OOIR: Observatory of International Research

Papers

(The TQCC of Journal of Enzyme Inhibition and Medicinal Chemistry is 13. The table below lists those papers that are above that threshold based on CrossRef citation counts [max. 250 papers]. The publications cover those that have been published in the past four years, i.e., from 2021-05-01 to 2025-05-01.)

Article	Citations
Synthesis, DFT calculations, and anti-proliferative evaluation of pyrimidine and selenadiazolopyrimidine derivatives as dual Topoisomerase II and HSP90 inhibitors	140
Design, synthesis, and biological evaluation of biotinylated colchicine derivatives as potential antitumor agents	111
Recombinant ferritins for multimodal nanomedicine	81
Diversely substituted sulfamides for fragment-based drug discovery of carbonic anhydrase inhibitors: synthesis and inhibitory profile	69
Discovery and SAR analysis of phenylbenzo[d][1,3]dioxole-based proprotein convertase subtilisin/kexin type 9 inhibitors	60
Novel harmine derivatives as potent acetylcholinesterase and amyloid beta aggregation dual inhibitors for management of Alzheimer’s disease	54
Design, synthesis, and biological evaluation of potent FAK-degrading PROTACs	52
Mechanism of biotin carboxylase inhibition by ethyl 4-[[2-chloro-5-(phenylcarbamoyl)phenyl]sulphonylamino]benzoate	47
Recent progress in chemistry and bioactivity of monoterpenoid indole alkaloids from the genus gelsemium : a comprehensive review	47
4-Cyanamidobenzenesulfonamide derivatives: a novel class of human and bacterial carbonic anhydrase inhibitors	45
Design, synthesis, and molecular docking studies of novel pomalidomide-based PROTACs as potential anti-cancer agents targeting EGFR^WT and EGFR^T790M	43
Different chemical proteomic approaches to identify the targets of lapatinib	43
Design, synthesis and antitumor evaluation of novel pyrazolo[3,4- d ]pyrimidines incorporating different amino acid conjugates as potential DHFR inhibitors	42
Ultrasound promoted green synthesis, anticancer evaluation, and molecular docking studies of hydrazines: a pilot trial	42
Myeloperoxidase as a therapeutic target for oxidative damage in Alzheimer’s disease	42
Synthesis, biological evaluation, and in silico studies of new CDK2 inhibitors based on pyrazolo[3,4-d]pyrimidine and pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine scaffo	41
Identification of novel non-toxic and anti-angiogenic α-fluorinated chalcones as potent colchicine binding site inhibitors	40
Towards safer anti-inflammatory therapy: synthesis of new thymol–pyrazole hybrids as dual COX-2/5-LOX inhibitors	40
Development of new thiazolidine-2,4-dione hybrids as aldose reductase inhibitors endowed with antihyperglycaemic activity: design, synthesis, biological investigations, and in silico	40
Discovery of a selective PI3Kα inhibitor via structure-based virtual screening for targeted colorectal cancer therapy	39
Development of novel 9-O-substituted-13-octylberberine derivatives as potential anti-hepatocellular carcinoma agents	37
Promising inhibition of diabetes-related enzymes and antioxidant properties of Ptilostemon casabonae leaves extract	37
From Antarctica to cancer research: a novel human DNA topoisomerase 1B inhibitor from Antarctic sponge Dendrilla antarctica	37
Synthesis, molecular modelling and QSAR study of new N-phenylacetamide-2-oxoindole benzensulfonamide conjugates as carbonic anhydrase inhibitors with antiproliferative activity	37
1,3,4-Oxadiazole-naphthalene hybrids as potential VEGFR-2 inhibitors: design, synthesis, antiproliferative activity, apoptotic effect, and in silico studies	37

Investigation of the enantioselectivity of acetylcholinesterase and butyrylcholinesterase upon inhibition by tacrine-iminosugar heterodimers	37
Targeting the glutamine-arginine-proline metabolism axis in cancer	35
2,5-Dihydroxyphenylethanone: an anti-melanogenic bioactive compound isolated from Ganoderma cochlear	34
Development of ketobenzothiazole-based peptidomimetic TMPRSS13 inhibitors with low nanomolar potency	34
Antifungal and anti-biofilm effects of hydrazone derivatives on Candida spp	34
New imidazole-2-thiones linked to acenaphythylenone as dual DNA intercalators and topoisomerase II inhibitors: structural optimization, docking, and apoptosis studies	33
GC-MS metabolites profiling of anethole-rich oils by different extraction techniques: antioxidant, cytotoxicity and in-silico enzymes inhibitory insights	32
New benzoxazole derivatives as potential VEGFR-2 inhibitors and apoptosis inducers: design, synthesis, anti-proliferative evaluation, flowcytometric analysis, and in silico studies	32
Searching for drug leads targeted to the hydrophobic cleft of dengue virus capsid protein	31
Selisistat, a SIRT1 inhibitor, enhances paclitaxel activity in luminal and triple-negative breast cancer: in silico, in vitro, and in vivo studies	31
Synthesis and structure–activity relationships for some novel diflapolin derivatives with benzimidazole subunit	31
Drug-like molecules with anti-trypanothione synthetase activity identified by high throughput screening	31
Dithiocarbamates effectively inhibit the α-carbonic anhydrase from Neisseria gonorrhoeae	31
Heterologous expression and biochemical characterisation of the recombinant β-carbonic anhydrase (MpaCA) from the warm-blooded vertebrate pathogen malassezia pachydermatis	31
Discovery of a novel Aurora B inhibitor GSK650394 with potent anticancer and anti-aspergillus fumigatus dual efficacies in vitro	30
3 H -1,2-Benzoxaphosphepine 2-oxides as selective inhibitors of carbonic anhydrase IX and XII	30
Structure-based virtual screening and biological evaluation of novel small-molecule BTK inhibitors	29
Identification of sulphonamide-tethered N -((triazol-4-yl)methyl)isatin derivatives as inhibitors of SARS-CoV-2 main protease	28
Design, synthesis, docking, and anticancer evaluations of new thiazolo[3,2- a ] pyrimidines as topoisomerase II inhibitors	28
Identification of new benzimidazole-triazole hybrids as anticancer agents: multi-target recognition, in vitro and in silico studies	28
Development of potent and effective SARS-CoV-2 main protease inhibitors based on maleimide analogs for the potential treatment of COVID-19	28
Anti-obesity carbonic anhydrase inhibitors: challenges and opportunities	28
Fragment-based design, synthesis and biological evaluation of theophylline derivatives as ATAD2 inhibitors in BT-549 cells	28
Development of naringenin-O-alkylamine derivatives as multifunctional agents for the treatment of Alzheimer’s disease	27
1,2,3-Benzoxathiazine-2,2-dioxides – effective inhibitors of human carbonic anhydrases	26
Crystal structure of ricin toxin A chain complexed with a highly potent pterin-based small-molecular inhibitor	26
Design, synthesis, biological evaluation and QSAR analysis of novel N-substituted benzimidazole derived carboxamides	26
Structural comparison of substrate-binding pockets of serine β-lactamases in classes A, C, and D	25
PD-L1 dimerisation induced by biphenyl derivatives mediates anti-breast cancer activity via the non-immune PD-L1–AKT–mTOR/Bcl2 pathway	25
Discovery of novel polysubstituted N -alkyl acridone analogues as histone deacetylase isoform-selective inhibitors for cancer therapy	25
Regioselective approach to colchiceine tropolone ring functionalization at C(9) and C(10) yielding new anticancer hybrid derivatives containing heterocyclic structural motifs	25
Searching for novel MDM2/MDMX dual inhibitors through a drug repurposing approach	25
Probing mutation-induced conformational transformation of the GTP/M-RAS complex through Gaussian accelerated molecular dynamics simulations	24
Unveiling the mechanism of action of acylated temporin L analogues against multidrug-resistant Candida albicans	24
Recent progress in discovery of novel AAK1 inhibitors: from pain therapy to potential anti-viral agents	24
Selective inhibition of carbonic anhydrase IX by sulphonylated 1,2,3-triazole incorporated benzenesulphonamides capable of inducing apoptosis	24
Antiglycoxidative properties of amantadine – a systematic review and comprehensive in vitro study	24
Challenging the Biginelli scaffold to surpass the first line antitubercular drugs: Mycobacterium tuberculosis thymidine monophosphate kinase (TMPK mt	24
o-Vanillin binds covalently to MAL/TIRAP Lys-210 but independently inhibits TLR2	23
Design, synthesis, and study of novel phenethyl-based antitumor phospholipids downregulating p38 mitogen-activated protein kinase	23
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/ EG	23
Exploring covalent inhibitors of SARS-CoV-2 main protease: from peptidomimetics to novel scaffolds	23
Statement of Retraction: Dihydroartemisinin enhances the anti-tumor effect of photodynamic therapy by targeting PKM2-mediated glycolysis in esophageal cancer cell	23
Discovery of an effective anti-inflammatory agent for inhibiting the activation of NF-κB	22
Design, synthesis, molecular modelling and antitumor evaluation of S -glucosylated rhodanines through topo II inhibition and DNA intercalation	21
Heterocycle-containing tranylcypromine derivatives endowed with high anti-LSD1 activity	21
Identification of putative allosteric inhibitors of BCKDK via virtual screening and biological evaluation	21
Coumarins inhibit η-class carbonic anhydrase from Plasmodium falciparum	21
Discovery of selective ACAT2 antagonist via a combination strategy based on deep docking, pharmacophore modelling, and molecular dynamics simulation	20
A polypeptide inhibitor of calcineurin blocks the calcineurin-NFAT signalling pathway in vivo and in vitro	20

New 1,2,3-triazole linked ciprofloxacin-chalcones induce DNA damage by inhibiting human topoisomerase I& II and tubulin polymerization	20
Anti-breast cancer sinomenine derivatives via mechanisms of apoptosis induction and metastasis reduction	20
Fluorinated indeno-quinoxaline bearing thiazole moieties as hypoglycaemic agents targeting α -amylase, and α -glucosidase: synthesis, mole	20
Development of novel anilinoquinazoline-based carboxylic acids as non-classical carbonic anhydrase IX and XII inhibitors	20
Design and biological evaluation of substituted 5,7-dihydro-6H-indolo[2,3-c]quinolin-6-one as novel selective Haspin inhibitors	20
Discovery of benzochromene derivatives first example with dual cytotoxic activity against the resistant cancer cell MCF-7/ADR and inhibitory effect of the P -glycoprotei	19
Charged pyridinium oximes with thiocarboxamide moiety are equally or less effective reactivators of organophosphate-inhibited cholinesterases compared to analogous carboxamides	19
Design and synthesis of some new benzoylthioureido benzenesulfonamide derivatives and their analogues as carbonic anhydrase inhibitors	19
Design, synthesis, and bioevaluation of 1 h -pyrrolo[3,2- c ]pyridine derivatives as colchicine-binding site inhibitors with potent antica	19
Arctigenin: pharmacology, total synthesis, and progress in structure modification	19
Discovery of a novel PLK1 inhibitor with high inhibitory potency using a combined virtual screening strategy	19
Design and synthesis of novel HDAC6 inhibitor dimer as HDAC6 degrader for cancer treatment by palladium catalysed dimerisation	19
Insights into the inhibitory activities of neolignans and diarylnonanoid derivatives from nutmeg ( Myristica fragrans Houtt.) seeds on soluble epoxide hydrolase using	18
The importance of including the C-terminal domain of PTP1B _1-400 to identify potential antidiabetic inhibitors	18
Design, synthesis, anti-inflammatory evaluation, and molecular modelling of new coumarin-based analogs combined curcumin and other heterocycles as potential TNF-α production inhibitors	18
Flavonoids as tyrosinase inhibitors in in silico and in vitro models: basic framework of SAR using a statistical modelling approach	18
Discovery of novel paeonol-based derivatives against skin inflammation in vitro and in vivo	18
Purification and characterisation of glutathione reductase from scorpionfish (scorpaena porcus) and investigation of heavy metal ions inhibition	18
Fourth-generation EGFR-TKI to overcome C797S mutation: past, present, and future	18
Thio- and selenosemicarbazones as antiprotozoal agents against Trypanosoma cruzi and Trichomonas vaginalis	18
Discovering a novel dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A) inhibitor and its impact on tau phosphorylation and amyloid-β formation	17
Short divalent ethacrynic amides as pro-inhibitors of glutathione S-transferase isozyme Mu and potent sensitisers of cisplatin-resistant ovarian cancers	17
TNP and its analogs: Modulation of IP6K and CYP3A4 inhibition	17
Investigation of novel alkyl/benzyl (4-sulphamoylphenyl)carbamimidothioates as carbonic anhydrase inhibitors	17
Synthesis and biological evaluation of ortho -phenyl phenylhydroxamic acids containing phenothiazine with improved selectivity for class IIa histone deacetylases	16
Synthesis, biological evaluation, and computational studies of N -benzyl pyridinium–curcumin derivatives as potent AChE inhibitors with antioxidant activity	16
Design, synthesis and biological evaluation of novel diarylpyridine derivatives as tubulin polymerisation inhibitors	16
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	16
Discovery of novel biphenyl compounds bearing hydroxamic acid moiety as the first PD-L1/class I HDACs dual inhibitors	16
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	16
Druggable cavities and allosteric modulators of the cell division cycle 7 (CDC7) kinase	16
Novel benzo chromene derivatives: design, synthesis, molecular docking, cell cycle arrest, and apoptosis induction in human acute myeloid leukemia HL-60 cells	15
Structure-activity exploration of a small-molecule allosteric inhibitor of T790M/L858R double mutant EGFR	15
Replacing the phthalimide core in thalidomide with benzotriazole	15
Identification of potential inhibitors against Staphylococcus aureus shikimate dehydrogenase through virtual screening and susceptibility test	15
Design, synthesis and antitumor activity of 5-trifluoromethylpyrimidine derivatives as EGFR inhibitors	15
Dentine biomodification by sulphonamides pre-treatment: bond strength, proteolytic inhibition, and antimicrobial activity	15
Correction	15
Prospecting in silico antibacterial activity of a peptide from trypsin inhibitor isolated from tamarind seed	15
Mixed and non-competitive enzyme inhibition: underlying mechanisms and mechanistic irrelevance of the formal two-site model	15
5-(Sulfamoyl)thien-2-yl 1,3-oxazole inhibitors of carbonic anhydrase II with hydrophilic periphery	15
Design and synthesis of new spirooxindole candidates and their selenium nanoparticles as potential dual Topo I/II inhibitors, DNA intercalators, and apoptotic inducers	15
Discovery of lignans as the effective inhibitors of CES1A alleviate lipid droplets formation	15
Peptide foldamer-based inhibitors of the SARS-CoV-2 S protein–human ACE2 interaction	14
Structure-activity relationship studies for inhibitors for vancomycin-resistant Enterococcus and human carbonic anhydrases	14
Rational repurposing, synthesis, in vitro and in silico studies of chromone-peptidyl hybrids as potential agents against Le	14
Design, synthesis, biological evaluation and molecular docking study of novel pleuromutilin derivatives containing substituted benzoxazole as antibacterial agents	14
Design, synthesis and evaluation of novel small molecules acting as Keap1-Nrf2 protein-protein interaction inhibitors	14
3-aryl-4-(3,4,5-trimethoxyphenyl)pyridines inhibit tubulin polymerisation and act as anticancer agents	14
Dyhidro-β-agarofurans natural and synthetic as acetylcholinesterase and COX inhibitors: interaction with the peripheral anionic site (AChE-PAS), and anti-inflammatory potentials	14
Inhibitory effect of roburic acid in combination with docetaxel on human prostate cancer cells	14
The inhibitory effect of boric acid on hypoxia-regulated tumour-associated carbonic anhydrase IX	14
Effect of trypsin inhibitor isolated from tamarind seed (TTI) on caenorhabditis elegans survival under bacterial infection	14
Latest advances in dual inhibitors of acetylcholinesterase and monoamine oxidase B against Alzheimer’s disease	14
Discovery of new 1H-pyrazolo[3,4-d]pyrimidine derivatives as anticancer agents targeting EGFR^WT and EGFR^T790M	14
Synthesis and antitumor activity of litseaone B analogues as tubulin polymerisation inhibitors	14
Discovery of new pyridine-quinoline hybrids as competitive and non-competitive PIM-1 kinase inhibitors with apoptosis induction and caspase 3/7 activation capabilities	14
Synthesis and evaluation of 5, 6-dihydro-8 H -isoquinolino[1, 2- b ]quinazolin-8-one derivatives as novel non-lipogenic ABCA1 up-regulator	13
Design, synthesis and evaluation of quinoline- O -carbamate derivatives as multifunctional agents for the treatment of Alzheimer’s disease	13
Chromone-based monoamine oxidase B inhibitor with potential iron-chelating activity for the treatment of Alzheimer’s disease	13
Discovery and development of steroidal enzyme inhibitors as anti-cancer drugs: state-of-the-art and future perspectives	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 celecoxib analogs:	13
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
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 cardio vascular ris	13