OOIR: Observatory of International Research

Papers

(The TQCC of Journal of Enzyme Inhibition and Medicinal Chemistry is 15. 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 2022-01-01 to 2026-01-01.)

Article	Citations
4-Cyanamidobenzenesulfonamide derivatives: a novel class of human and bacterial carbonic anhydrase inhibitors	195
Recombinant ferritins for multimodal nanomedicine	93
Different chemical proteomic approaches to identify the targets of lapatinib	81
Development of new thiazolidine-2,4-dione hybrids as aldose reductase inhibitors endowed with antihyperglycaemic activity: design, synthesis, biological investigations, and in s	73
Design, synthesis, and evaluation of 1, 3-dioxo- N- phenylisoindoline-5-carboxamide derivatives as potent reversible inhibitors of human monoamine oxidas	66
Development of eugenol derivatives with 5-LOX inhibitory activity	60
Synthesis, DFT calculations, and anti-proliferative evaluation of pyrimidine and selenadiazolopyrimidine derivatives as dual Topoisomerase II and HSP90 inhibitors	60
Recent progress in chemistry and bioactivity of monoterpenoid indole alkaloids from the genus gelsemium : a comprehensive review	59
Towards safer anti-inflammatory therapy: synthesis of new thymol–pyrazole hybrids as dual COX-2/5-LOX inhibitors	59
Identification of novel non-toxic and anti-angiogenic α-fluorinated chalcones as potent colchicine binding site inhibitors	58
Synthesis, biological evaluation, and in silico studies of new CDK2 inhibitors based on pyrazolo[3,4- d ]p	58
Discovery and SAR analysis of phenylbenzo[d][1,3]dioxole-based proprotein convertase subtilisin/kexin type 9 inhibitors	58
Design, synthesis, and molecular docking studies of novel pomalidomide-based PROTACs as potential anti-cancer agents targeting EGFR ^WT and EGFR	57
Diversely substituted sulfamides for fragment-based drug discovery of carbonic anhydrase inhibitors: synthesis and inhibitory profile	54
Design, synthesis, and biological evaluation of potent FAK-degrading PROTACs	53
Design, synthesis and antitumor evaluation of novel pyrazolo[3,4- d ]pyrimidines incorporating different amino acid conjugates as potential DHFR inhibito	52
Novel harmine derivatives as potent acetylcholinesterase and amyloid beta aggregation dual inhibitors for management of Alzheimer’s disease	50
Natural product sennoside B disrupts liquid-liquid phase separation of SARS-CoV-2 nucleocapsid protein by inhibiting its RNA-binding activity	48
Antifungal and anti-biofilm effects of hydrazone derivatives on Candida spp	45
Myeloperoxidase as a therapeutic target for oxidative damage in Alzheimer’s disease	45
Discovery of a selective PI3Kα inhibitor via structure-based virtual screening for targeted colorectal cancer therapy	45
Targeting the glutamine-arginine-proline metabolism axis in cancer	44
Synthesis, molecular modelling and QSAR study of new N- phenylacetamide-2-oxoindole benzensulfonamide conjugates as carbonic anhydrase inhibitors with an	43
Development of novel 9- O -substituted-13-octylberberine derivatives as potential anti-hepatocellular carcinoma agents	43
From Antarctica to cancer research: a novel human DNA topoisomerase 1B inhibitor from Antarctic sponge Dendrilla antarctica	42

Investigation of the enantioselectivity of acetylcholinesterase and butyrylcholinesterase upon inhibition by tacrine-iminosugar heterodimers	41
Promising inhibition of diabetes-related enzymes and antioxidant properties of Ptilostemon casabonae leaves extract	41
Structure-based design of new potent and highly selective PARP-1 inhibitor for treating colorectal cancer	40
2,5-Dihydroxyphenylethanone: an anti-melanogenic bioactive compound isolated from Ganoderma cochlear	39
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	39
Molecular screening of natural compounds targeting KRAS(G12C): a multi-parametric strategy against acute lymphoblastic leukemia	38
Design, synthesis, docking, and anticancer evaluations of new thiazolo[3,2- a ] pyrimidines as topoisomerase II inhibitors	38
The key enzyme PYCR1 in proline metabolism: a dual driver of cancer progression and fibrotic remodeling	38
Selisistat, a SIRT1 inhibitor, enhances paclitaxel activity in luminal and triple-negative breast cancer: in silico, in vitro, and in vivo studies	38
3 H -1,2-Benzoxaphosphepine 2-oxides as selective inhibitors of carbonic anhydrase IX and XII	37
Development of ketobenzothiazole-based peptidomimetic TMPRSS13 inhibitors with low nanomolar potency	37
Fragment-based design, synthesis and biological evaluation of theophylline derivatives as ATAD2 inhibitors in BT-549 cells	37
Identification of sulphonamide-tethered N -((triazol-4-yl)methyl)isatin derivatives as inhibitors of SARS-CoV-2 main protease	37
Synthesis of novel pyrazole derivatives and neuroprotective effect investigation	37
GC-MS metabolites profiling of anethole-rich oils by different extraction techniques: antioxidant, cytotoxicity and in-silico enzymes inhibitory insights	36
Development of naringenin- O -alkylamine derivatives as multifunctional agents for the treatment of Alzheimer’s disease	36
Synthesis and structure–activity relationships for some novel diflapolin derivatives with benzimidazole subunit	35
Drug-like molecules with anti-trypanothione synthetase activity identified by high throughput screening	35
Identification of new benzimidazole-triazole hybrids as anticancer agents: multi-target recognition, in vitro and in silico	34
Development of potent and effective SARS-CoV-2 main protease inhibitors based on maleimide analogs for the potential treatment of COVID-19	33
Design and synthesis of 1,4,8-triazaspiro[4.5]decan-2-one derivatives as novel mitochondrial permeability transition pore inhibitors	33
o-Vanillin binds covalently to MAL/TIRAP Lys-210 but independently inhibits TLR2	32
Anti-obesity carbonic anhydrase inhibitors: challenges and opportunities	32
Searching for novel MDM2/MDMX dual inhibitors through a drug repurposing approach	32
New imidazole-2-thiones linked to acenaphythylenone as dual DNA intercalators and topoisomerase II inhibitors: structural optimization, docking, and apoptosis studies	32
Antiglycoxidative properties of amantadine – a systematic review and comprehensive in vitro study	31
1,2,3-Benzoxathiazine-2,2-dioxides – effective inhibitors of human carbonic anhydrases	31
Discovery of novel polysubstituted N -alkyl acridone analogues as histone deacetylase isoform-selective inhibitors for cancer therapy	31
PD-L1 dimerisation induced by biphenyl derivatives mediates anti-breast cancer activity via the non-immune PD-L1–AKT–mTOR/Bcl2 pathway	31
Crystal structure of ricin toxin A chain complexed with a highly potent pterin-based small-molecular inhibitor	31
Structural comparison of substrate-binding pockets of serine β-lactamases in classes A, C, and D	31
Structural isomerisation affects the antitubercular activity of adamantyl-isoxyl adducts	30
Unveiling the mechanism of action of acylated temporin L analogues against multidrug-resistant Candida albicans	30
Challenging the Biginelli scaffold to surpass the first line antitubercular drugs: Mycobacterium tuberculosis thymidine monophosphate kinase (TMPK mt	30
Design, synthesis, biological evaluation and QSAR analysis of novel N -substituted benzimidazole derived carboxamides	29
Probing mutation-induced conformational transformation of the GTP/M-RAS complex through Gaussian accelerated molecular dynamics simulations	29
Regioselective approach to colchiceine tropolone ring functionalization at C(9) and C(10) yielding new anticancer hybrid derivatives containing heterocyclic structural motifs	29
Statement of Retraction: Dihydroartemisinin enhances the anti-tumor effect of photodynamic therapy by targeting PKM2-mediated glycolysis in esophageal cancer cell	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 selective ACAT2 antagonist via a combination strategy based on deep docking, pharmacophore modelling, and molecular dynamics simulation	28
Selective inhibition of carbonic anhydrase IX by sulphonylated 1,2,3-triazole incorporated benzenesulphonamides capable of inducing apoptosis	28
Recent progress in discovery of novel AAK1 inhibitors: from pain therapy to potential anti-viral agents	28
Design, synthesis, and study of novel phenethyl-based antitumor phospholipids downregulating p38 mitogen-activated protein kinase	27
Design and synthesis of some new benzoylthioureido benzenesulfonamide derivatives and their analogues as carbonic anhydrase inhibitors	27
Identification of putative allosteric inhibitors of BCKDK via virtual screening and biological evaluation	27
Discovery and characterization of novel hematopoietic prostaglandin D synthase inhibitors from traditional Chinese medicine: the bioactive potential of dihydroberberine in treatments of Duchenne muscu	27
Discovery of an effective anti-inflammatory agent for inhibiting the activation of NF-κB	27
Development of novel anilinoquinazoline-based carboxylic acids as non-classical carbonic anhydrase IX and XII inhibitors	27
Design and biological evaluation of substituted 5,7-dihydro-6 H -indolo[2,3- c ]quinolin-6-one as novel se	26
Design, synthesis, molecular modelling and antitumor evaluation of S -glucosylated rhodanines through topo II inhibition and DNA intercalation	26

Arctigenin: pharmacology, total synthesis, and progress in structure modification	26
Coumarins inhibit η-class carbonic anhydrase from Plasmodium falciparum	26
Discovery of benzochromene derivatives first example with dual cytotoxic activity against the resistant cancer cell MCF-7/ADR and inhibitory effect of the P	25
Anti-breast cancer sinomenine derivatives via mechanisms of apoptosis induction and metastasis reduction	25
New 1,2,3-triazole linked ciprofloxacin-chalcones induce DNA damage by inhibiting human topoisomerase I& II and tubulin polymerization	25
Fluorinated indeno-quinoxaline bearing thiazole moieties as hypoglycaemic agents targeting α -amylase, and α -glucosidase: synthesis, mole	24
Exploring covalent inhibitors of SARS-CoV-2 main protease: from peptidomimetics to novel scaffolds	24
Investigation of novel alkyl/benzyl (4-sulphamoylphenyl)carbamimidothioates as carbonic anhydrase inhibitors	23
The importance of including the C-terminal domain of PTP1B _1-400 to identify potential antidiabetic inhibitors	23
Heterocycle-containing tranylcypromine derivatives endowed with high anti-LSD1 activity	23
Design, synthesis, and bioevaluation of 1 h -pyrrolo[3,2- c ]pyridine derivatives as colchicine-binding site inhibitors with potent antica	22
Discovery of a novel PLK1 inhibitor with high inhibitory potency using a combined virtual screening strategy	22
Thio- and selenosemicarbazones as antiprotozoal agents against Trypanosoma cruzi and Trichomonas vaginalis	22
Design and synthesis of novel HDAC6 inhibitor dimer as HDAC6 degrader for cancer treatment by palladium catalysed dimerisation	22
Design, synthesis and biological evaluation of novel urolithin derivatives targeting liver cancer cells	22
Fourth-generation EGFR-TKI to overcome C797S mutation: past, present, and future	22
Enzyme sequence optimisation via Gromov-Wasserstein Autoencoders integrating MSA techniques	22
Purification and characterisation of glutathione reductase from scorpionfish (scorpaena porcus) and investigation of heavy metal ions inhibition	22
Farnesiferol C enhances the effects of chemotherapy and ionising radiation in human melanoma cells via targeting topoisomerase II alpha	22
Discovery of novel paeonol-based derivatives against skin inflammation in vitro and in vivo	22
Novel benzo chromene derivatives: design, synthesis, molecular docking, cell cycle arrest, and apoptosis induction in human acute myeloid leukemia HL-60 cells	21
Discovering a novel dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A) inhibitor and its impact on tau phosphorylation and amyloid-β formation	21
Charged pyridinium oximes with thiocarboxamide moiety are equally or less effective reactivators of organophosphate-inhibited cholinesterases compared to analogous carboxamides	21
Design, synthesis, and bioevaluation of pyrazole-containing tubulin polymerisation inhibitors based on conformational constraint strategy	21
Druggable cavities and allosteric modulators of the cell division cycle 7 (CDC7) kinase	21
Insights into the inhibitory activities of neolignans and diarylnonanoid derivatives from nutmeg ( Myristica fragrans Houtt.) seeds on soluble epoxide hy	21
Prospecting in silico antibacterial activity of a peptide from trypsin inhibitor isolated from tamarind seed	21
Synthesis and biological evaluation of ortho -phenyl phenylhydroxamic acids containing phenothiazine with improved selectivity for class IIa histone deacetylases	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
Short divalent ethacrynic amides as pro-inhibitors of glutathione S -transferase isozyme Mu and potent sensitisers of cisplatin-resistant ovarian cancers	20
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
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	19
Targeting RIPK1 to modulate cell death and tumour microenvironment in cancer therapy	19
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	19
Green ultrasound‑assisted deep eutectic solvent extraction of flavonoid enzyme inhibitors from Blumea aromatica : process optimization, characterization,	19
Synthesis, biological evaluation, and computational studies of N -benzyl pyridinium–curcumin derivatives as potent AChE inhibitors with antioxidant activ	19
Discovery of novel biphenyl compounds bearing hydroxamic acid moiety as the first PD-L1/class I HDACs dual inhibitors	19
Discovery of lignans as the effective inhibitors of CES1A alleviate lipid droplets formation	19
Peptide foldamer-based inhibitors of the SARS-CoV-2 S protein–human ACE2 interaction	18
Phytochemical constituents of Hydrangea macrophylla var. acuminata leaves and their inhibitory activity ag	18
3-aryl-4-(3,4,5-trimethoxyphenyl)pyridines inhibit tubulin polymerisation and act as anticancer agents	18
Design, synthesis and evaluation of novel small molecules acting as Keap1-Nrf2 protein-protein interaction inhibitors	18
Identification of potential inhibitors against Staphylococcus aureus shikimate dehydrogenase through virtual screening and susceptibility test	18
Effect of trypsin inhibitor isolated from tamarind seed (TTI) on caenorhabditis elegans survival under bacterial infection	18
Dentine biomodification by sulphonamides pre-treatment: bond strength, proteolytic inhibition, and antimicrobial activity	18
Structure-activity exploration of a small-molecule allosteric inhibitor of T790M/L858R double mutant EGFR	18
Mixed and non-competitive enzyme inhibition: underlying mechanisms and mechanistic irrelevance of the formal two-site model	18
Design and synthesis of new spirooxindole candidates and their selenium nanoparticles as potential dual Topo I/II inhibitors, DNA intercalators, and apoptotic inducers	18
5-(Sulfamoyl)thien-2-yl 1,3-oxazole inhibitors of carbonic anhydrase II with hydrophilic periphery	17
Discovery of new 1 H -pyrazolo[3,4- d ]pyrimidine derivatives as anticancer agents targeting EGFR	17
The inhibitory effect of boric acid on hypoxia-regulated tumour-associated carbonic anhydrase IX	17
Correction	17
Structure-activity relationship studies for inhibitors for vancomycin-resistant Enterococcus and human carbonic anhydrases	17
Synthesis and antitumor activity of litseaone B analogues as tubulin polymerisation inhibitors	17
Replacing the phthalimide core in thalidomide with benzotriazole	17
Latest advances in dual inhibitors of acetylcholinesterase and monoamine oxidase B against Alzheimer’s disease	17
Inhibitory effect of roburic acid in combination with docetaxel on human prostate cancer cells	17
Novel N -methylsulfonyl-indole derivatives: biological activity and COX-2/5-LOX inhibitory effect with improved gastro protective profile and reduced car	16
Design, synthesis, biological evaluation and molecular docking study of novel pleuromutilin derivatives containing substituted benzoxazole as antibacterial agents	16
Synthesis and evaluation of 5, 6-dihydro-8 H -isoquinolino[1, 2- b ]quinazolin-8-one derivatives as novel	16
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	16
Discovery and development of steroidal enzyme inhibitors as anti-cancer drugs: state-of-the-art and future perspectives	16
Design, synthesis and evaluation of quinoline- O -carbamate derivatives as multifunctional agents for the treatment of Alzheimer’s disease	16
Dyhidro-β-agarofurans natural and synthetic as acetylcholinesterase and COX inhibitors: interaction with the peripheral anionic site (AChE-PAS), and anti-inflammatory potentials	16
Chemical composition, antioxidant activities, and enzyme inhibitory effects of Lespedeza bicolour Turcz. essential oil	16
Evaluation of the anticancer effects exerted by 5-fluorouracil and heme oxygenase-1 inhibitor hybrids in HTC116 colorectal cancer cells	16
Effect of hydrophobic extension of aryl enaminones and pyrazole-linked compounds combined with sulphonamide, sulfaguanidine, or carboxylic acid functionalities on carbonic anhydrase inhibitory potency	16
Rational repurposing, synthesis, in vitro and in silico studies of chromone-peptidyl hybrids as potential	16
Discovery of new pyridine-quinoline hybrids as competitive and non-competitive PIM-1 kinase inhibitors with apoptosis induction and caspase 3/7 activation capabilities	16
Design, synthesis, and evaluation of cyclic C7-bridged monocarbonyl curcumin analogs containing an o -methoxy phenyl group as potential agents against gastric cancer	16
Pyridine indole hybrids as novel potent CYP17A1 inhibitors	15
Discovery of novel 2-aminopyridine derivatives as ROS1 and ALK dual inhibitors to combat drug-resistant mutants including ROS1 ^G2032R and ALK	15
Statement of Retraction: Dependence on linkers’ flexibility designed for benzenesulfonamides targeting discovery of novel hCA IX inhibitors as potent anticancer agents	15
Chromone-based monoamine oxidase B inhibitor with potential iron-chelating activity for the treatment of Alzheimer’s disease	15
Ferroptosis and hearing loss: from molecular mechanisms to therapeutic interventions	15
Advances in ERK1/2 inhibition: a medicinal chemistry perspective on structure and regulation	15
Design, synthesis and biological evaluation of 4-aminoquinoline derivatives as receptor-interacting protein kinase 2 (RIPK2) inhibitors	15