Bioorganic & Medicinal Chemistry Letters

Papers
(The median citation count of Bioorganic & Medicinal Chemistry Letters is 2. 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 2022-06-01 to 2026-06-01.)
ArticleCitations
Editorial Board108
Pyrazolo-1-carbothioamides as EGR-1–DNA binding disruptors75
Discovery of TNG-6132, a potent, selective, and orally bioavailable USP1 inhibitor56
Armeniaspirol analogues disrupt the electrical potential (ΔΨ) of the proton motive force52
Graphical Abstract TOC44
Editorial Board39
Neuropilin 1-targeted near-infrared fluorescence probes for tumor diagnosis37
Contents continued34
Synthesis and biological evaluation of novel 1,2,3,4-tetrahydro-β-carboline derivatives as potential antibacterial agents33
Studies on in vitro modulatory effects to base excision repair enzymes induced by small molecule binding to Deaminated CAG repeat hairpin30
Design, synthesis and biological evaluation of alginate oligosaccharide derivatives30
Design and evaluation of anaplastic lymphoma kinase degraders using a covalent fumarate handle30
Discovery of multitargeting single agents as a novel route to the potential treatment of neurodegenerative diseases29
SARS-CoV-2 papain-like protease (PLpro) inhibitory and antiviral activity of small molecule derivatives for drug leads27
Design and synthesis of Tetrahydroindeno[4,5-c]chromen-4(3H)-one derivatives as antiproliferative agents for prostate Cancer cells27
Phytochemical investigation of Asarum sieboldii var. seoulense and the phenotypic profiles of its constituents against a Parkinson’s Disease olfactory cell line26
Discovery of DS-1093a: An oral hypoxia-inducible factor prolyl hydroxylase inhibitor for the treatment of renal anemia26
Epigallocatechin and epigallocatechin-3-gallate are not inhibitors of tyrosinase26
Improved synthesis and anticancer activity of a potent neuronal nitric oxide synthase inhibitor25
Revisiting the dipeptidyl carboxypeptidase inhibitor captopril as a source of pan anti-trypanosomatid agents25
New class of fused [3,2-b][1,2,4]triazolothiazoles for targeting glioma in vitro24
Discovery of structural diverse reversible BTK inhibitors utilized to develop a novel in vivo CD69 and CD86 PK/PD mouse model24
Synthesis and evaluation of novel oxanthrene scaffold-derived oxazolidinone antibiotics with potent antitubercular activity and low cellular toxicity24
Green synthesis and anti-biofilm activities of 3,5-disubstituted isoxazoline/isoxazole-linked secondary sulfonamide derivatives on Pseudomonas aeruginosa24
Development of a highly potent and selective degrader of LRRK223
Recent progress in synthetic strategies to develop potent, HDAC8-selective, small-molecule inhibitors23
Design, synthesis and characterizations of prodrugs of brexanolone23
4′-O-methoxyethyl-2′-deoxy-uridine and cytidine ribonucleotides improve duplex stability, nuclease resistance, and elicit efficient knockdown of Bcl-2 expression22
Discovery of a macrocyclic FAK inhibitor GZD-257 for treatment of glioblastoma22
A PSMA-targeted doxorubicin small-molecule drug conjugate22
Design, synthesis and biological evaluation of tanshinone IIA derivatives as NLRP3 inflammasome inhibitors21
Design and structural optimization of thiadiazole derivatives with potent GLS1 inhibitory activity21
A simple yet multifaceted 90 years old, evergreen enzyme: Carbonic anhydrase, its inhibition and activation21
Contents continued20
A concise review on MDM2 inhibitors and recent progress in radiopharmaceutical development for imaging MDM2 expression in tumors with PET or SPECT20
Contents continued20
Design and activity evaluation of new EGFR tyrosine kinase inhibitors containing cyclic polyamines20
Contents continued20
Design, synthesis, and biological evaluation of 5ʹ-deoxy (N)-methanocarbanucleoside derivatives as A3 adenosine receptor ligands19
Photocrosslinking and capture for the analysis of carbohydrate-dependent interactions19
Design, synthesis, and biological evaluation of cytochrome P450 CYP11A1 inhibitors18
Combined antitumor efficacy of a new tanshinone IIA analog and irinotecan with alleviating gastrointestinal side effect18
PEG-lipid-modified agonistic antibody against tumor necrosis factor receptor family elicits superior apoptosis-inducing activity against human carcinoma17
α-Fluorination of tropane compounds and its impact on physicochemical and ADME properties17
Synthesis and evaluation of 3-hydroxyquinolin-2(1H)-one derivatives as inhibitors of tyrosinase17
Discovery of 3-phenyl-1H-5-pyrazolylamides as PLpro inhibitors through virtual screening and structure optimization17
Design, synthesis and properties of peptide inhibitors based on BRCA1856-87117
11C-labeling of 20(S)-protopanaxadiol, an aglycon of ginsenoside, based on the use of Pd(0)-mediated rapid C-[11C]methylation of boronic precursors17
Design and synthesis of novel fluorene derivatives as inhibitors of pyruvate dehydrogenase kinase16
DDD-028: A potent, neuroprotective, non-opioid compound for the treatment of diabetic neuropathy16
Graphical abstract TOC16
Biocatalytic synthesis and evaluation of antioxidant and antibacterial activities of hydroxyequols16
Exploratory study of oxatomide derivatives with high P2X7 receptor inhibitory activity16
Design, synthesis and biological evaluation of pyrimidine base hydroxamic acid derivatives as dual JMJD3 and HDAC inhibitors16
Graphical abstract TOC16
Editorial Board16
Graphical abstract TOC15
Ultrasound-dependent RNAi using TatU1A-rose bengal conjugate15
Optimisation of momelotinib with improved potency and efficacy as pan-JAK inhibitor15
Graphical abstract TOC15
Design, synthesis and biological evaluation of pteridine-7(8H)-one derivatives as potent and selective CDK4/6 inhibitors15
A photoactivatable self-localizing ligand with improved photosensitivity for chemo-optogenetic control of protein localization in living cells15
Design, synthesis, and activity evaluation of RET protein degradation based on PROTAC and HyTTD techniques14
Synthesis and pharmacological characterization of multiply substituted 2H-chromene derivatives as P2Y6 receptor antagonists14
Natural products targeting the NF-κB signaling pathway:Potential therapeutic drug candidates14
Lysine-reactive tag system for cell-surface protein labeling via N-acyl-N-alkyl sulfonamide chemistry14
Design, synthesis and biological evaluation of novel cyano-cinnamate derivatives as mitochondrial pyruvate carrier inhibitors14
Design, synthesis, and evaluation of 1,3,4-oxadiazole-based EGFR inhibitors14
Discovery and optimization of 2,3-Dihydroindole derivatives as STING receptor allosteric agonists14
Discovery of arylsulfonamides as a novel class of allosteric integrase inhibitors with antiviral activity14
An overview of cyclopropenone derivatives as promising bioactive molecules14
Structure-based discovery of sulfamoyl-ethyl-4-oxo-3,4-dihydro-7H-pyrrolo[2,3-d]pyrimidine amides and sulfonamides as potent B-Cell Lymphoma 6 (BCL6)-BTB inhibitors14
Stereochemical inversion at a 1,4-cyclohexyl PROTAC linker fine-tunes conformation and binding affinity14
High-yield and high-purity amide bond formation using DMTMM PF6 for DNA-encoded libraries14
Synthesis and evaluation of lipoic acid – donepezil hybrids for Alzheimer’s disease using a straightforward strategy14
Discovery and optimization of (2-naphthylthio)acetic acid derivative as selective Bfl-1 inhibitor13
Pharmacokinetic analysis of 6-O-[18F]FEE for PET imaging of EGFR mutation13
Graphical abstract TOC13
Structure-activity relationship of dual inhibitors containing maleimide and imidazole motifs against glutaminyl cyclase and glycogen synthase kinase-3β13
Neratinib derivative 7A induces apoptosis in colon cancer cells via the p53 pathway13
Comparative analysis of p-terphenylquinone and seriniquinone derivatives as reactive oxygen species-modulating agents13
Biological evaluation of newly synthesized α-benzil monoxime thiocarbohydrazide derivatives as an antimicrobial and anticancer agent: In vitro screening and ADMET predictions13
Structure-activity relationship study of HIF-2α inhibitors with tricyclic scaffold13
(E)-3-(3-([1,1′-Biphenyl]-4-yl)-1-phenyl-1H-pyrazol-4-yl)-1-phenylprop-2-en-1-ones inducing reactive oxygen species generation through glutathione depletion13
Discovery of triazenyl triazoles as Nav1.1 channel blockers for treatment of epilepsy13
Retraction notice to “Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities” [Bioorg. Med. Chem. Lett. 22(9) (2012) 3067–13
Rational design, synthesis and biological evaluation of novel HIV-1 protease inhibitors containing 2-phenylacetamide derivatives as P2 ligands with potent activity against DRV-Resistant HIV-1 variants13
Editorial Board13
Discovery of sinomenine/8-Bis(benzylthio)octanoic acid hybrids as potential anti-leukemia drug candidate via mitochondrial pathway13
Graphical abstract TOC13
Identification of potent and selective inhibitors of PKR via virtual screening and traditional design12
Graphical abstract TOC12
Graphical abstract TOC12
Graphical abstract TOC12
Discovery of novel 4-aminobenzamide derivatives as small molecule CBX2 inhibitors12
Design, synthesis and biological evaluation of cajanonic acid A analogues as potent PPAR γ antagonists12
Graphical abstract TOC12
Editorial Board12
6-Aryl-quinazolines as novel GABAB receptor positive allosteric modulators12
Design, synthesis, in silico studies, and antiproliferative evaluations of novel indolin-2-one derivatives containing 3-hydroxy-4-pyridinone fragment12
Editorial Board12
Strengths and limitations of Ba/F3 cells in modelling FLT3-driven AML resistance12
Contents continued12
Syntheses and antitumor activities of neorautenol and shinpterocarpin analogs12
Structure-activity relationship of dibenzylideneacetone analogs against the neglected disease pathogen, Trypanosoma brucei12
Design, synthesis, and antitumor activity study of novel oleanolic acid structural derivatives targeting c-Kit11
Synthesis of a tricyclic hexapeptide –via two consecutive ruthenium-catalyzed macrocyclization steps– with a constrained topology to mimic vancomycin's binding properties toward D-Ala-D-Ala dipeptide11
Improving reactivity of naphthalimide-based GST probe by imparting TPP cation: Development and application for live cell imaging11
Synthesis of a new series of quinoline/pyridine indole-3-sulfonamide hybrids as selective carbonic anhydrase IX inhibitors11
Enzymatic reconstitution of salicylate formation in promysalin biosynthesis11
Design, synthesis and evaluation of pterostilbene-indole hybrids as potential anticancer agents11
Reinvestigation of clopidogrel bioactivation unveils new cytochrome P450-catalyzed thioester cleavage mechanism11
Discovery of novel N-(1-benzyl-1H-imidazol-2-yl)amide derivatives as melanocortin 1 receptor agonists11
Synthesis of dolutegravir derivatives modified by 1,2,3-triazole structure and their anti-inflammatory activity in LPS-induced BV2 cells11
Discovery and characterization a new collagenase from Hathewaya massiliensis for effective subcutaneous adipolysis11
Phenyl urea based adjuvants for β-lactam antibiotics against methicillin resistant Staphylococcus aureus11
Design, synthesis and activity evaluation of Hedgehog inhibitor Itraconazole derivatives in A549 cells11
Discovery of N-Ts-3-benzylidene-indolin-2-imines as potent anti-colorectal cancer agents through suppression of the PI3K-AKT pathway11
Potent and selective carbonic anhydrase inhibition activities of pyrazolones bearing benzenesulfonamides11
Investigation of the site 2 pocket of Grp94 with KUNG65 benzamide derivatives11
Design, synthesis and biological evaluation of novel cationic liposomes loaded with melphalan for the treatment of cancer11
Direct-to-biology platform: From synthesis to biological evaluation of SHP2 allosteric inhibitors11
Exploration of imidazothiazole and imidazopyrimidine carboxamides for enhanced antitubercular activity11
Recent advances and perspectives in therapeutics for mpox11
Editorial Board10
Synthesis and functional evaluation of tetrahydroisoquinoline and polysubstituted benzylamine derivatives as sigma-2 receptor-targeted small-molecule probes10
Contents continued10
Design, synthesis and evaluation of clickable photoaffinity probes for nuclear lamins10
Hydrazinecarbonyl-thiazol-2-acetamides with pronounced apoptotic behavior: synthesis, in vitro/in vivo anti-proliferative activity and molecular modeling simulations10
A guanidinium group is an effective mimic of the tertiary carbocation formed by isopentenyl diphosphate isomerase10
Permeation behavior of porphyrin derivatives with different functional group positions across cancer cell membranes10
Graphical abstract TOC10
Discovery of a proteolysis targeting chimera (PROTAC) as a potent regulator of FOXP310
The Pyrimidinyl Hydrazones: Selective for anti-Cancer cytotoxicity10
Design, synthesis and anti-pneumonic activity evaluation of shikonin ester derivatives10
Synthesis and biological evaluation of biotinylated ZJ-10110
PSMA-targeted SMART molecules outfitted with SN3810
Synthesis, modeling, and biological evaluation of anti-tubulin indole-substituted furanones10
Graphical abstract TOC10
A small molecule binding to TGGAA pentanucleotide repeats that cause spinocerebellar ataxia type 3110
Discovery of a potent orally available pyrazolopyridone derivative as a novel selective bromodomain and extra-terminal domain (BET)-first bromodomain (BD1) inhibitor10
Contents continued10
Study of the reversal of metallo-β-lactamase-mediated resistance in Gram-negative bacteria by EDTMP10
Graphical abstract TOC10
Methyl N-(tert-butoxycarbonyl)pyridine-2-carbimidothioate: A new reagent for the synthesis of N-phenylpyridinecarboxamidine (“arylimidamide”) DNA-minor groove binders from poorly nucleophilic amines10
Further structural optimization and SAR study of sungsanpin derivatives as cell-invasion inhibitors10
Graphical abstract TOC10
Cyano-Hydrol green derivatives: Expanding the 9-cyanopyronin-based resonance Raman vibrational palette9
Discovery of a potent and subtype-selective TYK2 degrader based on an allosteric TYK2 inhibitor9
Photo-regulated PROTACs: A novel tool for temporal control of targeted protein degradation9
Genipin derivative induced the apoptosis and inhibited the invasion and migration of A549 cancer cells via regulation of EGFR/JAK1/STAT3 signaling9
Synthesis of triazolopyrimidinone- and imidazotriazinone-based tankyrase inhibitors: Identification of Basroparib (STP1002) as a clinical candidate9
Design, synthesis and antitumor evaluation of a novel nectin-4 targeting bicyclic toxin conjugate9
Evaluation of an ester-linked immunosuppressive payload: A case study in understanding the stability and cleavability of ester-containing ADC linkers9
Synthesis of mizoribine prodrugs and their in vivo evaluation as immunosuppressive agents9
Synthesis, in vitro cytotoxicity evaluation and mechanism of 5′ monosubstituted chalcone derivatives as antitumor agents9
Highly potent anti-inflammatory, analgesic and antioxidant activities of 3,5-disubstituted tetrahydro-2H-1,3,5-thiadiazine thiones9
New diarylpentanoids and chalcones as potential antimicrobial adjuvants9
Discovery of an ellipticine derivative as TLR3 inhibitor against influenza A virus and SARS-CoV-29
Design, synthesis, and bioevaluation of SOS1 PROTACs derived from pyrido[2,3-d]pyrimidin-7-one-based SOS1 inhibitor9
Corrigendum to “Discovery of 4-aminopyrimidine analogs as highly potent dual P70S6K/Akt inhibitors” [Bioorgan. Med. Chem. Lett. 50 (2021) 128352]9
Discovery of 3-acyl-2-anilino-1,4-dihydroquinolin-4-one derivatives as potential inhibitors of methicillin-resistant Staphylococcus aureus9
Development of novel GI-centric prostaglandin E2 receptor type 4 (EP4) agonist prodrugs as treatment for ulcerative colitis and other intestinal inflammatory diseases9
A potent and selective RORγ inhibitor for the treatment of autoimmune diseases9
Conversion of oxadiazolo[3,4-b]pyrazines to imidazo[4,5-b]pyrazines via a tandem reduction-cyclization sequence generates new mitochondrial uncouplers9
Zinc-dependent deacetylases (HDACs) as potential targets for treating Alzheimer’s disease9
Imidazo[2,1-b]thiazole based indoleamine-2,3-dioxygenase 1 (IDO1) inhibitor: Structure based design, synthesis, bio-evaluation and docking studies9
Design, synthesis and biological evaluation of novel indole-piperazine derivatives as antibacterial agents9
Synthesis of esters and amides of 2-aryl-1-hydroxy-4-methyl-1H-imidazole-5-carboxylic acids and study of their antiviral activity against orthopoxviruses9
Discovery of BI-9787, a potent zwitterionic ketohexokinase inhibitor with oral bioavailability9
A small-molecule pretargeting approach for PSMA-targeted conjugates9
Iodophenyl-conjugated closo-dodecaborate as a promising small boron molecule that binds to serum albumin and accumulates in tumor9
Synthesis of substrate peptides incorporating non-natural amino acids and screening study using BACE19
Harnessing dual-mode RIPK1 ligands for cross-species anti-necroptosis inhibitor compounds9
Design, synthesis, and biological evaluation of 2,4-diaminopyrimidine inhibitors of hematopoietic progenitor kinase 19
Exploration of inhibitors of the bacterial LexA repressor-protease8
SAR study of niclosamide derivatives for neuroprotective function in SH-SY5Y neuroblastoma8
Novel imidazo[1,5-a]quinoxaline derivatives: SAR, selectivity and modeling challenges en route to the identification of an α5-GABAA receptor NAM8
Graphical abstract TOC8
Graphical Abstract TOC8
Development of chromone-thiazolidine-2,4-dione Knoevenagel conjugates as apoptosis inducing agents8
Synthesis and preliminary immunologic properties of di-/trisaccharide-conjugates related to Bacillus anthracis8
Editorial Board8
5-Fluoro-2′-deoxyuridine as an efficient 19F NMR reporter for G-quadruplex and i-motif structures8
Design, synthesis and evaluation of the Brigatinib analogues as potent inhibitors against tertiary EGFR mutants (EGFRdel19/T790M/C797S and EGFRL858R/T790M/C797S)8
Synthesis, antiproliferative activity, and biological profiling of C-19 trityl and silyl ether andrographolide analogs in colon cancer and breast cancer cells8
Design, synthesis, and antibacterial activity evaluation of tryptanthrin derivatives8
Design, synthesis, and activity evaluation of Asiatic acid derivatives as Survivin inhibitors8
Synthesis and antitumor activity of a series of novel N-aryl-5-(2,2,2-trifluoroethoxy)-1,5-dihydro-2H-pyrrol-2-ones derivatives8
Multifaceted roles of HDAC7 in disease and the evolving chemical toolkit for its modulation8
Graphical Abstract Contents Continued8
Diamino variants of piperazine-based tissue transglutaminase inhibitors8
Contents continued8
Contents continued8
Thiamine analogues featuring amino-oxetanes as potent and selective inhibitors of pyruvate dehydrogenase8
Novel drug discovery approaches for MMP-13 inhibitors in the treatment of osteoarthritis8
Graphical abstract TOC8
Synthesis and evaluation of catecholamine derivatives as amyloid-beta aggregation inhibitors8
Design, synthesis, and biological evaluation of novel HDAC inhibitors with a 3-(benzazol-2-yl)quinoxaline framework8
Sensitive and reliable gastric ulcer related MicroRNA detection by bridge catalytic hairpin assembly (bCHA) mediated primer exchange reaction8
Synthesis of proposed structure of ledebourin A8
Design, synthesis and antitumor activity of novel 4-oxobutanamide derivatives8
The structural modification and biological evaluation of tetrahydrothienopyridine derivatives as selective BChE inhibitors8
Discovery of novel imidazo[4,5-b]pyridine derivatives as noncovalent reversible Bruton’s tyrosine kinase inhibitors8
Graphical Abstract TOC8
Short synthesis of a broadly Reactive, cell permeable serine hydrolase Fluorophosphonate-Alkyne probe8
Graphical abstract TOC8
Discovery of acyl ureas as highly selective small molecule CSF1R kinase inhibitors8
Synthesis of drimanyl indole fragments of drimentine alkaloids and their antibacterial activities8
Graphical abstract TOC8
Editorial Board8
Multigram-scale total synthesis of (±)-ambreinolide by a diastereoselective polyene cyclization8
Targeted design, synthesis, molecular simulation, ADME-T and in-vitro anticancer assessment of phenyl-substituted-thioxo-tetrahydro-pyrimidin-benzenesulfonamide derivatives as potential BRAFV600E/WT i8
Azolo[5′,1′,2,3]pyrimido[5,4-e]tetrazolo[1,5-c]pyrimidines as dual-action antiglycators and α-glucosidase inhibitors7
Discovery of the potent covalent inhibitor with an acrylate warhead for SARS-CoV-2 3CL protease7
A FOXC2 inhibitor, MC-1-F2, as a therapeutic candidate for targeting EMT in castration-resistant prostate cancer7
Thermal treatment affects aptamers’ structural profiles7
Editorial Board7
Fragment-based discovery of novel phenyltriazolyl derivatives as allosteric type-I1/2 ALK inhibitors with promising antitumor effects7
Lipid bilayer membrane permeability mechanism of the K-Ras(G12D)-inhibitory bicyclic peptide KS-58 elucidated by molecular dynamics simulations7
Modification of the phenyl ring B of phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates by pyridinyl moiety leads to novel antimitotics targeting the colchicine-binding site7
Siderophores: Chemical tools for precise antibiotic delivery7
Discovery of EP300/CBP histone acetyltransferase inhibitors through scaffold hopping of 1,4-oxazepane ring7
Inhibitors for metallo-β-lactamases from the B1 and B3 subgroups provide an avenue to combat a major mechanism of antibiotic resistance7
The association between oxidized low-density lipoprotein and cancer: An emerging targeted therapeutic approach?7
Diffusion of 1O2 along the PNA backbone diminishes the efficiency of photooxidation of PNA/DNA duplexes by biphenyl photosensitizer7
Synthesis and properties of PNA containing a dicationic nucleobase based on N4-benzoylated cytosine7
Discovery of L15 as a novel Vif PROTAC degrader with antiviral activity against HIV-17
Conformationally constrained potent inhibitors for enhancer of zeste homolog 2 (EZH2)7
A self-assembling peptide platform enables plasma membrane protein degradation7
Editorial Board7
Graphical abstract TOC7
Discovery of 5-methyl-1H-benzo[d]imidazole derivatives as novel P2X3 Receptor antagonists7
Discovery of PFI-6, a small-molecule chemical probe for the YEATS domain of MLLT1 and MLLT37
Discovery of benzimidazole-2-amide BNZ-111 as new tubulin inhibitor7
Graphical abstract TOC7
Inhibition of glutathione S-transferases by photoactive calix[4]arene α-ketophosphonic acids7
Graphical abstract TOC7
Discovery of 4-((quinolin-8-ylthio)methyl)benzamide derivatives as a new class of SARS-CoV-2 nsp13 inhibitors7
Design, synthesis and biological evaluation of sulfonylurea derivatives as NLRP3 inflammasome inhibitors7
The potential of Rhein's aromatic amines for Parkinson's disease prevention and treatment: α-Synuclein aggregation inhibition and disaggregation of preformed fibers7
An ascidian Polycarpa aurata-derived pan-inhibitor against coronaviruses targeting Mpro7
Identification of sugar-containing natural products that interact with i-motif DNA7
Synthesis and analysis of novel catecholic ligands as inhibitors of catechol-O-methyltransferase7
A conformationally-locked p-hydroxybenzylidene imidazolinone derivative for detecting Aβ42 aggregation7
Identification of small molecule activators targeting TYK2 pseudokinase domain7
Structure-activity relationship study of antitrypanosomal analogues of gibbilimbol B using multivariate analysis and computation-aided drug design7
Split luciferase-based estimation of cytosolic cargo concentration delivered intracellularly via attenuated cationic amphiphilic lytic peptides7
Identification of (−)-Epigallocateshin gallate derivatives promoting innate immune activation via 2′,3′-cyclic GMP-AMP-stimulator of interferon genes pathway7
Stanolone-1,2,3-Triazole derivatives: Synthesis, DNA damage in tumor cells and anti-prostate Cancer activity study7
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