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 2021-04-01 to 2025-04-01.)

Article	Citations
Mechanism of biotin carboxylase inhibition by ethyl 4-[[2-chloro-5-(phenylcarbamoyl)phenyl]sulphonylamino]benzoate	133
Natural product as a lead for impairing mitochondrial respiration in cancer cells	110
Rational design of biodegradable sulphonamide candidates treating septicaemia by synergistic dual inhibition of COX-2/PGE2 axis and DHPS enzyme	81
Click chemistry approaches for developing carbonic anhydrase inhibitors and their applications	67
New benzothiazole hybrids as potential VEGFR-2 inhibitors: design, synthesis, anticancer evaluation, and in silico study	57
Discovery of novel biphenyl compounds bearing hydroxamic acid moiety as the first PD-L1/class I HDACs dual inhibitors	52
Methotrexate, an anti-inflammatory drug, inhibits Hepatitis E viral replication	50
New spiro-indeno[1,2- b ]quinoxalines clubbed with benzimidazole scaffold as CDK2 inhibitors for halting non-small cell lung cancer; stereoselective synthesis, molecular	47
Discovery of novel 2-(4-(benzyloxy)-5-(hydroxyl) phenyl) benzothiazole derivatives as multifunctional MAO-B inhibitors for the treatment of Parkinson’s disease	46
Different chemical proteomic approaches to identify the targets of lapatinib	44
4-Cyanamidobenzenesulfonamide derivatives: a novel class of human and bacterial carbonic anhydrase inhibitors	42
Development of PD3 and PD3-B for PDEδ inhibition to modulate KRAS activity	41
Automated approach for the evaluation of glutathione-S-transferase P1-1 inhibition by organometallic anticancer compounds	41
Druggable cavities and allosteric modulators of the cell division cycle 7 (CDC7) kinase	41
Prospecting in silico antibacterial activity of a peptide from trypsin inhibitor isolated from tamarind seed	41
Design, synthesis, and biological evaluation of new thieno[2,3-d] pyrimidine derivatives as targeted therapy for PI3K with molecular modelling study	41
Myeloperoxidase as a therapeutic target for oxidative damage in Alzheimer’s disease	38
The new thiazolidine-2,4-dione-based hybrids with promising antimycobacterial activity: design, synthesis, biological evaluation, and drug interaction analysis	38
Discovery of new thymol-3,4-disubstituted thiazole hybrids as dual COX-2/5-LOX inhibitors with in vivo proof	37
Identification of novel non-toxic and anti-angiogenic α-fluorinated chalcones as potent colchicine binding site inhibitors	37
Discovery of 1,3-disubstituted prop-2-en-1-one derivatives as inhibitors of neutrophilic inflammation via modulation of MAPK and Akt pathways	36
Synthesis and biological evaluation of ortho -phenyl phenylhydroxamic acids containing phenothiazine with improved selectivity for class IIa histone deacetylases	36
Diversely substituted sulfamides for fragment-based drug discovery of carbonic anhydrase inhibitors: synthesis and inhibitory profile	35
Short divalent ethacrynic amides as pro-inhibitors of glutathione S-transferase isozyme Mu and potent sensitisers of cisplatin-resistant ovarian cancers	35
Upregulation of p53 through induction of MDM2 degradation: improved potency through the introduction of an alkylketone sidechain on the anthraquinone core	34

Development of Praziquantel sulphonamide derivatives as antischistosomal drugs	33
Design, synthesis, and molecular docking studies of novel pomalidomide-based PROTACs as potential anti-cancer agents targeting EGFR^WT and EGFR^T790M	33
Discovery and SAR analysis of 5-chloro-4-((substituted phenyl)amino)pyrimidine bearing histone deacetylase inhibitors	32
Discovery ofN-quinazolinone-4-hydroxy-2-quinolone-3-carboxamides as DNA gyrase B-targeted antibacterial agents	32
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	32
Identification of 1H-pyrazolo[3,4-b]pyridine derivatives as novel and potent TBK1 inhibitors: design, synthesis, biological evaluation, and molecular docking study	31
Recombinant ferritins for multimodal nanomedicine	31
Multitarget drugs as potential therapeutic agents for alzheimer’s disease. A new family of 5-substituted indazole derivatives as cholinergic and BACE1 inhibitors	31
Privileged multi-target directed propargyl-tacrines combining cholinesterase and monoamine oxidase inhibition activities	31
Discovery and SAR analysis of phenylbenzo[d][1,3]dioxole-based proprotein convertase subtilisin/kexin type 9 inhibitors	30
Discovery of a new class of triazole based inhibitors of acetyl transferase KAT2A	30
Overcoming the imatinib-resistant BCR-ABL mutants with new ureidobenzothiazole chemotypes endowed with potent and broad-spectrum anticancer activity	30
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	30
Styrylquinazoline derivatives as ABL inhibitors selective for different DFG orientations	29
Design, synthesis and biological evaluation of novel diarylpyridine derivatives as tubulin polymerisation inhibitors	29
Synthesis, kinetic studies and in-silico investigations of novel quinolinyl-iminothiazolines as alkaline phosphatase inhibitors	28
Sulphonamide inhibition studies of the β-carbonic anhydrase GsaCAβ present in the salmon platyhelminth parasite Gyrodactylus salaris	28
Novel isobavachalcone derivatives induce apoptosis and necroptosis in human non-small cell lung cancer H1975 cells	27
Investigating the potential anticancer activities of antibiotics as topoisomerase II inhibitors and DNA intercalators: in vitro , molecular docking, molecular dynamics,	27
Ligand-based pharmacophore modelling, structure optimisation, and biological evaluation for the identification of 2-heteroarylthio- N -arylacetamides as novel HSP90 C-te	27
Fluorine and chlorine substituted adamantyl-urea as molecular tools for inhibition of human soluble epoxide hydrolase with picomolar efficacy	27
Synthesis, biological evaluation, and computational studies of N -benzyl pyridinium–curcumin derivatives as potent AChE inhibitors with antioxidant activity	27
Design, synthesis and in vitro biological studies of novel triazoles with potent and broad-spectrum antifungal activity	26
Synthesis, DFT calculations, and anti-proliferative evaluation of pyrimidine and selenadiazolopyrimidine derivatives as dual Topoisomerase II and HSP90 inhibitors	25
Click estradiol dimers with novel aromatic bridging units: synthesis and anticancer evaluation	25
Discovery of novel FGFR4 inhibitors through a build-up fragment strategy	25
Design, synthesis, and biological evaluation of biotinylated colchicine derivatives as potential antitumor agents	24
Discovering a novel dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A) inhibitor and its impact on tau phosphorylation and amyloid-β formation	24
TNP and its analogs: Modulation of IP6K and CYP3A4 inhibition	24
Interactions of 2,6-substituted purines with purine nucleoside phosphorylase from Helicobacter pylori in solution and in the crystal, and the effects of these compounds on cell cultures of this	24
Synthesis and in vitro evaluation of benzo[b]thiophene-3-carboxylic acid 1,1-dioxide derivatives as anticancer agents targeting the RhoA/ROCK pathway	24
Highly potent inhibitors of cathepsin K with a differently positioned cyanohydrazide warhead: structural analysis of binding mode to mature and zymogen-like enzymes	23
Discovery of triterpenoids as potent dual inhibitors of pancreatic lipase and human carboxylesterase 1	23
Design, synthesis, and biological evaluation of potent FAK-degrading PROTACs	23
Correction	22
Design, synthesis, and biological investigation of oxadiazolyl, thiadiazolyl, and pyrimidinyl linked antipyrine derivatives as potential non-acidic anti-inflammatory agents	22
Proteolysis-targeting chimaeras (PROTACs) as pharmacological tools and therapeutic agents: advances and future challenges	22
Correction	22
Development of new thiazolidine-2,4-dione hybrids as aldose reductase inhibitors endowed with antihyperglycaemic activity: design, synthesis, biological investigations, and in silico	21
Potent inhibition of human tyrosinase inhibitor by verproside from the whole plant of Pseudolysimachion rotundum var. subintegrum	21
Recent progress in chemistry and bioactivity of monoterpenoid indole alkaloids from the genus gelsemium : a comprehensive review	21
Novel harmine derivatives as potent acetylcholinesterase and amyloid beta aggregation dual inhibitors for management of Alzheimer’s disease	21
Inhibitors of phosphoinositide 3-kinase (PI3K) and phosphoinositide 3-kinase-related protein kinase family (PIKK)	21
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	20
Ultrasound promoted green synthesis, anticancer evaluation, and molecular docking studies of hydrazines: a pilot trial	20
Design, synthesis and antitumor activity of 5-trifluoromethylpyrimidine derivatives as EGFR inhibitors	20
Discovery of novel thiazolyl-pyrazolines as dual EGFR and VEGFR-2 inhibitors endowed with in vitro antitumor activity towards non-small lung cancer	20
Towards safer anti-inflammatory therapy: synthesis of new thymol–pyrazole hybrids as dual COX-2/5-LOX inhibitors	19
Novel benzo chromene derivatives: design, synthesis, molecular docking, cell cycle arrest, and apoptosis induction in human acute myeloid leukemia HL-60 cells	19
Design, synthesis, and biological evaluation of (thio)urea derivatives as potent Escherichia coli β -glucuronidase inhibitors	19

Phosphorus containing analogues of SAHA as inhibitors of HDACs	19
Identification of potential inhibitors against Staphylococcus aureus shikimate dehydrogenase through virtual screening and susceptibility test	19
Mixed and non-competitive enzyme inhibition: underlying mechanisms and mechanistic irrelevance of the formal two-site model	19
Design, synthesis and antitumor evaluation of novel pyrazolo[3,4- d ]pyrimidines incorporating different amino acid conjugates as potential DHFR inhibitors	19
A method for the efficient evaluation of substrate-based cholinesterase imaging probes for Alzheimer’s disease	18
Inhibitory effects of sulfenimides on human and bovine carbonic anhydrase enzymes	18
Biotin conjugates in targeted drug delivery: is it mediated by a biotin transporter, a yet to be identified receptor, or (an)other unknown mechanism(s)?	18
Synthesis and bioactivities evaluation of oleanolic acid oxime ester derivatives as α-glucosidase and α-amylase inhibitors	18
Development of certain benzylidene coumarin derivatives as anti-prostate cancer agents targeting EGFR and PI3Kβ kinases	18
Design and synthesis of novel rigid dibenzo[ b,f ]azepines through ring closure technique as promising anticancer candidates against leukaemia and acting as selective to	17
Inhibition of pathogenic bacterial carbonic anhydrases by monothiocarbamates	17
Design, synthesis, and antitumor efficacy of novel 5-deazaflavin derivatives backed by kinase screening, docking, and ADME studies	17
2-Arylquinolines as novel anticancer agents with dual EGFR/FAK kinase inhibitory activity: synthesis, biological evaluation, and molecular modelling insights	17
Discovery of a selective PI3Kα inhibitor via structure-based virtual screening for targeted colorectal cancer therapy	17
Biological evaluation, docking studies, and in silico ADME prediction of some pyrimidine and pyridine derivatives as potential EGFR ^WT	17
Synthesis, biological evaluation and theoretical studies of ( E )-1-(4-sulfamoyl-phenylethyl)-3-arylidene-5-aryl-1H-pyrrol-2(3H)-ones as human carbonic anhydrase inhibit	16
Benzoxazole derivatives as new VEGFR-2 inhibitors and apoptosis inducers: design, synthesis, in silico studies, and antiproliferative evaluation	16
Dasatinib ameliorates thioacetamide-induced liver fibrosis: modulation of miR-378 and miR-17 and their linked Wnt/β-catenin and TGF-β/smads pathways	16
Indirubin-3′-oxime as a dual-action agent: mitigating heat-induced male infertility in Drosophila melanogaster and inhibiting soluble epoxide hydrolase	16
Correction	16
Effect of in vitro simulated digestion on the anti- Helicobacter Pylori activity of different Propolis extracts	16
Development of novel 9-O-substituted-13-octylberberine derivatives as potential anti-hepatocellular carcinoma agents	16
From the Wuhan-Hu-1 strain to the XD and XE variants: is targeting the SARS-CoV-2 spike protein still a pharmaceutically relevant option against COVID-19?	15
Predicting potentially pathogenic effects of hRPE65 missense mutations: a computational strategy based on molecular dynamics simulations	15
Evaluation of N -alkyl isatins and indoles as acetylcholinesterase and butyrylcholinesterase inhibitors	15
In-cell bioluminescence resonance energy transfer (BRET)-based assay uncovers ceritinib and CA-074 as SARS-CoV-2 papain-like protease inhibitors	15
Synthesis, molecular modelling and QSAR study of new N-phenylacetamide-2-oxoindole benzensulfonamide conjugates as carbonic anhydrase inhibitors with antiproliferative activity	15
Dentine biomodification by sulphonamides pre-treatment: bond strength, proteolytic inhibition, and antimicrobial activity	15
Novel dual-targeting inhibitors of NSD2 and HDAC2 for the treatment of liver cancer: structure-based virtual screening, molecular dynamics simulation, and in vitro and	15
Replacing the phthalimide core in thalidomide with benzotriazole	15
Antibacterial action mechanisms and mode of trypsin inhibitors: a systematic review	15
Vitamin B6 inhibits activity of Helicobacter pylori adenylosuccinate synthetase and growth of reference and clinical, antibiotic-resistant H. pylori	15
Correction	15
Reply letter to Dr. Wojtasek regarding: Oxidation of flavonoids by tyrosinase and by o-quinones–comment on "Flavonoids as tyrosinase inhibitors in in silico and	14
Latest advances in dual inhibitors of acetylcholinesterase and monoamine oxidase B against Alzheimer’s disease	14
Comparative chemical and biological hydrolytic stability of homologous esters and isosteres	14
5-(Sulfamoyl)thien-2-yl 1,3-oxazole inhibitors of carbonic anhydrase II with hydrophilic periphery	14
Suppression of lipopolysaccharide-induced COX-2 expression via p38MAPK, JNK, and C/EBPβ phosphorylation inhibition by furomagydarin A, a benzofuran glycoside from Magydaris pastinacea	14
Correction	14
Oxidation of flavonoids by tyrosinase and by o -quinones–comment on "Flavonoids as tyrosinase inhibitors in in silico and i	14
Biological investigation of N-methyl thiosemicarbazones as antimicrobial agents and bacterial carbonic anhydrases inhibitors	14
Synthesis, computational study and biological evaluation of 9-acridinyl and 1-coumarinyl-1,2,3-triazole-4-yl derivatives as topoisomerase II inhibitors	14
Angiogenesis and anti-leukaemia activity of novel indole derivatives as potent colchicine binding site inhibitors	14
Cloning, expression, and purification of an α-carbonic anhydrase from Toxoplasma gondii to unveil its kinetic parameters and anion inhibition profile.	14
Correction	14
Paving the way towards effective plant-based inhibitors of hyaluronidase and tyrosinase: a critical review on a structure–activity relationship	14
Targeting carbonic anhydrase IX and XII isoforms with small molecule inhibitors and monoclonal antibodies	14
Design and synthesis of benzodiazepines as brain penetrating PARP-1 inhibitors	14
Antifungal and anti-biofilm effects of hydrazone derivatives on Candida spp	14
Investigation of the enantioselectivity of acetylcholinesterase and butyrylcholinesterase upon inhibition by tacrine-iminosugar heterodimers	13
Novel hydroxyl carboximates derived from β-elemene: design, synthesis and anti-tumour activities evaluation	13
Structure-activity exploration of a small-molecule allosteric inhibitor of T790M/L858R double mutant EGFR	13
From Antarctica to cancer research: a novel human DNA topoisomerase 1B inhibitor from Antarctic sponge Dendrilla antarctica	13
Isocoumarins: a new class of selective carbonic anhydrase IX and XII inhibitors	13
Structure-guided approach on the role of substitution on amide-linked bipyrazoles and its effect on their anti-inflammatory activity	13
TXNIP inhibition in the treatment of type 2 diabetes mellitus: design, synthesis, and biological evaluation of quinazoline derivatives	13
Discovery of the SHP2 allosteric inhibitor 2-((3R,4R)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl)-5-(2,3-dichlorophenyl)-3-methylpyrrolo[2,1-f][1,2,4] triazin-4(3H)-one	13
Structure-activity relationship studies for inhibitors for vancomycin-resistant Enterococcus and human carbonic anhydrases	13
Discovery of coumaric acid derivatives hinted by coastal marine source to seek for uric acid lowering agents	13
Derivatives of 4-methyl-1,2,3-benzoxathiazine 2,2-dioxide as selective inhibitors of human carbonic anhydrases IX and XII over the cytosolic isoforms I and II	13
4-(3-Alkyl/benzyl-guanidino)benzenesulfonamides as selective carbonic anhydrase VII inhibitors	13