OOIR: Observatory of International Research

Papers

(The TQCC of Journal of Enzyme Inhibition and Medicinal Chemistry is 12. 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 2022-08-01 to 2026-08-01.)

Article	Citations
Different chemical proteomic approaches to identify the targets of lapatinib	85
Design, synthesis, and evaluation of 1, 3-dioxo- N- phenylisoindoline-5-carboxamide derivatives as potent reversible inhibitors of human monoamine oxidas	81
Discovery of 2-phenylethyl chromones as potent and selective CYP1B1 inhibitors	80
Design, synthesis and antitumor evaluation of novel pyrazolo[3,4- d ]pyrimidines incorporating different amino acid conjugates as potential DHFR inhibito	74
Design, synthesis, and biological evaluation of potent FAK-degrading PROTACs	72
Recent progress in chemistry and bioactivity of monoterpenoid indole alkaloids from the genus gelsemium : a comprehensive review	67
Novel harmine derivatives as potent acetylcholinesterase and amyloid beta aggregation dual inhibitors for management of Alzheimer’s disease	62
Natural product sennoside B disrupts liquid-liquid phase separation of SARS-CoV-2 nucleocapsid protein by inhibiting its RNA-binding activity	59
Towards safer anti-inflammatory therapy: synthesis of new thymol–pyrazole hybrids as dual COX-2/5-LOX inhibitors	52
4-Cyanamidobenzenesulfonamide derivatives: a novel class of human and bacterial carbonic anhydrase inhibitors	52
Myeloperoxidase as a therapeutic target for oxidative damage in Alzheimer’s disease	51
Synthesis, DFT calculations, and anti-proliferative evaluation of pyrimidine and selenadiazolopyrimidine derivatives as dual Topoisomerase II and HSP90 inhibitors	51
Development of eugenol derivatives with 5-LOX inhibitory activity	49
Recombinant ferritins for multimodal nanomedicine	49
Development of new thiazolidine-2,4-dione hybrids as aldose reductase inhibitors endowed with antihyperglycaemic activity: design, synthesis, biological investigations, and in s	48
Development of novel 9- O -substituted-13-octylberberine derivatives as potential anti-hepatocellular carcinoma agents	47
Molecular screening of natural compounds targeting KRAS(G12C): a multi-parametric strategy against acute lymphoblastic leukemia	46
Identification of a peptide inhibitor disrupting the PCSK9-LDLR interaction via pharmacophore-based virtual screening, molecular dynamics simulations and	45
Identification of novel potent peptide inhibitors targeting the polo-box domain of PLK1: structure-based pharmacophore modelling, virtual screening, molecular docking, molecular dynamics study and bio	44
Investigation of the enantioselectivity of acetylcholinesterase and butyrylcholinesterase upon inhibition by tacrine-iminosugar heterodimers	44
Antifungal and anti-biofilm effects of hydrazone derivatives on Candida spp	43
2,5-Dihydroxyphenylethanone: an anti-melanogenic bioactive compound isolated from Ganoderma cochlear	43
Discovery of a selective PI3Kα inhibitor via structure-based virtual screening for targeted colorectal cancer therapy	43
Radioiodinated compound FJR01: a novel P2X7R-targeted SPECT tracer for visualizing glioma-associated microglia/macrophages in a rat glioblastoma model	41
The key enzyme PYCR1 in proline metabolism: a dual driver of cancer progression and fibrotic remodeling	40

Promising inhibition of diabetes-related enzymes and antioxidant properties of Ptilostemon casabonae leaves extract	40
Structure-based design of new potent and highly selective PARP-1 inhibitor for treating colorectal cancer	39
Targeting the glutamine-arginine-proline metabolism axis in cancer	38
Development of potent and effective SARS-CoV-2 main protease inhibitors based on maleimide analogs for the potential treatment of COVID-19	37
Integrating virtual screening and molecular dynamics simulations to identify emodin as a PYCR1 inhibitor modulating docetaxel sensitivity in prostate cancer	37
Synthesis and structure–activity relationships for some novel diflapolin derivatives with benzimidazole subunit	37
3 H -1,2-Benzoxaphosphepine 2-oxides as selective inhibitors of carbonic anhydrase IX and XII	36
Development of ketobenzothiazole-based peptidomimetic TMPRSS13 inhibitors with low nanomolar potency	36
New imidazole-2-thiones linked to acenaphythylenone as dual DNA intercalators and topoisomerase II inhibitors: structural optimization, docking, and apoptosis studies	34
Design, synthesis, docking, and anticancer evaluations of new thiazolo[3,2- a ] pyrimidines as topoisomerase II inhibitors	33
Design and synthesis of 1,4,8-triazaspiro[4.5]decan-2-one derivatives as novel mitochondrial permeability transition pore inhibitors	33
Identification of sulphonamide-tethered N -((triazol-4-yl)methyl)isatin derivatives as inhibitors of SARS-CoV-2 main protease	33
Fragment-based design, synthesis and biological evaluation of theophylline derivatives as ATAD2 inhibitors in BT-549 cells	32
Identification of new benzimidazole-triazole hybrids as anticancer agents: multi-target recognition, in vitro and in silico	32
Synthesis of novel pyrazole derivatives and neuroprotective effect investigation	32
Anti-obesity carbonic anhydrase inhibitors: challenges and opportunities	32
o-Vanillin binds covalently to MAL/TIRAP Lys-210 but independently inhibits TLR2	31
Selisistat, a SIRT1 inhibitor, enhances paclitaxel activity in luminal and triple-negative breast cancer: in silico, in vitro, and in vivo studies	31
Crystal structure of ricin toxin A chain complexed with a highly potent pterin-based small-molecular inhibitor	29
Antiglycoxidative properties of amantadine – a systematic review and comprehensive in vitro study	29
1,2,3-Benzoxathiazine-2,2-dioxides – effective inhibitors of human carbonic anhydrases	29
Probing mutation-induced conformational transformation of the GTP/M-RAS complex through Gaussian accelerated molecular dynamics simulations	29
Searching for novel MDM2/MDMX dual inhibitors through a drug repurposing approach	29
PD-L1 dimerisation induced by biphenyl derivatives mediates anti-breast cancer activity via the non-immune PD-L1–AKT–mTOR/Bcl2 pathway	28
Design, synthesis, apoptotic, and antiproliferative effects of 5-chloro-3- (2-methoxyvinyl)-indole-2-carboxamides and pyrido[3,4-b]indol-1-ones as potent EGFR ^WT/	28
Discovery of novel polysubstituted N -alkyl acridone analogues as histone deacetylase isoform-selective inhibitors for cancer therapy	28
Recent progress in discovery of novel AAK1 inhibitors: from pain therapy to potential anti-viral agents	27
Structural isomerisation affects the antitubercular activity of adamantyl-isoxyl adducts	27
Structural comparison of substrate-binding pockets of serine β-lactamases in classes A, C, and D	27
Challenging the Biginelli scaffold to surpass the first line antitubercular drugs: Mycobacterium tuberculosis thymidine monophosphate kinase (TMPK mt	27
Discovery of benzochromene derivatives first example with dual cytotoxic activity against the resistant cancer cell MCF-7/ADR and inhibitory effect of the P	26
Design and synthesis of some new benzoylthioureido benzenesulfonamide derivatives and their analogues as carbonic anhydrase inhibitors	26
Statement of Retraction: Dihydroartemisinin enhances the anti-tumor effect of photodynamic therapy by targeting PKM2-mediated glycolysis in esophageal cancer cell	26
Cadmium inhibits hSMUG1-mediated uracil excision: quantitative analysis and mitigation by Ganoderma lucidum extracts	26
Unveiling the mechanism of action of acylated temporin L analogues against multidrug-resistant Candida albicans	26
From bench to brain: novel thieno-oxazine hybrids as potent pleiotropic anti-Alzheimer’s agents with in vivo / in vitro	24
Arctigenin: pharmacology, total synthesis, and progress in structure modification	24
Investigation of exercise-mimetic bioactive molecules as modulators of MMP activity and expression in cancer cells	23
Fluorinated indeno-quinoxaline bearing thiazole moieties as hypoglycaemic agents targeting α -amylase, and α -glucosidase: synthesis, mole	23
Discovery and characterization of novel hematopoietic prostaglandin D synthase inhibitors from traditional Chinese medicine: the bioactive potential of dihydroberberine in treatments of Duchenne muscu	23
Discovery of an effective anti-inflammatory agent for inhibiting the activation of NF-κB	23
Design, synthesis, and study of novel phenethyl-based antitumor phospholipids downregulating p38 mitogen-activated protein kinase	23
Identification of putative allosteric inhibitors of BCKDK via virtual screening and biological evaluation	22
Development of novel anilinoquinazoline-based carboxylic acids as non-classical carbonic anhydrase IX and XII inhibitors	22
Trichodermin exhibits potent anti-glioblastoma activity by inducing cell cycle arrest and apoptosis, suppressing invasion, and enhancing temozolomide efficacy	22
Exploring covalent inhibitors of SARS-CoV-2 main protease: from peptidomimetics to novel scaffolds	22
Discovery of selective ACAT2 antagonist via a combination strategy based on deep docking, pharmacophore modelling, and molecular dynamics simulation	22
Design, synthesis, molecular modelling and antitumor evaluation of S -glucosylated rhodanines through topo II inhibition and DNA intercalation	22
Enzyme sequence optimisation via Gromov-Wasserstein Autoencoders integrating MSA techniques	21
Design and synthesis of novel HDAC6 inhibitor dimer as HDAC6 degrader for cancer treatment by palladium catalysed dimerisation	21

Design, synthesis, and bioevaluation of 1 h -pyrrolo[3,2- c ]pyridine derivatives as colchicine-binding site inhibitors with potent antica	21
Design, synthesis, anti-inflammatory evaluation, and molecular modelling of new coumarin-based analogs combined curcumin and other heterocycles as potential TNF-α production inhibitors	21
Design, synthesis and biological evaluation of novel urolithin derivatives targeting liver cancer cells	21
Farnesiferol C enhances the effects of chemotherapy and ionising radiation in human melanoma cells via targeting topoisomerase II alpha	21
Purification and characterisation of glutathione reductase from scorpionfish (scorpaena porcus) and investigation of heavy metal ions inhibition	21
Fourth-generation EGFR-TKI to overcome C797S mutation: past, present, and future	21
Insights into the inhibitory activities of neolignans and diarylnonanoid derivatives from nutmeg ( Myristica fragrans Houtt.) seeds on soluble epoxide hy	21
Discovery of a novel PLK1 inhibitor with high inhibitory potency using a combined virtual screening strategy	21
Investigation of novel alkyl/benzyl (4-sulphamoylphenyl)carbamimidothioates as carbonic anhydrase inhibitors	21
Design, synthesis and biological evaluation of novel diarylpyridine derivatives as tubulin polymerisation inhibitors	20
Design, synthesis and antitumor activity of 5-trifluoromethylpyrimidine derivatives as EGFR inhibitors	20
Identification of the first peptide inhibitor of UBE2C enzymatic activity: insights from metadynamics-guided folding and binding studies	20
Synthesis and biological evaluation of ortho -phenyl phenylhydroxamic acids containing phenothiazine with improved selectivity for class IIa histone deacetylases	20
Synthesis, biological evaluation, and computational studies of N -benzyl pyridinium–curcumin derivatives as potent AChE inhibitors with antioxidant activ	20
The importance of including the C-terminal domain of PTP1B _1-400 to identify potential antidiabetic inhibitors	20
Green ultrasound‑assisted deep eutectic solvent extraction of flavonoid enzyme inhibitors from Blumea aromatica : process optimization, characterization,	19
In vitro screening of compounds for targeting gastric cancer with Y220C p53 mutation: a molecule combining zinc chelation and a Michael acceptor drives <	18
Discovery of azaindole/indole-fused pyrimidine tetracyclic scaffolds as novel potent CDK7 inhibitors	18
Design, synthesis, and bioevaluation of pyrazole-containing tubulin polymerisation inhibitors based on conformational constraint strategy	18
Design, synthesis, biological evaluation and molecular docking study of 2,4-diarylimidazoles and 2,4-bis(benzyloxy)-5-arylpyrimidines as novel HSP90 N-terminal inhibitors	18
Druggable cavities and allosteric modulators of the cell division cycle 7 (CDC7) kinase	18
The mechanism and pharmacodynamics of 2-((1H-indol-3-yl)thio/sulfinyl)-N-pheny acetamide derivative as a novel inhibitor against human respiratory syncytial virus	18
Targeting RIPK1 to modulate cell death and tumour microenvironment in cancer therapy	17
Novel benzo chromene derivatives: design, synthesis, molecular docking, cell cycle arrest, and apoptosis induction in human acute myeloid leukemia HL-60 cells	17
Discovery of lignans as the effective inhibitors of CES1A alleviate lipid droplets formation	17
Prospecting in silico antibacterial activity of a peptide from trypsin inhibitor isolated from tamarind seed	17
Discovery of novel biphenyl compounds bearing hydroxamic acid moiety as the first PD-L1/class I HDACs dual inhibitors	17
Dentine biomodification by sulphonamides pre-treatment: bond strength, proteolytic inhibition, and antimicrobial activity	16
Discovering a novel dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A) inhibitor and its impact on tau phosphorylation and amyloid-β formation	16
Peptide foldamer-based inhibitors of the SARS-CoV-2 S protein–human ACE2 interaction	16
A comprehensive review of small molecule drugs approved by the FDA in 2025: advance and prospect	16
Mixed and non-competitive enzyme inhibition: underlying mechanisms and mechanistic irrelevance of the formal two-site model	16
Identification of potential inhibitors against Staphylococcus aureus shikimate dehydrogenase through virtual screening and susceptibility test	16
PROTACs in cancer therapy: targeted degradation of GPX4, PARP and epigenetic regulators	15
Latest advances in dual inhibitors of acetylcholinesterase and monoamine oxidase B against Alzheimer’s disease	15
Expression of Concern	15
Discovery of new 1 H -pyrazolo[3,4- d ]pyrimidine derivatives as anticancer agents targeting EGFR	15
Effect of trypsin inhibitor isolated from tamarind seed (TTI) on caenorhabditis elegans survival under bacterial infection	15
Correction	15
Inhibition of prolyl-tRNA synthetase and efflux pumps as a dual-targeting strategy against multidrug-resistant bacteria	15
Design, synthesis and evaluation of novel small molecules acting as Keap1-Nrf2 protein-protein interaction inhibitors	15
Palladium-catalysed synthesis of small-molecule epigenetic inhibitors as anticancer therapeutics	14
Phytochemical constituents of Hydrangea macrophylla var. acuminata leaves and their inhibitory activity ag	14
Synthesis and evaluation of 5, 6-dihydro-8 H -isoquinolino[1, 2- b ]quinazolin-8-one derivatives as novel	14
Synthesis and antitumor activity of litseaone B analogues as tubulin polymerisation inhibitors	14
Design and synthesis of new spirooxindole candidates and their selenium nanoparticles as potential dual Topo I/II inhibitors, DNA intercalators, and apoptotic inducers	14
Design, synthesis and anti-breast cancer activity evaluation of 6,7-dihydro-5 H -pyrrolo[3,4- d ]pyrimidin	14
3-aryl-4-(3,4,5-trimethoxyphenyl)pyridines inhibit tubulin polymerisation and act as anticancer agents	14
Structure-activity exploration of a small-molecule allosteric inhibitor of T790M/L858R double mutant EGFR	14
Effect of hydrophobic extension of aryl enaminones and pyrazole-linked compounds combined with sulphonamide, sulfaguanidine, or carboxylic acid functionalities on carbonic anhydrase inhibitory potency	13
Rational repurposing, synthesis, in vitro and in silico studies of chromone-peptidyl hybrids as potential	13
Discovery of new pyridine-quinoline hybrids as competitive and non-competitive PIM-1 kinase inhibitors with apoptosis induction and caspase 3/7 activation capabilities	13
LDH isozymes as targets for cancer therapy	13
Chemical composition, antioxidant activities, and enzyme inhibitory effects of Lespedeza bicolour Turcz. essential oil	13
Novel N -methylsulfonyl-indole derivatives: biological activity and COX-2/5-LOX inhibitory effect with improved gastro protective profile and reduced car	13
New 1,2,3-triazole/1,2,4-triazole hybrids linked to oxime moiety as nitric oxide donor selective COX-2, aromatase, B-RAF ^V600E and EGFR inhibitors ce	13
Design, synthesis and evaluation of quinoline- O -carbamate derivatives as multifunctional agents for the treatment of Alzheimer’s disease	13
Design, synthesis, biological evaluation and molecular docking study of novel pleuromutilin derivatives containing substituted benzoxazole as antibacterial agents	13
Discovery and development of steroidal enzyme inhibitors as anti-cancer drugs: state-of-the-art and future perspectives	13
Selective targeting phosphodiesterase-5 (PDE5): clinical progress, design strategies, and emerging prospects	13
Correction	12
Pyridine indole hybrids as novel potent CYP17A1 inhibitors	12
Design, synthesis and biological evaluation of 4-aminoquinoline derivatives as receptor-interacting protein kinase 2 (RIPK2) inhibitors	12
Selected strategies to fight pathogenic bacteria	12
Statement of Retraction: Dependence on linkers’ flexibility designed for benzenesulfonamides targeting discovery of novel hCA IX inhibitors as potent anticancer agents	12
Ferroptosis and hearing loss: from molecular mechanisms to therapeutic interventions	12
Design, synthesis, and evaluation of cyclic C7-bridged monocarbonyl curcumin analogs containing an o -methoxy phenyl group as potential agents against gastric cancer	12
Discovery of novel 2-aminopyridine derivatives as ROS1 and ALK dual inhibitors to combat drug-resistant mutants including ROS1 ^G2032R and ALK	12
Study on the synthesis and biological activity of kojic acid triazol thiosemicarbazide Schiff base derivatives	12
Activation studies with amino acids and amines of a β-carbonic anhydrase from Mammaliicoccus (Staphylococcus) sciuri previously annotated as	12
Evaluation of the anticancer effects exerted by 5-fluorouracil and heme oxygenase-1 inhibitor hybrids in HTC116 colorectal cancer cells	12