European Journal of Medicinal Chemistry

Article	Citations
Contents continued	237
Graphical abstract TOC	191
Graphical abstract TOC	186
A brain-targeting dl-3-n-butylphthalide prodrug to treat ischemic stroke	177
Structure-based approaches for the design of 6-aryl-1-(3,4,5-trimethoxyphenyl)-1H-benzo[d][1,2,3]triazoles as tubulin polymerization inhibitors	158
[18F]R91150: Improved radiosynthesis and in vivo evaluation as imaging probe for 5-HT2A receptors	144
Synthesis of cinnamoyl tethered indoline derivatives with anti-inflammatory and antioxidant activities	118
Corrigendum to “Structure-based development of N-Arylindole derivatives as Pks13 inhibitors against Mycobacterium tuberculosis” [Europ. J. Med. Chem. 283 (2025) 117148]	114
Novel pterostilbene derivatives ameliorate heart failure by reducing oxidative stress and inflammation through regulating Nrf2/NF-κB signaling pathway	112
Identification of novel tetrahydroquinoxaline derived phenyl ureas as modulators of the hepatitis B virus nucleocapsid assembly	108
Synthesis and evaluation of (E)-4-hydroxy-3-methyl-but-2-enyl diphosphate analogs as competitive partial agonists of butyrophilin 3A1	106
Editorial Board	106
Discovery of novel fluorine-containing parthenolide analogues as potential antitumor agents	104
Structure-based discovery of a 4,5-Dihydropyrazole-cored PET ligand for imaging of receptor-interacting serine/threonine-protein kinase 1 (RIPK1) in the brain	103
Inhibitors of membrane associated serine proteases block replication of coronavirus SARS-CoV-2 and influenza virus H1N1	99
Identification of “dual-site”-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase	92
Design and syntheses of a bimolecular STING agonist based on the covalent STING antagonist	92
Novel bifluorescent Zn(II)–cryptolepine–cyclen complexes trigger apoptosis induced by nuclear and mitochondrial DNA damage in cisplatin-resistant lung tumor cells	91
Rational molecular design converting fascaplysin derivatives to potent broad-spectrum inhibitors against bacterial pathogens via targeting FtsZ	91
Design, synthesis, and biological evaluation of piperazine derivatives as pan-PPARs agonists for the treatment of liver fibrosis	90
Antitumor activity and transcriptome sequencing (RNA-seq) analyses of hepatocellular carcinoma cells in response to exposure triterpene-nucleoside conjugates	89
A pro-death autophagy-based nanoplatform for enhancing antitumour efficacy with improved immune responses	89
Design, synthesis and promising anti-tumor efficacy of novel imidazo[1,2-a]pyridine derivatives as potent autotaxin allosteric inhibitors	88
Rational design, synthesis and biological evaluation of dual PARP-1/2 and TNKS1/2 inhibitors for cancer therapy	88
An update on small molecule compounds targeting synthetic lethality for cancer therapy	87

Design, synthesis, and biological evaluation of hybrids from both nitrones with eNOS-mimicking activity and selective iNOS inhibitors for the treatment of ischemic stroke	85
Discovery of tetrahydrothiazolopyridine-incorporated curcumol derivatives as novel and highly potent anti-cancer agents	83
A medicinal chemistry perspective on disruptor of telomeric silencing 1-like: Its mechanisms and modulators in cancer treatment	81
6-Regioisomeric 5,8-quinolinediones as potent CDC25 inhibitors against colorectal cancers	80
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 arthritis	79
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 inhibitor	79
Identification of novel diarylpyrimidine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against wild-type and K103N mutant viruses	79
Exploring the modulatory influence on the antimalarial activity of amodiaquine using scaffold hybridisation with ferrocene integration	79
Trimethyl Lock-2Cl (TML-2Cl): A self-cyclizing adapter for molecular release in antibody-drug conjugates	78
Design and synthesis of forsythin derivatives as anti-inflammatory agents for acute lung injury	75
The mechanism of UNC-51-like kinase 1 and the applications of small molecule modulators in cancer treatment	75
Nature-inspired new isoindole-based Passerini adducts as efficient tumor-selective apoptotic inducers via caspase-3/7 activation	74
Oleanolic acid derivatives against drug-resistant bacteria and fungi by multi-targets to avoid drug resistance	74
Novel 1,3,4-oxadiazole chalcogen analogues: Synthesis and cytotoxic activity	74
Synthesis of diarylpentane derivatives as novel α-glucosidase inhibitors: Their inhibitory mechanism and hypoglycemic effects	73
Editorial Board	73
Multitarget-directed carbamate and carbamothioate derivatives: Cholinesterase and monoamine oxidase inhibition, anti-β-amyloid (Aβ) aggregation, antioxidant and blood–brain barrier permeation properti	72
Histone deacetylases (HDACs) as the promising immunotherapeutic targets for hematologic cancer treatment	71
Synthesis and evaluation of 3,4,5-trisubstituted triazoles as G protein-biased kappa opioid receptor agonists	71
Discovery of the novel Benzo[b]thiophene 1,1-dioxide derivatives as a potent STAT3 inhibitor against idiopathic pulmonary fibrosis	70
Novel β-carboline derivatives show promise as dual-target inhibitors of DNA and TOP2A for the treatment of triple negative breast cancer	70
Discovery of anti-tumor targets based on photo-affinity labeling	68
Discovery of small molecules for autophagy-lysosome degradation of immune checkpoint proteins	67
Discovery and optimization of 4-pyrazolyl-2-aminopyrimidine derivatives as potent spleen tyrosine kinase (SYK) inhibitors	66
A decade of USFDA-approved small molecules as anti-inflammatory agents: Recent trends and Commentaries on the “industrial” perspective	65
Novel nitrogen mustard-artemisinin hybrids with potent anti-leukemia action through DNA damage and activation of GPx	65
Arginine and tryptophan-rich dendritic antimicrobial peptides that disrupt membranes for bacterial infection in vivo	64
Active fragment assembly strategy enabling fast discovery of KRAS inhibitors against pancreatic cancer cells	64
Novel 6-hydroxybenzothiazol-2-carboxamides as potent and selective monoamine oxidase B inhibitors endowed with neuroprotective activity	63
Discovery of ML210-Based glutathione peroxidase 4 (GPX4) degrader inducing ferroptosis of human cancer cells	62
Discovery of novel Thieno[2,3-d]imidazole derivatives as agonists of human STING for antitumor immunotherapy using systemic administration	62
Amino acid–modified chalcone derivatives with in vitro and in vivo efficacy against colon cancer	62
Engineering a biomimicking strategy for discovering nonivamide-based quorum-sensing inhibitors for controlling bacterial infection	61
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	61
Ligand-based design and synthesis of new trityl histamine and trityl cysteamine derivatives as SIRT2 inhibitors for cancer therapy	61
Application of deuterium in research and development of drugs	60
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.	59
Fluorinated sulfonamide-flavonoid derivatives as novel Keap1-Nrf2 inhibitors: Potent induction of cytoprotective gene HO-1 in vivo	59
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 cytotoxicity	59
Exploring Si-phthalocyanines with different valency for PSMA-targeted photodynamic therapy: Synthesis and preclinical validation	58
Design, synthesis and bioevaluation of PI3Kα-selective inhibitors as potential colorectal cancer drugs	58
Monoamine oxidase inhibitors: A concise review with special emphasis on structure activity relationship studies	57
Discovery of a potent, selective and cell active inhibitor of m6A demethylase ALKBH5	57
Functional quinoline-malononitriles for enhanced wound repair and monitoring	57
Structure-activity relationship of N-cyclopropylmethyl-7α-(m-methylaminophenyl)-6,14-endoethano-northebaine derivatives as G-protein-biased KOR-selective agonists	57
Recent developments in the synthesis of indolizines and their derivatives as compounds of interest in medicinal chemistry: a review	55
Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis	55
Synthesis, anti-allergic rhinitis evaluation and mechanism investigation of novel 1,2,4-triazole-enamides as CB1 R antagonist	55
Discovery of N-(5-amido-2-methylphenyl)-5-methylisoxazole-3-carboxamide as dual CSF-1R/c-Kit Inhibitors with improved stability and BBB permeability	54
A glycyrrhetinic acid-iridium(III) conjugate as a theranostic NIR probe for hepatocellular carcinoma with mitochondrial-targeting ability	54

Discovery and biological evaluation of 6-aryl-4-(3,4,5-trimethoxyphenyl)quinoline derivatives with promising antitumor activities as novel colchicine-binding site inhibitors	54
Insight on pyrimido[5,4-g]indolizine and pyrimido[4,5-c]pyrrolo[1,2-a]azepine systems as promising photosensitizers on malignant cells	54
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 therapy	53
1,3-Thiazole nucleus as promising molecular platform against antimicrobial resistance: a recent overview in drug discovery	53
Design, synthesis, evaluation and X-ray structural studies of potent HIV-1 protease inhibitors containing substituted oxaspirocyclic carbamates as the P2 ligands	53
Poly(ADP-ribose) polymerase-1 (PARP1)-based dual inhibitors targeting cancer synthetic lethality (2022-present): advances and perspectives	53
Peptide inhibitors targeting Ras and Ras-associated protein–protein interactions	52
Synthesis and evaluation of a novel class of spiro[chromene-2,2′-indoline] derivatives as potent inhibitors of peptidylarginine deiminase IV to treat rheumatoid arthritis	52
Discovery, structural optimization, and anti-tumor bioactivity evaluations of betulinic acid derivatives as a new type of RORγ antagonists	52
Exploration of P1 and P4 modifications of nirmatrelvir: Design, synthesis, biological evaluation, and X-ray structural studies of SARS-CoV-2 Mpro inhibitors	52
Estrogen receptor β-targeted hypoxia-responsive near-infrared fluorescence probes for prostate cancer study	52
New β-arylchalcogeno amines with procognitive properties targeting Carbonic Anhydrases and Monoamine Oxidases	51
Discovery of p300 histone acetyltransferase inhibitors bearing an imidazo[4,5-b]pyridine-2-one scaffold for the treatment of multiple myeloma	51
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 model	51
Water molecules in the cannabinoid receptor 2 binding site crucially impact the discovery of novel ligands	50
EGCG-like non-competitive inhibitor of DYRK1A rescues cognitive defect in a down syndrome model	50
Bestatin analogs-4-quinolinone hybrids as antileishmanial hits: Design, repurposing rational, synthesis, in vitro and in silico studies	50
The first ADC bearing the ferroptosis inducer RSL3 as a payload with conservation of the fragile electrophilic warhead	50
Discovery of novel fused-heterocycle-bearing diarypyrimidine derivatives as HIV-1 potent NNRTIs targeting tolerant region I for enhanced antiviral activity and resistance profile	50
Synthesis and biological evaluation of α-D-tocopherol derivatives as anticancer agents targeting mitochondrial metabolism	49
Discovery of novel dual tubulin and MMPs inhibitors for the treatment of lung cancer and overcoming drug resistance	49
Design and synthesis of benzothiazole aryl urea derivatives as potent anti-staphylococcal agents targeting autolysin-mediated peptidoglycan hydrolases	49
Design, synthesis and biological evaluation of N-benzylaryl cinnamide derivatives as tubulin polymerization inhibitors capable of promoting YAP degradation with potent anti-gastric cancer activities	49
Small-molecule MDM2 inhibitors in clinical trials for cancer therapy	48
Synthesis and biological evaluation of novel pyrazole amides as potent mitochondrial complex I inhibitors	48
Synthesis and evaluation of a new class of MIF-inhibitors in activated macrophage cells and in experimental septic shock in mice	48
Synthesis and antibacterial medicinal evaluation of carbothioamido hydrazonyl thiazolylquinolone with multitargeting antimicrobial potential to combat increasingly global resistance	48
Applications of oxetanes in drug discovery and medicinal chemistry	48
Graphical abstract TOC	47
Highly potent dipeptidyl peptidase 8/9 (DPP8/9) inhibitors designed via relative binding free energy calculations	47
Graphical abstract TOC	46
Benzimidazole analogues active against adult Schistosoma mansoni: SAR analyses, In vivo efficacy in mice, and preliminary mechanistic studies as potential inhibitors of hemozoin formation	46
Novel angiogenesis inhibitors with superoxide anion radical amplification effect: Surmounting the Achilles’ heels of angiogenesis inhibitors and photosensitizers	46
Recent advances on the development of NO-releasing molecules (NORMs) for biomedical applications	46
Editorial Board	46
Development of a next-generation endogenous OCT4 inducer and its anti-aging effect in vivo	46
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 pathway	46
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 neuroprotection	46
An overview on Estrogen receptors signaling and its ligands in breast cancer	45
Development of novel S-N3-DABO derivatives as potent non-nucleoside reverse transcriptase inhibitors with improved potency and selectivity	45
Antibody-drug conjugates for targeted cancer therapy: Recent advances in potential payloads	45
Assessing the anti-leukemic efficacy of a curcuminoid in cellular and animal models	44
Structure-based discovery of potent USP28 inhibitors derived from Vismodegib	44
Synthesis of 10,10′-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro	44
Discovery of 4-(N-dithiobenzyl piperazine)-1,8-naphthalimide as a potent multi-target antitumor agent with good efficacy, limited toxicity, and low resistance	44
Rational design of next-generation FLT3 inhibitors in acute myeloid leukemia: From laboratory to clinics	44
Graphical abstract TOC	44
Synthesis and evaluation of chemical linchpins for highly selective CK2α targeting	44
Novel dual-target FAAH and TRPV1 ligands as potential pharmacotherapeutics for pain management	44
Ketoconazole-carbonic anhydrase inhibitors as potential anticancer agents	44
Hydrazinecarboxamides: Comprehensive review of their anticancer, anticonvulsive, anti-inflammatory, enzyme inhibition, antioxidant and other activities	44
Novel boron-modified aza-BODIPY photosensitizers for low-dose light-dependent anti-cancer photodynamic therapy	44
Structure-activity relationship studies and design of a PTPN22 inhibitor with enhanced isozyme selectivity and cellular efficacy	44
New broad-spectrum and potent antibacterial agents with dual-targeting mechanism: Promoting FtsZ polymerization and disrupting bacterial membranes	44
Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models	43
Antimicrobial activity of natural and semi-synthetic carbazole alkaloids	43
Amphiphilic small molecule antimicrobials: From cationic antimicrobial peptides (CAMPs) to mechanism-related, structurally-diverse antimicrobials	43
Structure-guided expansion strategy unveils potent allosteric SHP2 inhibitors with synergistic efficacy against AML through MCL-1 co-targeting	43
Targeted vancomycin delivery via in situ albumin conjugation and acid-triggered drug release for reduced nephrotoxicity	43
A deep learning model for structure-based bioactivity optimization and its application in the bioactivity optimization of a SARS-CoV-2 main protease inhibitor	43
Expanding the antiviral arsenal: N-arylated 1,2,4-oxadiazol-5(4H)-ones show high activity against orthopoxviruses	43
Research and development of natural product Salidroside: Pharmacology, total synthesis and structural modifications	43
Mitochondrial targeted hierarchical drug delivery system based on HA-modified liposomes for cancer therapy	43
3-Hydroxy-pyridin-4(1H)-ones as siderophores mediated delivery of isobavachalcone enhances antibacterial activity against pathogenic Pseudomonas aeruginosa	42
SAR and lead optimization of (Z)-5-(4-hydroxy-3-methoxybenzylidene)-3-(2-morpholinoacetyl)thiazolidine-2,4-dione as a potential multi-target antidiabetic agent	42
Graphical abstract TOC	42
Nonsteroidal anti-inflammatory drugs (NSAIDs) and nucleotide analog GS-441524 conjugates with potent in vivo efficacy against coronaviruses	42
Contents continued	42
Targeting p53 activation: Recent therapeutic advances in cancer and diabetic macular edema	41
Immunosuppressive effects of new thiophene-based KV1.3 inhibitors	41
Discovery, enantioselective synthesis of myrtucommulone E analogues as tyrosyl-DNA phosphodiesterase 2 inhibitors and their biological activities	41
Inhibitors of ABCG2-mediated multidrug resistance: Lead generation through computer-aided drug design	41
Design, synthesis, and biological activity evaluation of novel HDAC3 selective inhibitors for combination with Venetoclax against acute myeloid leukemia	41
Synthesis and evaluation of small molecule inhibitors of LSD1 for use against MYCN-expressing neuroblastoma	40
Microbial-derived peptides with anti-mycobacterial potential	40
The journey of p38 MAP kinase inhibitors: From bench to bedside in treating inflammatory diseases	40
Design and synthesis of new 1,2,3-triazoles derived from eugenol and analogues with in vitro and in vivo activity against Trypanosoma cruzi	40
Design, synthesis, in vitro – In vivo biological evaluation of novel thiazolopyrimidine compounds as antileishmanial agent with PTR1 inhibition	40
Structure-directed identification of pyridine-2-methylamine derivatives as MmpL3 inhibitors for use as antitubercular agents	40
Structure-based development of potent Plasmodium falciparum M1 and M17 aminopeptidase selective and dual inhibitors via S1′-region optimisation	40

Discovery of indolinone-based covalent ULK1 inhibitors that suppressed autophagy and induced apoptosis against colorectal carcinoma	40
Discovery of novel hybrids containing clioquinol−1-benzyl-1,2,3,6-tetrahydropyridine as multi-target-directed ligands (MTDLs) against Alzheimer's disease	40
Reversal of subtype-selectivity and function by the introduction of a para-benzamidyl substituent to N-cyclopropylmethyl nornepenthone	39
Natural alkaloids with therapeutic potential against Alzheimer's disease through cholinesterase inhibition	39
Advancing Src kinase inhibition: From structural design to therapeutic innovation - A comprehensive review	39
The novel SIRT2-targeted PROTAC degraders as the efficient agents for the treatment of ovarian cancer	39
Promises of anionic calix[n]arenes in life science: State of the art in 2023	39
Novel neuroprotective 5,6-dihydropyrido[2′,1':2,3]imidazo[4,5-c]quinoline derivatives acting through cholinesterase inhibition and CB2 signaling modulation	39
The roles of fused-cyclopropanes in medicinal chemistry: Insights from the past decade	39
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 n	39
Progress of NIR-II fluorescence imaging technology applied to disease diagnosis and treatment	39
Recent progress toward developing axial chirality bioactive compounds	39
Synthesis, design, and optimization of a potent and selective series of pyridylpiperazines as promising antimalarial agents	39
Discovery and optimization of isoliquiritigenin as a death-associated protein kinase 1 inhibitor	38
Recent advances in triazoles as tyrosinase inhibitors	38
Design and synthesis of harmiquins, harmine and chloroquine hybrids as potent antiplasmodial agents	38
Fenbendazole–amino acid derivatives as novel anthelmintic candidates: Synthesis, activity against Haemonchus contortus, and in silico profiling	38
Synthetic α-glucosidase inhibitory peptides designed by molecular docking: In vitro screening and anti-hyperglycemic efficacy in diabetic mice	38
Development of fibroblast activation protein-α radiopharmaceuticals: Recent advances and perspectives	38
O-derivatization of natural tropolone and β-thujaplicin leading to effective inhibitors of human carbonic anhydrases IX and XII	38
Accelerated de novo design of xanthine oxidase-inhibitory peptides via physics-informed computational approaches	38
Design, development and evaluation of a prodrug-type TrkA-selective inhibitor with antinociceptive effects in vivo	37
Recent developments in antimalarial activities of 4-aminoquinoline derivatives	37
Synthesis and application of small molecules approved for the treatment of lymphoma	37
Design, synthesis and evaluation of novel oxadiazole-based compounds as potential Rac1 inhibitors against breast cancer	37
Design, synthesis, and antitumor evaluation of triazolopyridine derivatives as novel inhibitors for BRD4	37
Briarane-type diterpenoids, the inhibitors of osteoclast formation by interrupting Keap1-Nrf2 interaction and activating Nrf2 pathway	37
Design, synthesis and anticancer evaluation of novel Se-NSAID hybrid molecules: Identification of a Se-indomethacin analog as a potential therapeutic for breast cancer	37
Exploring the potential of histone demethylase inhibition in multi-therapeutic approaches for cancer treatment	37
2-Phenoxy-3, 4′-bipyridine derivatives inhibit AURKB-dependent mitotic processes by disrupting its localization	37
Synthesis and biological evaluation of C-28-modified pyrazole-fused betulinic acid derivatives as potent antiosteoporosis agents	37
Synthesis of amide-linked panaxadiol-indolinedione derivatives: A novel NSD2/H3K36me2 epigenetic modulator with significant antitumor efficacy	37
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 of	37
Bioisosteric replacement of 1H-1,2,3-triazole with 1H-tetrazole ring enhances anti-leukemic activity of (5-benzylthiazol-2-yl)benzamides	37
Design, synthesis, and biological evaluation of diphenyl ether substituted quinazolin-4-amine derivatives as potent EGFRL858R/T790M/C797S inhibitors	37
Novel antimalarial 3-substituted quinolones isosteres with improved pharmacokinetic properties	37
Design and synthesis of novel cyclin-dependent kinase 4/6(CDK4/6) and histone deacetylase (HDAC) dual inhibitors: In vitro and in vivo anticancer activity	37
Corrigendum to “Discovery of novel tetrahydroquinoline derivatives as potent, selective, and orally Available AR antagonists” [Eur. J. Med. Chem. 291 (2025) 117566]	36
Discovery of novel diaryl substituted isoquinolin-1(2H)-one derivatives as hypoxia-inducible factor-1 signaling inhibitors for the treatment of rheumatoid arthritis	36
Discovery of novel triazine derivatives as potent retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists	36
Monofunctional dimetallic Ru(η6-arene) complexes inhibit NOTCH1 signaling pathway and synergistically enhance anticancer effect in combination with cisplatin or vitamin C	36
N-acylated aminoguanidine-benzenesulfonamides: rational design, synthesis, and dual apoptotic mechanisms of anticancer activity involving VEGFR-2 inhibition and VEGFR-2–independent pathways	36
Mucormycosis: A hidden mystery of fungal infection, possible diagnosis, treatment and development of new therapeutic agents	36
Synthesis and biological evaluation of tyrosine derivatives as peripheral 5HT2A receptor antagonists for nonalcoholic fatty liver disease	36
Synthesis and evaluation of novel ebselen derivatives as urease inhibitors for combating Helicobacter pylori infections	36
Design, synthesis and biological evaluation of new parbendazole derivatives for the treatment of HNSCC	36
Discovery of a novel dual-target inhibitor of CDK12 and PARP1 that induces synthetic lethality for treatment of triple-negative breast cancer	35
Rational design and appraisal of selective Cdc2-Like kinase 1 (Clk1) inhibitors as novel autophagy inducers for the treatment of acute liver injury (ALI)	35
Discovery of antileishmanial hits in the 3-nitroimidazo[1,2-a]pyridine series via newly optimized tetrakis(dimethylamino)ethylene (TDAE) methodology at position 2	35
Contents continued	35
Graphical abstract TOC	35
Design, synthesis and activity evaluation of benzene sulfonamide derivatives as novel androgen receptor antagonist	35
From garden to lab: C-3 chemical modifications of tomatidine unveil broad-spectrum ATP synthase inhibitors to combat bacterial resistance	35
Macrocyclic-based strategy in drug design: From lab to the clinic	35
Integration of computational and experimental techniques for the discovery of PLpro covalent inhibitors. When large virtual screening and rational design meet	35
Multicomponent syntheses enable the discovery of novel quisinostat-derived chemotypes as histone deacetylase inhibitors	35
Graphical abstract TOC	35
Design, synthesis and biological evaluation of conformationnally-restricted analogues of E7010 as inhibitors of tubulin assembly (ITA) and vascular disrupting agents (VDA)	35
Covalent fragment mapping of KRasG12C revealed novel chemotypes with in vivo potency	35
Anti-cancer efficacy of novel lonidamine derivatives: Design, synthesis, in vitro, in vivo, and computational studies targeting hexokinase-2	35
Aporphines: A privileged scaffold in CNS drug discovery	35
Synthesis and evaluation of N-sulfonylpiperidine-3-carboxamide derivatives as capsid assembly modulators inhibiting HBV in vitro and in HBV-transgenic mice	35
Graphical abstract TOC	35
Small molecular inhibitors targeting Janus kinases (JAKs) for the treatment of psoriasis	35
The application prospects of amino acid deprivation for cancer therapy	35
How generative Artificial Intelligence can transform drug discovery?	34
Mechanistic analysis of diverse click reactions along with their applications	34
Design, synthesis, and biological evaluation of novel 7-substituted 10,11-methylenedioxy-camptothecin derivatives against drug-resistant small-cell lung cancer in vitro and in vivo	34
New antitubercular pretomanid analogues as potent payloads in polymeric micelles: Leveraging zebrafish assays to accelerate lead optimisation	34
Novel dihydropyrimidines as promising EGFR & HER2 inhibitors: Insights from experimental and computational studies	34
Sensitive quantification of fibroblast activation protein and high-throughput screening for inhibition by FDA-approved compounds	34
Synthesis and structure-activity relationships of novel 14-membered 2-fluoro ketolides with structural modification at the C11 position	34
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 mice	34
Discovery of potent and selective c-Met inhibitors for MET-amplified hepatocellular carcinoma treatment	34
Design, synthesis, and evaluation of novel matrine derivatives as topoisomerase I inhibitors for anticancer agents	33
Plant-derived strategies to fight against severe acute respiratory syndrome coronavirus 2	33
Editorial Board	33
Acyclic purine and pyrimidine nucleotide analogs as ecto-5′-nucleotidase (CD73) inhibitors	33
SILAC-based chemoproteomics reveals a neoligan analogue as an anti-inflammatory agent targeting IRGM to ameliorate cytokine storm	33
Structure-based discovery of potent myosin inhibitors to guide antiparasite drug development	33
Design, synthesis and biological evaluation of biaryl amide derivatives against SARS-CoV-2 with dual-target mechanism	33
Graphical abstract TOC	33
Editorial Board	33
2-(Phenylamino)-7,8-dihydroquinazolin-5(6H)-one, a promising scaffold for MAO-B inhibitors with potential GSK3β targeting	33
The antibacterial properties of branched peptides based on poly(l-arginine): In vitro antibacterial evaluation and molecular dynamic simulations	33
Graphical abstract TOC	33
Expanding the utilization of binding pockets proves to be effective for noncovalent small molecule inhibitors against SARS-CoV-2 Mpro	33
Carbamoylation at C-8 position of natural 3-arylcoumarin scaffold for the discovery of novel PARP-1 inhibitors with potent anticancer activity	32
Design, synthesis and biological evaluation of novel FXIa inhibitors featuring five-membered heterocycles as P2’ fragments	32
Comprehensive coverage on anti-mycobacterial endeavour reported during 2022	32
Design, synthesis and anti-ovarian cancer activities of thieno[2,3-d]pyrimidine based chimeric BRD4 inhibitor/nitric oxide-donator	32
Identification and immunological evaluation of novel TLR2 agonists through structural optimization of Diprovocim	32
Quaternary ammonium cations conjugated 5,15-diaryltetranaphtho[2,3]porphyrins as photosensitizers for photodynamic therapy	32
PITB: A high affinity transthyretin aggregation inhibitor with optimal pharmacokinetic properties	32
Designed and synthesized novel tripeptides targeting diabetes and its related pathologies	32