylase ALKBH5100
Synthesis of cinnamoyl tethered indoline derivatives with anti-inflammatory and antioxidant activities100
Exploration of P1 and P4 modifications of nirmatrelvir: Design, synthesis, biological evaluation, and X-ray structural studies of SARS-CoV-2 Mpro inhibitors97
A brain-targeting dl-3-n-butylphthalide prodrug to treat ischemic stroke97
Identification of novel diarylpyrimidine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against wild-type and K103N mutant viruses95
Discovery of novel Thieno[2,3-d]imidazole derivatives as agonists of human STING for antitumor immunotherapy using systemic administration95
Design and synthesis of forsythin derivatives as anti-inflammatory agents for acute lung injury93
A glycyrrhetinic acid-iridium(III) conjugate as a theranostic NIR probe for hepatocellular carcinoma with mitochondrial-targeting ability93
Anthraquinone derivatives as ADP-competitive inhibitors of liver pyruvate kinase91
Estrogen receptor β-targeted hypoxia-responsive near-infrared fluorescence probes for prostate cancer study89
Discovery of ML210-Based glutathione peroxidase 4 (GPX4) degrader inducing ferroptosis of human cancer cells86
From tryptophan-based amides to tertiary amines: Optimization of a butyrylcholinesterase inhibitor series86
Histone deacetylases (HDACs) as the promising immunotherapeutic targets for hematologic cancer treatment85
Discovery and biological evaluation of 6-aryl-4-(3,4,5-trimethoxyphenyl)quinoline derivatives with promising antitumor activities as novel colchicine-binding site inhibitors83
Exploring Si-phthalocyanines with different valency for PSMA-targeted photodynamic therapy: Synthesis and preclinical validation83
Fluorinated sulfonamide-flavonoid derivatives as novel Keap1-Nrf2 inhibitors: Potent induction of cytoprotective gene HO-1 in vivo82
Synthesis and evaluation of (E)-4-hydroxy-3-methyl-but-2-enyl diphosphate analogs as competitive partial agonists of butyrophilin 3A182
Discovery, structural optimization, and anti-tumor bioactivity evaluations of betulinic acid derivatives as a new type of RORγ antagonists82
Discovery of novel fused-heterocycle-bearing diarypyrimidine derivatives as HIV-1 potent NNRTIs targeting tolerant region I for enhanced antiviral activity and resistance profile81
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. 81
Synthesis of tropane-based σ1 receptor antagonists with antiallodynic activity80
EGCG-like non-competitive inhibitor of DYRK1A rescues cognitive defect in a down syndrome model79
Discovery and optimization of 4-pyrazolyl-2-aminopyrimidine derivatives as potent spleen tyrosine kinase (SYK) inhibitors79
Discovery of novel fluorine-containing parthenolide analogues as potential antitumor agents79
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 inhibitor78
The first ADC bearing the ferroptosis inducer RSL3 as a payload with conservation of the fragile electrophilic warhead76
Discovery of small molecules for autophagy-lysosome degradation of immune checkpoint proteins75
An update on small molecule compounds targeting synthetic lethality for cancer therapy75
Peptide inhibitors targeting Ras and Ras-associated protein–protein interactions74
Cinnamic acid derivatives linked to arylpiperazines as novel potent inhibitors of tyrosinase activity and melanin synthesis73
Design, synthesis and promising anti-tumor efficacy of novel imidazo[1,2-a]pyridine derivatives as potent autotaxin allosteric inhibitors73
Synthesis and antibacterial medicinal evaluation of carbothioamido hydrazonyl thiazolylquinolone with multitargeting antimicrobial potential to combat increasingly global resistance73
1,2,4-Triazolo[1,5-a]pyrimidines: Efficient one-step synthesis and functionalization as influenza polymerase PA-PB1 interaction disruptors73
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 therapy73
Novel bifluorescent Zn(II)–cryptolepine–cyclen complexes trigger apoptosis induced by nuclear and mitochondrial DNA damage in cisplatin-resistant lung tumor cells72
Novel 1,3,4-oxadiazole chalcogen analogues: Synthesis and cytotoxic activity72
Design, synthesis and biological evaluation of N-benzylaryl cinnamide derivatives as tubulin polymerization inhibitors capable of promoting YAP degradation with potent anti-gastric cancer activities71
Discovery of novel dual tubulin and MMPs inhibitors for the treatment of lung cancer and overcoming drug resistance69
Discovery of 3H-pyrrolo[2,3-c]quinolines with activity against Mycobacterium tuberculosis by allosteric inhibition of the glutamate-5-kinase enzyme69
Current trends in computer aided drug design and a highlight of drugs discovered via computational techniques: A review68
Applications of oxetanes in drug discovery and medicinal chemistry67
The mechanism of UNC-51-like kinase 1 and the applications of small molecule modulators in cancer treatment67
Monoamine oxidase inhibitors: A concise review with special emphasis on structure activity relationship studies66
Engineering a biomimicking strategy for discovering nonivamide-based quorum-sensing inhibitors for controlling bacterial infection65
Platinum(IV) complexes as inhibitors of CD47-SIRPα axis for chemoimmunotherapy of cancer65
Novel 6-hydroxybenzothiazol-2-carboxamides as potent and selective monoamine oxidase B inhibitors endowed with neuroprotective activity64
Probing benzenesulfonamide–thiazolidinone hybrids as multitarget directed ligands for efficient control of type 2 diabetes mellitus through targeting the enzymes: α-glucosidase and carbonic anhydrase 63
Discovery and biological evaluation of phthalazines as novel non-kinase TGFβ pathway inhibitors63
Antibacterial sulfonimidamide-based oligopeptides as type I signal peptidase inhibitors: Synthesis and biological evaluation63
Arginine and tryptophan-rich dendritic antimicrobial peptides that disrupt membranes for bacterial infection in vivo61
Application of deuterium in research and development of drugs60
Synthesis of 8-aminomorphans with high KOR affinity60
Straightforward access to novel mitochondriotropics derived from 2-arylethanol as potent and selective antiproliferative agents59
Rational drug design to explore the structure-activity relationship (SAR) of TRK inhibitors with 2,4-diaminopyrimidine scaffold59
H2dpa derivatives containing pentadentate ligands: An acyclic adjuvant potentiates meropenem activity in vitro and in vivo against metallo-β-lactamase-producing Enterobacterales59
Coumarin–benzimidazole hybrids: A review of developments in medicinal chemistry59
Nature-inspired new isoindole-based Passerini adducts as efficient tumor-selective apoptotic inducers via caspase-3/7 activation58
Antioxidant, anti-inflammatory and immunomodulatory roles of vitamins in COVID-19 therapy58
Exploration of 2-phenylquinoline-4-carboxamide linked benzene sulfonamide derivatives as isoform selective inhibitors of transmembrane human carbonic anhydrases58
Identification of “dual-site”-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase57
Inhibition of Histone Deacetylase 6 (HDAC6) as a therapeutic strategy for Alzheimer's disease: A review (2010–2020)57
Small-molecule MDM2 inhibitors in clinical trials for cancer therapy57
Editorial Board57
Discovery of the novel Benzo[b]thiophene 1,1-dioxide derivatives as a potent STAT3 inhibitor against idiopathic pulmonary fibrosis57
Rational design, synthesis and biological evaluation of dual PARP-1/2 and TNKS1/2 inhibitors for cancer therapy56
Novel nitrogen mustard-artemisinin hybrids with potent anti-leukemia action through DNA damage and activation of GPx56
Synthesis and evaluation of a new class of MIF-inhibitors in activated macrophage cells and in experimental septic shock in mice56
Identification of novel tetrahydroquinoxaline derived phenyl ureas as modulators of the hepatitis B virus nucleocapsid assembly55
New β-arylchalcogeno amines with procognitive properties targeting Carbonic Anhydrases and Monoamine Oxidases55
Bestatin analogs-4-quinolinone hybrids as antileishmanial hits: Design, repurposing rational, synthesis, in vitro and in silico studies55
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 cytotoxicity55
Insight on pyrimido[5,4-g]indolizine and pyrimido[4,5-c]pyrrolo[1,2-a]azepine systems as promising photosensitizers on malignant cells55
Synthesis and biological evaluation of novel pyrazole amides as potent mitochondrial complex I inhibitors54
Novel pterostilbene derivatives ameliorate heart failure by reducing oxidative stress and inflammation through regulating Nrf2/NF-κB signaling pathway54
A pro-death autophagy-based nanoplatform for enhancing antitumour efficacy with improved immune responses54
6-Regioisomeric 5,8-quinolinediones as potent CDC25 inhibitors against colorectal cancers54
Ligand-based design and synthesis of new trityl histamine and trityl cysteamine derivatives as SIRT2 inhibitors for cancer therapy54
Design, synthesis and bioevaluation of PI3Kα-selective inhibitors as potential colorectal cancer drugs54
Structure-based approaches for the design of 6-aryl-1-(3,4,5-trimethoxyphenyl)-1H-benzo[d][1,2,3]triazoles as tubulin polymerization inhibitors54
A decade of USFDA-approved small molecules as anti-inflammatory agents: Recent trends and Commentaries on the “industrial” perspective53
Discovery of N-(5-amido-2-methylphenyl)-5-methylisoxazole-3-carboxamide as dual CSF-1R/c-Kit Inhibitors with improved stability and BBB permeability53
Graphical abstract TOC53
Design, synthesis, and biological activity evaluation of novel HDAC3 selective inhibitors for combination with Venetoclax against acute myeloid leukemia52
Contents continued52
Graphical abstract TOC52
Benzimidazole analogues active against adult Schistosoma mansoni: SAR analyses, In vivo efficacy in mice, and preliminary mechanistic studies as potential inhibitors of hemozoin formation51
Targeted vancomycin delivery via in situ albumin conjugation and acid-triggered drug release for reduced nephrotoxicity51
Bioisosteric replacement of 1H-1,2,3-triazole with 1H-tetrazole ring enhances anti-leukemic activity of (5-benzylthiazol-2-yl)benzamides51
Immunosuppressive effects of new thiophene-based KV1.3 inhibitors51
A deep learning model for structure-based bioactivity optimization and its application in the bioactivity optimization of a SARS-CoV-2 main protease inhibitor51
Structure-based development of potent Plasmodium falciparum M1 and M17 aminopeptidase selective and dual inhibitors via S1′-region optimisation51
Synthesis, design, and optimization of a potent and selective series of pyridylpiperazines as promising antimalarial agents51
O-derivatization of natural tropolone and β-thujaplicin leading to effective inhibitors of human carbonic anhydrases IX and XII51
Nonsteroidal anti-inflammatory drugs (NSAIDs) and nucleotide analog GS-441524 conjugates with potent in vivo efficacy against coronaviruses51
Novel antimalarial 3-substituted quinolones isosteres with improved pharmacokinetic properties50
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 pathway50
Multicomponent syntheses enable the discovery of novel quisinostat-derived chemotypes as histone deacetylase inhibitors49
2-Phenoxy-3, 4′-bipyridine derivatives inhibit AURKB-dependent mitotic processes by disrupting its localization49
Anti-cancer efficacy of novel lonidamine derivatives: Design, synthesis, in vitro, in vivo, and computational studies targeting hexokinase-249
Synthesis and application of small molecules approved for the treatment of lymphoma49
Discovery of novel β-carboline derivatives as selective AChE inhibitors with GSK-3β inhibitory property for the treatment of Alzheimer's disease48
Progress of NIR-II fluorescence imaging technology applied to disease diagnosis and treatment48
From garden to lab: C-3 chemical modifications of tomatidine unveil broad-spectrum ATP synthase inhibitors to combat bacterial resistance48
Antibody-drug conjugates for targeted cancer therapy: Recent advances in potential payloads48
An overview on Estrogen receptors signaling and its ligands in breast cancer48
Development of a next-generation endogenous OCT4 inducer and its anti-aging effect in vivo48
Novel dual-target FAAH and TRPV1 ligands as potential pharmacotherapeutics for pain management48
Aporphines: A privileged scaffold in CNS drug discovery47
Discovery, enantioselective synthesis of myrtucommulone E analogues as tyrosyl-DNA phosphodiesterase 2 inhibitors and their biological activities47
Development of fibroblast activation protein-α radiopharmaceuticals: Recent advances and perspectives47
Design, synthesis and bioactivity evaluation of novel evodiamine derivatives with excellent potency against gastric cancer46
Discovery of novel hybrids containing clioquinol−1-benzyl-1,2,3,6-tetrahydropyridine as multi-target-directed ligands (MTDLs) against Alzheimer's disease46
Design and synthesis of harmiquins, harmine and chloroquine hybrids as potent antiplasmodial agents46
Hydrazinecarboxamides: Comprehensive review of their anticancer, anticonvulsive, anti-inflammatory, enzyme inhibition, antioxidant and other activities46
Briarane-type diterpenoids, the inhibitors of osteoclast formation by interrupting Keap1-Nrf2 interaction and activating Nrf2 pathway46
Recent advances on the development of NO-releasing molecules (NORMs) for biomedical applications45
Design, synthesis and biological evaluation of pleuromutilin-Schiff base hybrids as potent anti-MRSA agents in vitro and in vivo45
Mitochondrial targeted hierarchical drug delivery system based on HA-modified liposomes for cancer therapy45
Amphiphilic small molecule antimicrobials: From cationic antimicrobial peptides (CAMPs) to mechanism-related, structurally-diverse antimicrobials45
Microbial-derived peptides with anti-mycobacterial potential45
Design, synthesis, and antitumor evaluation of triazolopyridine derivatives as novel inhibitors for BRD444
Graphical abstract TOC44
Synthesis and biological evaluation of tyrosine derivatives as peripheral 5HT2A receptor antagonists for nonalcoholic fatty liver disease44
Graphical abstract TOC44
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
Editorial Board44
Synthesis and evaluation of chemical linchpins for highly selective CK2α targeting43
Structure-activity relationship studies and design of a PTPN22 inhibitor with enhanced isozyme selectivity and cellular efficacy43
Macrocyclic-based strategy in drug design: From lab to the clinic43
Exploring the potential of histone demethylase inhibition in multi-therapeutic approaches for cancer treatment43
Discovery of novel triazine derivatives as potent retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists43
Discovery and optimization of isoliquiritigenin as a death-associated protein kinase 1 inhibitor43
Novel angiogenesis inhibitors with superoxide anion radical amplification effect: Surmounting the Achilles’ heels of angiogenesis inhibitors and photosensitizers42
Reversal of subtype-selectivity and function by the introduction of a para-benzamidyl substituent to N-cyclopropylmethyl nornepenthone42
Corrigendum to “Discovery of novel tetrahydroquinoline derivatives as potent, selective, and orally Available AR antagonists” [Eur. J. Med. Chem. 291 (2025) 117566]42
Design, synthesis, and biological evaluation of diphenyl ether substituted quinazolin-4-amine derivatives as potent EGFRL858R/T790M/C797S inhibitors42
Design, development and evaluation of a prodrug-type TrkA-selective inhibitor with antinociceptive effects in vivo42
Design, synthesis and biological evaluation of new parbendazole derivatives for the treatment of HNSCC42
Discovery of 4-(N-dithiobenzyl piperazine)-1,8-naphthalimide as a potent multi-target antitumor agent with good efficacy, limited toxicity, and low resistance41
Mucormycosis: A hidden mystery of fungal infection, possible diagnosis, treatment and development of new therapeutic agents41
The journey of p38 MAP kinase inhibitors: From bench to bedside in treating inflammatory diseases41
Discovery of novel diaryl substituted isoquinolin-1(2H)-one derivatives as hypoxia-inducible factor-1 signaling inhibitors for the treatment of rheumatoid arthritis41
Synthesis of 10,10′-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro41
Covalent fragment mapping of KRasG12C revealed novel chemotypes with in vivo potency41
Aurora kinase inhibitors as potential anticancer agents: Recent advances40
Rational design of next-generation FLT3 inhibitors in acute myeloid leukemia: From laboratory to clinics40
Recent developments in antimalarial activities of 4-aminoquinoline derivatives40
Promises of anionic calix[n]arenes in life science: State of the art in 202340
Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo40
Antimicrobial activity of natural and semi-synthetic carbazole alkaloids40
Amidoxime prodrugs convert to potent cell-active multimodal inhibitors of the dengue virus protease40
Tandem construction of biological relevant aliphatic 5-membered N-heterocycles39
Advancing Src kinase inhibition: From structural design to therapeutic innovation - A comprehensive review39
3-Hydroxy-pyridin-4(1H)-ones as siderophores mediated delivery of isobavachalcone enhances antibacterial activity against pathogenic Pseudomonas aeruginosa39
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
Structure-based discovery of potent USP28 inhibitors derived from Vismodegib39
Synthesis and evaluation of novel ebselen derivatives as urease inhibitors for combating Helicobacter pylori infections39
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 n39
Design, synthesis and anticancer evaluation of novel Se-NSAID hybrid molecules: Identification of a Se-indomethacin analog as a potential therapeutic for breast cancer39
Novel neuroprotective 5,6-dihydropyrido[2′,1':2,3]imidazo[4,5-c]quinoline derivatives acting through cholinesterase inhibition and CB2 signaling modulation39
Design and synthesis of new 1,2,3-triazoles derived from eugenol and analogues with in vitro and in vivo activity against Trypanosoma cruzi38
Contents continued38
Discovery of a novel dual-target inhibitor of CDK12 and PARP1 that induces synthetic lethality for treatment of triple-negative breast cancer38
Targeting transthyretin in Alzheimer's disease: Drug discovery of small-molecule chaperones as disease-modifying drug candidates for Alzheimer's disease38
Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models38
Recent advances in triazoles as tyrosinase inhibitors38
Graphical abstract TOC38
Synthesis and evaluation of small molecule inhibitors of LSD1 for use against MYCN-expressing neuroblastoma38
Recent progress toward developing axial chirality bioactive compounds37
New broad-spectrum and potent antibacterial agents with dual-targeting mechanism: Promoting FtsZ polymerization and disrupting bacterial membranes37
Contents continued37
Monofunctional dimetallic Ru(η6-arene) complexes inhibit NOTCH1 signaling pathway and synergistically enhance anticancer effect in combination with cisplatin or vitamin C37
Inhibitors of ABCG2-mediated multidrug resistance: Lead generation through computer-aided drug design37
Development of novel S-N3-DABO derivatives as potent non-nucleoside reverse transcriptase inhibitors with improved potency and selectivity37
Editorial Board37
Design, synthesis, in vitro – In vivo biological evaluation of novel thiazolopyrimidine compounds as antileishmanial agent with PTR1 inhibition37
Rational design and appraisal of selective Cdc2-Like kinase 1 (Clk1) inhibitors as novel autophagy inducers for the treatment of acute liver injury (ALI)37
Graphical abstract TOC37
Structure-directed identification of pyridine-2-methylamine derivatives as MmpL3 inhibitors for use as antitubercular agents37
Design, synthesis, biological evaluation of urea substituted 1,2,5-oxadiazole-3-carboximidamides as novel indoleamine 2,3-dioxygenase-1 (IDO1) inhibitors36
Targeting RIPK1-mediated necroptosis, oxidative stress, and ferroptosis: A novel multitarget therapy for ischemic stroke36
An oleanic acid decorated gold nanorod for highly efficient inhibition of hemagglutinin and visible rapid detection of the influenza virus36
Discovery of benzopyridone cyanoacetates as new type of potential broad-spectrum antibacterial candidates36
Discovery of juglone and its derivatives as potent SARS-CoV-2 main proteinase inhibitors36
Data-oriented protein kinase drug discovery36
Graphical abstract TOC36
How many organic small molecules might be used to treat COVID-19? From natural products to synthetic agents36
Sensitive quantification of fibroblast activation protein and high-throughput screening for inhibition by FDA-approved compounds36
Quaternary ammonium cations conjugated 5,15-diaryltetranaphtho[2,3]porphyrins as photosensitizers for photodynamic therapy36
Design, synthesis and biological evaluation of N-substituted nipecotamide derivatives as multifunctional agents for epilepsy treatment36
Graphical abstract TOC36
Synthesis and evaluation of N-sulfonylpiperidine-3-carboxamide derivatives as capsid assembly modulators inhibiting HBV in vitro and in HBV-transgenic mice36
4,6-Disubstituted-1H-Indazole-4-Amine derivatives with immune-chemotherapy effect and in vivo antitumor activity36
Identification of a dual acting SARS-CoV-2 proteases inhibitor through in silico design and step-by-step biological characterization36
Mechanistic analysis of diverse click reactions along with their applications35
Positive allosteric modulators of purinergic P2X4 receptors: design, synthesis and therapeutic potential of “click” ligands for multiple sclerosis35
Design, synthesis and biological evaluation of dapsone derivatives with broad-spectrum antiviral activity35
Designed and synthesized novel tripeptides targeting diabetes and its related pathologies35
Discovery of a potential anti-ischemic stroke agent by suppressing ferroptosis through the ATF3/SLC7A11/GPX4 pathway35
Contents continued35
SAR investigation and optimization of benzimidazole-based derivatives as antimicrobial agents against Gram-negative bacteria35
AR-A014418-based dual Glycogen Synthase Kinase 3β/Histone Deacetylase inhibitors as potential therapeutics for Alzheimer's disease35
Unveiling ortho-phenolic Mannich ciprofloxacin-chalcone conjugates with potential antineoplastic activity: synthesis, mechanistic study, in silico docking and molecular dynamic simulation35
Prominent supramolecular systems for cancer Therapy: From structural design to tailored applications35
Novel E-F ring derivatives of aconitine scaffold as potent Hsp90 inhibitors for the treatment of colorectal cancer35
2-(Phenylamino)-7,8-dihydroquinazolin-5(6H)-one, a promising scaffold for MAO-B inhibitors with potential GSK3β targeting34
Acyclic purine and pyrimidine nucleotide analogs as ecto-5′-nucleotidase (CD73) inhibitors34
Bicyclic 2-aminopyrimidine derivatives as potent VEGFR-2 inhibitors and apoptosis Inducers: Structure-Guided design, synthesis, anticancer assessment, and in-silico exploration34
Editorial Board34
Editorial Board34
Graphical abstract TOC34
Discovery of 6-aryl-2-(3,4,5-trimethoxyphenyl)thiazole[3,2-b][1,2,4]triazoles as potent tubulin polymerization inhibitors34
Comprehensive coverage on anti-mycobacterial endeavour reported during 202234
Carbamoylation at C-8 position of natural 3-arylcoumarin scaffold for the discovery of novel PARP-1 inhibitors with potent anticancer activity34
Defining the structure-activity relationship for a novel class of allosteric MKP5 inhibitors34
Design, synthesis and activity evaluation of benzene sulfonamide derivatives as novel androgen receptor antagonist34
2-Substituted quinazolines: Partial agonistic and antagonistic ligands of the constitutive androstane receptor (CAR)34
Covalent inhibitors meet epigenetics: New opportunities34
Hit-to-lead optimization of 4,5-dihydrofuran-3-sulfonyl scaffold against Leishmania amazonensis. Effect of an aliphatic moiety34
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) inhibitors34
Synthesis and structure-activity relationships of novel 14-membered 2-fluoro ketolides with structural modification at the C11 position34
Recent advances in the development of inhibitors targeting KRAS-G12C and its related pathways33
Structure-activity relationship study of new carbazole sulfonamide derivatives as anticancer agents with dual-target mechanism33
The antibacterial properties of branched peptides based on poly(l-arginine): In vitro antibacterial evaluation and molecular dynamic simulations33
Isoalantolactone/hydroxamic acid hybrids as potent dual STAT3/HDAC inhibitors and self-assembled nanoparticles for cancer therapy33
A novel viscosity sensitive hemicyanine fluorescent dye for real-time imaging of amyloid-β aggregation33
An unanticipated discovery towards novel naphthalimide corbelled aminothiazoximes as potential anti-MRSA agents and allosteric modulators for PBP2a33
Structural basis for specific inhibition of salicylate synthase from Mycobacterium abscessus33
Design, synthesis and biological characterization of novel activators of the TrkB neurotrophin receptor33
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