Journal of Enzyme Inhibition and Medicinal Chemistry

Papers
(The TQCC of Journal of Enzyme Inhibition and 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 2021-07-01 to 2025-07-01.)
ArticleCitations
Recombinant ferritins for multimodal nanomedicine151
Synthesis, DFT calculations, and anti-proliferative evaluation of pyrimidine and selenadiazolopyrimidine derivatives as dual Topoisomerase II and HSP90 inhibitors111
Ultrasound promoted green synthesis, anticancer evaluation, and molecular docking studies of hydrazines: a pilot trial85
Design, synthesis, and biological evaluation of potent FAK-degrading PROTACs72
Identification of novel non-toxic and anti-angiogenic α-fluorinated chalcones as potent colchicine binding site inhibitors61
Discovery and SAR analysis of phenylbenzo[d][1,3]dioxole-based proprotein convertase subtilisin/kexin type 9 inhibitors55
Synthesis, biological evaluation, and in silico studies of new CDK2 inhibitors based on pyrazolo[3,4- d ]pyrimidine and pyrazolo[4,3- 55
Design, synthesis, and biological evaluation of biotinylated colchicine derivatives as potential antitumor agents52
Mechanism of biotin carboxylase inhibition by ethyl 4-[[2-chloro-5-(phenylcarbamoyl)phenyl]sulphonylamino]benzoate50
Diversely substituted sulfamides for fragment-based drug discovery of carbonic anhydrase inhibitors: synthesis and inhibitory profile49
Design, synthesis and antitumor evaluation of novel pyrazolo[3,4- d ]pyrimidines incorporating different amino acid conjugates as potential DHFR inhibitors49
Different chemical proteomic approaches to identify the targets of lapatinib47
Novel harmine derivatives as potent acetylcholinesterase and amyloid beta aggregation dual inhibitors for management of Alzheimer’s disease46
4-Cyanamidobenzenesulfonamide derivatives: a novel class of human and bacterial carbonic anhydrase inhibitors45
Natural product sennoside B disrupts liquid-liquid phase separation of SARS-CoV-2 nucleocapsid protein by inhibiting its RNA-binding activity45
Towards safer anti-inflammatory therapy: synthesis of new thymol–pyrazole hybrids as dual COX-2/5-LOX inhibitors44
Development of new thiazolidine-2,4-dione hybrids as aldose reductase inhibitors endowed with antihyperglycaemic activity: design, synthesis, biological investigations, and in silico44
Myeloperoxidase as a therapeutic target for oxidative damage in Alzheimer’s disease43
Recent progress in chemistry and bioactivity of monoterpenoid indole alkaloids from the genus gelsemium : a comprehensive review42
Design, synthesis, and molecular docking studies of novel pomalidomide-based PROTACs as potential anti-cancer agents targeting EGFR WT and EGFR T79041
Discovery of a selective PI3Kα inhibitor via structure-based virtual screening for targeted colorectal cancer therapy41
2,5-Dihydroxyphenylethanone: an anti-melanogenic bioactive compound isolated from Ganoderma cochlear40
Promising inhibition of diabetes-related enzymes and antioxidant properties of Ptilostemon casabonae leaves extract40
Antifungal and anti-biofilm effects of hydrazone derivatives on Candida spp40
Investigation of the enantioselectivity of acetylcholinesterase and butyrylcholinesterase upon inhibition by tacrine-iminosugar heterodimers39
Development of novel 9- O -substituted-13-octylberberine derivatives as potential anti-hepatocellular carcinoma agents39
Synthesis, molecular modelling and QSAR study of new N- phenylacetamide-2-oxoindole benzensulfonamide conjugates as carbonic anhydrase inhibitors with antiproliferative 38
Targeting the glutamine-arginine-proline metabolism axis in cancer37
From Antarctica to cancer research: a novel human DNA topoisomerase 1B inhibitor from Antarctic sponge Dendrilla antarctica37
1,3,4-Oxadiazole-naphthalene hybrids as potential VEGFR-2 inhibitors: design, synthesis, antiproliferative activity, apoptotic effect, and in silico studies36
Development of ketobenzothiazole-based peptidomimetic TMPRSS13 inhibitors with low nanomolar potency35
Identification of sulphonamide-tethered N -((triazol-4-yl)methyl)isatin derivatives as inhibitors of SARS-CoV-2 main protease35
Design and synthesis of 1,4,8-triazaspiro[4.5]decan-2-one derivatives as novel mitochondrial permeability transition pore inhibitors34
Development of potent and effective SARS-CoV-2 main protease inhibitors based on maleimide analogs for the potential treatment of COVID-1934
Selisistat, a SIRT1 inhibitor, enhances paclitaxel activity in luminal and triple-negative breast cancer: in silico, in vitro, and in vivo studies34
Fragment-based design, synthesis and biological evaluation of theophylline derivatives as ATAD2 inhibitors in BT-549 cells34
Design, synthesis, docking, and anticancer evaluations of new thiazolo[3,2- a ] pyrimidines as topoisomerase II inhibitors34
Identification of new benzimidazole-triazole hybrids as anticancer agents: multi-target recognition, in vitro and in silico studies33
New imidazole-2-thiones linked to acenaphythylenone as dual DNA intercalators and topoisomerase II inhibitors: structural optimization, docking, and apoptosis studies33
Discovery of a novel Aurora B inhibitor GSK650394 with potent anticancer and anti- aspergillus fumigatus dual efficacies in vitro33
Heterologous expression and biochemical characterisation of the recombinant β-carbonic anhydrase (MpaCA) from the warm-blooded vertebrate pathogen malassezia pachydermatis32
GC-MS metabolites profiling of anethole-rich oils by different extraction techniques: antioxidant, cytotoxicity and in-silico enzymes inhibitory insights31
New benzoxazole derivatives as potential VEGFR-2 inhibitors and apoptosis inducers: design, synthesis, anti-proliferative evaluation, flowcytometric analysis, and in silico 31
Dithiocarbamates effectively inhibit the α-carbonic anhydrase from Neisseria gonorrhoeae30
Structure-based virtual screening and biological evaluation of novel small-molecule BTK inhibitors30
Searching for drug leads targeted to the hydrophobic cleft of dengue virus capsid protein29
Synthesis and structure–activity relationships for some novel diflapolin derivatives with benzimidazole subunit29
Drug-like molecules with anti-trypanothione synthetase activity identified by high throughput screening29
Anti-obesity carbonic anhydrase inhibitors: challenges and opportunities28
Development of naringenin- O -alkylamine derivatives as multifunctional agents for the treatment of Alzheimer’s disease28
3 H -1,2-Benzoxaphosphepine 2-oxides as selective inhibitors of carbonic anhydrase IX and XII28
1,2,3-Benzoxathiazine-2,2-dioxides – effective inhibitors of human carbonic anhydrases27
Crystal structure of ricin toxin A chain complexed with a highly potent pterin-based small-molecular inhibitor27
PD-L1 dimerisation induced by biphenyl derivatives mediates anti-breast cancer activity via the non-immune PD-L1–AKT–mTOR/Bcl2 pathway26
Unveiling the mechanism of action of acylated temporin L analogues against multidrug-resistant Candida albicans26
o-Vanillin binds covalently to MAL/TIRAP Lys-210 but independently inhibits TLR226
Searching for novel MDM2/MDMX dual inhibitors through a drug repurposing approach26
Probing mutation-induced conformational transformation of the GTP/M-RAS complex through Gaussian accelerated molecular dynamics simulations26
Structural comparison of substrate-binding pockets of serine β-lactamases in classes A, C, and D26
Recent progress in discovery of novel AAK1 inhibitors: from pain therapy to potential anti-viral agents26
Antiglycoxidative properties of amantadine – a systematic review and comprehensive in vitro study25
Structural isomerisation affects the antitubercular activity of adamantyl-isoxyl adducts25
Challenging the Biginelli scaffold to surpass the first line antitubercular drugs: Mycobacterium tuberculosis thymidine monophosphate kinase (TMPK mt 25
Design, synthesis, biological evaluation and QSAR analysis of novel N -substituted benzimidazole derived carboxamides24
Regioselective approach to colchiceine tropolone ring functionalization at C(9) and C(10) yielding new anticancer hybrid derivatives containing heterocyclic structural motifs24
Selective inhibition of carbonic anhydrase IX by sulphonylated 1,2,3-triazole incorporated benzenesulphonamides capable of inducing apoptosis24
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/ EG24
Discovery of novel polysubstituted N -alkyl acridone analogues as histone deacetylase isoform-selective inhibitors for cancer therapy24
Statement of Retraction: Dihydroartemisinin enhances the anti-tumor effect of photodynamic therapy by targeting PKM2-mediated glycolysis in esophageal cancer cell24
Development of novel anilinoquinazoline-based carboxylic acids as non-classical carbonic anhydrase IX and XII inhibitors23
Design and synthesis of some new benzoylthioureido benzenesulfonamide derivatives and their analogues as carbonic anhydrase inhibitors23
Discovery of an effective anti-inflammatory agent for inhibiting the activation of NF-κB23
Discovery of selective ACAT2 antagonist via a combination strategy based on deep docking, pharmacophore modelling, and molecular dynamics simulation23
Design, synthesis, molecular modelling and antitumor evaluation of S -glucosylated rhodanines through topo II inhibition and DNA intercalation23
Exploring covalent inhibitors of SARS-CoV-2 main protease: from peptidomimetics to novel scaffolds23
A polypeptide inhibitor of calcineurin blocks the calcineurin-NFAT signalling pathway in vivo and in vitro22
Design, synthesis, and study of novel phenethyl-based antitumor phospholipids downregulating p38 mitogen-activated protein kinase22
Coumarins inhibit η-class carbonic anhydrase from Plasmodium falciparum22
Anti-breast cancer sinomenine derivatives via mechanisms of apoptosis induction and metastasis reduction22
Heterocycle-containing tranylcypromine derivatives endowed with high anti-LSD1 activity22
Design and biological evaluation of substituted 5,7-dihydro-6 H -indolo[2,3- c ]quinolin-6-one as novel selective Haspin inhibitors22
Discovery of a novel PLK1 inhibitor with high inhibitory potency using a combined virtual screening strategy21
Discovery of benzochromene derivatives first example with dual cytotoxic activity against the resistant cancer cell MCF-7/ADR and inhibitory effect of the P -glycoprotei21
Arctigenin: pharmacology, total synthesis, and progress in structure modification21
Identification of putative allosteric inhibitors of BCKDK via virtual screening and biological evaluation21
New 1,2,3-triazole linked ciprofloxacin-chalcones induce DNA damage by inhibiting human topoisomerase I& II and tubulin polymerization21
Fluorinated indeno-quinoxaline bearing thiazole moieties as hypoglycaemic agents targeting α -amylase, and α -glucosidase: synthesis, mole21
Fourth-generation EGFR-TKI to overcome C797S mutation: past, present, and future20
Design, synthesis and biological evaluation of novel urolithin derivatives targeting liver cancer cells20
Flavonoids as tyrosinase inhibitors in in silico and in vitro models: basic framework of SAR using a statistical modelling approach20
Design, synthesis, and bioevaluation of 1 h -pyrrolo[3,2- c ]pyridine derivatives as colchicine-binding site inhibitors with potent antica20
Insights into the inhibitory activities of neolignans and diarylnonanoid derivatives from nutmeg ( Myristica fragrans Houtt.) seeds on soluble epoxide hydrolase using 20
Thio- and selenosemicarbazones as antiprotozoal agents against Trypanosoma cruzi and Trichomonas vaginalis20
Discovery of novel paeonol-based derivatives against skin inflammation in vitro and in vivo20
Design and synthesis of novel HDAC6 inhibitor dimer as HDAC6 degrader for cancer treatment by palladium catalysed dimerisation20
The importance of including the C-terminal domain of PTP1B 1-400 to identify potential antidiabetic inhibitors20
Purification and characterisation of glutathione reductase from scorpionfish (scorpaena porcus) and investigation of heavy metal ions inhibition20
Investigation of novel alkyl/benzyl (4-sulphamoylphenyl)carbamimidothioates as carbonic anhydrase inhibitors19
Discovering a novel dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A) inhibitor and its impact on tau phosphorylation and amyloid-β formation19
Synthesis and biological evaluation of ortho -phenyl phenylhydroxamic acids containing phenothiazine with improved selectivity for class IIa histone deacetylases19
Discovery of novel biphenyl compounds bearing hydroxamic acid moiety as the first PD-L1/class I HDACs dual inhibitors19
Design, synthesis, anti-inflammatory evaluation, and molecular modelling of new coumarin-based analogs combined curcumin and other heterocycles as potential TNF-α production inhibitors 19
Charged pyridinium oximes with thiocarboxamide moiety are equally or less effective reactivators of organophosphate-inhibited cholinesterases compared to analogous carboxamides19
Design, synthesis, biological evaluation and molecular docking study of 2,4-diarylimidazoles and 2,4-bis(benzyloxy)-5-arylpyrimidines as novel HSP90 N-terminal inhibitors18
TNP and its analogs: Modulation of IP6K and CYP3A4 inhibition18
The mechanism and pharmacodynamics of 2-((1H-indol-3-yl)thio/sulfinyl)-N-pheny acetamide derivative as a novel inhibitor against human respiratory syncytial virus18
Design, synthesis and antitumor activity of 5-trifluoromethylpyrimidine derivatives as EGFR inhibitors18
Prospecting in silico antibacterial activity of a peptide from trypsin inhibitor isolated from tamarind seed17
Short divalent ethacrynic amides as pro-inhibitors of glutathione S -transferase isozyme Mu and potent sensitisers of cisplatin-resistant ovarian cancers17
Synthesis, biological evaluation, and computational studies of N -benzyl pyridinium–curcumin derivatives as potent AChE inhibitors with antioxidant activity17
Discovery of lignans as the effective inhibitors of CES1A alleviate lipid droplets formation17
Mixed and non-competitive enzyme inhibition: underlying mechanisms and mechanistic irrelevance of the formal two-site model16
Peptide foldamer-based inhibitors of the SARS-CoV-2 S protein–human ACE2 interaction16
Novel benzo chromene derivatives: design, synthesis, molecular docking, cell cycle arrest, and apoptosis induction in human acute myeloid leukemia HL-60 cells16
Design, synthesis and biological evaluation of novel diarylpyridine derivatives as tubulin polymerisation inhibitors16
3-aryl-4-(3,4,5-trimethoxyphenyl)pyridines inhibit tubulin polymerisation and act as anticancer agents16
Identification of potential inhibitors against Staphylococcus aureus shikimate dehydrogenase through virtual screening and susceptibility test16
Effect of trypsin inhibitor isolated from tamarind seed (TTI) on caenorhabditis elegans survival under bacterial infection16
Dentine biomodification by sulphonamides pre-treatment: bond strength, proteolytic inhibition, and antimicrobial activity16
Druggable cavities and allosteric modulators of the cell division cycle 7 (CDC7) kinase16
Correction15
Structure-activity relationship studies for inhibitors for vancomycin-resistant Enterococcus and human carbonic anhydrases15
Design, synthesis, biological evaluation and molecular docking study of novel pleuromutilin derivatives containing substituted benzoxazole as antibacterial agents15
Synthesis and antitumor activity of litseaone B analogues as tubulin polymerisation inhibitors15
Replacing the phthalimide core in thalidomide with benzotriazole15
Design, synthesis and evaluation of novel small molecules acting as Keap1-Nrf2 protein-protein interaction inhibitors15
Latest advances in dual inhibitors of acetylcholinesterase and monoamine oxidase B against Alzheimer’s disease15
Synthesis and evaluation of 5, 6-dihydro-8 H -isoquinolino[1, 2- b ]quinazolin-8-one derivatives as novel non-lipogenic ABCA1 up-regulator15
Design and synthesis of new spirooxindole candidates and their selenium nanoparticles as potential dual Topo I/II inhibitors, DNA intercalators, and apoptotic inducers15
5-(Sulfamoyl)thien-2-yl 1,3-oxazole inhibitors of carbonic anhydrase II with hydrophilic periphery15
Structure-activity exploration of a small-molecule allosteric inhibitor of T790M/L858R double mutant EGFR15
Discovery of new 1 H -pyrazolo[3,4- d ]pyrimidine derivatives as anticancer agents targeting EGFR WT an15
Inhibitory effect of roburic acid in combination with docetaxel on human prostate cancer cells15
Rational repurposing, synthesis, in vitro and in silico studies of chromone-peptidyl hybrids as potential agents against Le14
Dyhidro-β-agarofurans natural and synthetic as acetylcholinesterase and COX inhibitors: interaction with the peripheral anionic site (AChE-PAS), and anti-inflammatory potentials14
Chemical composition, antioxidant activities, and enzyme inhibitory effects of Lespedeza bicolour Turcz. essential oil14
Evaluation of the anticancer effects exerted by 5-fluorouracil and heme oxygenase-1 inhibitor hybrids in HTC116 colorectal cancer cells14
Design, synthesis and evaluation of quinoline- O -carbamate derivatives as multifunctional agents for the treatment of Alzheimer’s disease14
Effect of hydrophobic extension of aryl enaminones and pyrazole-linked compounds combined with sulphonamide, sulfaguanidine, or carboxylic acid functionalities on carbonic anhydrase inhibitory potency14
The inhibitory effect of boric acid on hypoxia-regulated tumour-associated carbonic anhydrase IX14
Discovery of new pyridine-quinoline hybrids as competitive and non-competitive PIM-1 kinase inhibitors with apoptosis induction and caspase 3/7 activation capabilities14
Design, synthesis, and evaluation of cyclic C7-bridged monocarbonyl curcumin analogs containing an o -methoxy phenyl group as potential agents against gastric cancer14
Discovery and development of steroidal enzyme inhibitors as anti-cancer drugs: state-of-the-art and future perspectives14
Novel N -methylsulfonyl-indole derivatives: biological activity and COX-2/5-LOX inhibitory effect with improved gastro protective profile and reduced cardio vascular ris14
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:14
Design, synthesis and biological evaluation of 4-aminoquinoline derivatives as receptor-interacting protein kinase 2 (RIPK2) inhibitors14
Study on the synthesis and biological activity of kojic acid triazol thiosemicarbazide Schiff base derivatives14
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