Bioorganic & Medicinal Chemistry Letters

Papers
(The median citation count of Bioorganic & Medicinal Chemistry Letters is 1. 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.)
ArticleCitations
Revisiting the dipeptidyl carboxypeptidase inhibitor captopril as a source of pan anti-trypanosomatid agents159
Design, synthesis and biological evaluation of alginate oligosaccharide derivatives92
Design, synthesis and biological evaluation of tanshinone IIA derivatives as NLRP3 inflammasome inhibitors68
Discovery of DS-1093a: An oral hypoxia-inducible factor prolyl hydroxylase inhibitor for the treatment of renal anemia60
Editorial Board56
Amyloidogenic immunoglobulin light chain kinetic stabilizers comprising a simple urea linker module reveal a novel binding sub-site50
Synthesis and SAR of novel GPR39 agonists and positive allosteric modulators49
Design, synthesis, biological evaluation and molecular modeling of N-isobutyl-N-((2-(p-tolyloxymethyl)thiazol-4yl)methyl)benzo[d][1,3] dioxole-5-carboxamides as selective butyrylcholinesterase inhibit41
Enteroviral replication inhibition by N-Alkyl triazolopyrimidinone derivatives through a non-capsid binding mode40
Graphical Abstract TOC37
Editorial Board35
Synthesis and characterization of chiral 6-azaspiro[2.5]octanes as potent and selective antagonists of the M4 muscarinic acetylcholine receptor33
SARS-CoV-2 papain-like protease (PLpro) inhibitory and antiviral activity of small molecule derivatives for drug leads31
Neuropilin 1-targeted near-infrared fluorescence probes for tumor diagnosis30
Pyrazolo-1-carbothioamides as EGR-1–DNA binding disruptors30
Design, synthesis and characterizations of prodrugs of brexanolone28
Discovery of structural diverse reversible BTK inhibitors utilized to develop a novel in vivo CD69 and CD86 PK/PD mouse model27
Development of a highly potent and selective degrader of LRRK226
Phytochemical investigation of Asarum sieboldii var. seoulense and the phenotypic profiles of its constituents against a Parkinson’s Disease olfactory cell line26
Discovery of TNG-6132, a potent, selective, and orally bioavailable USP1 inhibitor25
Improved synthesis and anticancer activity of a potent neuronal nitric oxide synthase inhibitor25
Design and structural optimization of thiadiazole derivatives with potent GLS1 inhibitory activity25
Epigallocatechin and epigallocatechin-3-gallate are not inhibitors of tyrosinase24
Discovery of a macrocyclic FAK inhibitor GZD-257 for treatment of glioblastoma24
Contents continued24
A concise review on MDM2 inhibitors and recent progress in radiopharmaceutical development for imaging MDM2 expression in tumors with PET or SPECT23
Armeniaspirol analogues disrupt the electrical potential (ΔΨ) of the proton motive force22
Studies on in vitro modulatory effects to base excision repair enzymes induced by small molecule binding to Deaminated CAG repeat hairpin21
4′-O-methoxyethyl-2′-deoxy-uridine and cytidine ribonucleotides improve duplex stability, nuclease resistance, and elicit efficient knockdown of Bcl-2 expression21
Green synthesis and anti-biofilm activities of 3,5-disubstituted isoxazoline/isoxazole-linked secondary sulfonamide derivatives on Pseudomonas aeruginosa21
A fluorescent molecular rotor for the selective detection of the hybrid-conformation 22AG G-Quadruplex21
Synthesis and biological evaluation of novel 1,2,3,4-tetrahydro-β-carboline derivatives as potential antibacterial agents21
New class of fused [3,2-b][1,2,4]triazolothiazoles for targeting glioma in vitro20
A simple yet multifaceted 90 years old, evergreen enzyme: Carbonic anhydrase, its inhibition and activation20
New bis- and tetrakis-1,2,3-triazole derivatives: Synthesis, DNA cleavage, molecular docking, antimicrobial, antioxidant activity and acid dissociation constants20
Recent progress in synthetic strategies to develop potent, HDAC8-selective, small-molecule inhibitors20
Design and evaluation of anaplastic lymphoma kinase degraders using a covalent fumarate handle19
A PSMA-targeted doxorubicin small-molecule drug conjugate19
Contents continued19
Design and synthesis of Tetrahydroindeno[4,5-c]chromen-4(3H)-one derivatives as antiproliferative agents for prostate Cancer cells19
Contents continued19
Synthesis and evaluation of 3-hydroxyquinolin-2(1H)-one derivatives as inhibitors of tyrosinase18
Design, synthesis, and evaluation of 1,3,4-oxadiazole-based EGFR inhibitors18
Contents continued18
Design and activity evaluation of new EGFR tyrosine kinase inhibitors containing cyclic polyamines18
Design, synthesis, and biological evaluation of 5ʹ-deoxy (N)-methanocarbanucleoside derivatives as A3 adenosine receptor ligands17
Discovery and optimization of (2-naphthylthio)acetic acid derivative as selective Bfl-1 inhibitor17
Comparative analysis of p-terphenylquinone and seriniquinone derivatives as reactive oxygen species-modulating agents17
Design, synthesis and biological evaluation of pyrimidine base hydroxamic acid derivatives as dual JMJD3 and HDAC inhibitors17
α-Fluorination of tropane compounds and its impact on physicochemical and ADME properties17
Natural products targeting the NF-κB signaling pathway:Potential therapeutic drug candidates17
Photocrosslinking and capture for the analysis of carbohydrate-dependent interactions17
Structure-activity relationship study of HIF-2α inhibitors with tricyclic scaffold16
Discovery of 3-phenyl-1H-5-pyrazolylamides as PLpro inhibitors through virtual screening and structure optimization16
An overview of cyclopropenone derivatives as promising bioactive molecules16
Graphical abstract TOC16
Biocatalytic synthesis and evaluation of antioxidant and antibacterial activities of hydroxyequols16
PEG-lipid-modified agonistic antibody against tumor necrosis factor receptor family elicits superior apoptosis-inducing activity against human carcinoma16
11C-labeling of 20(S)-protopanaxadiol, an aglycon of ginsenoside, based on the use of Pd(0)-mediated rapid C-[11C]methylation of boronic precursors16
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) 3067–16
Design, synthesis and properties of peptide inhibitors based on BRCA1856-87116
Design and discovery of C2-fluoroalkyl iminothiazine dioxides as BACE inhibitors15
Exploratory study of oxatomide derivatives with high P2X7 receptor inhibitory activity15
Graphical abstract TOC15
Graphical abstract TOC15
Editorial Board15
Discovery of arylsulfonamides as a novel class of allosteric integrase inhibitors with antiviral activity15
Graphical abstract TOC15
Topoisomerase IIα inhibitory and antiproliferative activity of dihydroxylated 2,6-diphenyl-4-fluorophenylpyridines: Design, synthesis, and structure-activity relationships15
Ultrasound-dependent RNAi using TatU1A-rose bengal conjugate14
pH-responsive aggregates consisted of oligodeoxynucleotides bearing nitrophenol group that deliver drugs into acidic cells14
Biological evaluation of newly synthesized α-benzil monoxime thiocarbohydrazide derivatives as an antimicrobial and anticancer agent: In vitro screening and ADMET predictions14
Design, synthesis and biological evaluation of novel cyano-cinnamate derivatives as mitochondrial pyruvate carrier inhibitors14
nTZDpa (non-thiazolidinedione PPARγ partial agonist) derivatives retain antimicrobial activity without improving renal toxicity14
Graphical abstract TOC14
Stereochemical inversion at a 1,4-cyclohexyl PROTAC linker fine-tunes conformation and binding affinity14
Design, synthesis and biological evaluation of pteridine-7(8H)-one derivatives as potent and selective CDK4/6 inhibitors14
Optimisation of momelotinib with improved potency and efficacy as pan-JAK inhibitor14
A photoactivatable self-localizing ligand with improved photosensitivity for chemo-optogenetic control of protein localization in living cells14
DDD-028: A potent, neuroprotective, non-opioid compound for the treatment of diabetic neuropathy14
Design and synthesis of novel fluorene derivatives as inhibitors of pyruvate dehydrogenase kinase13
Structure-activity relationship of dual inhibitors containing maleimide and imidazole motifs against glutaminyl cyclase and glycogen synthase kinase-3β13
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
Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia13
Synthesis and pharmacological characterization of multiply substituted 2H-chromene derivatives as P2Y6 receptor antagonists13
Pharmacokinetic analysis of 6-O-[18F]FEE for PET imaging of EGFR mutation13
High-yield and high-purity amide bond formation using DMTMM PF6 for DNA-encoded libraries13
Synthesis and evaluation of lipoic acid – donepezil hybrids for Alzheimer’s disease using a straightforward strategy13
Editorial Board13
Rationalizing the binding and α subtype selectivity of synthesized imidazodiazepines and benzodiazepines at GABAA receptors by using molecular docking studies12
Graphical abstract TOC12
Graphical abstract TOC12
Synthesis of dolutegravir derivatives modified by 1,2,3-triazole structure and their anti-inflammatory activity in LPS-induced BV2 cells12
Identification of potent and selective inhibitors of PKR via virtual screening and traditional design12
Graphical abstract TOC12
Design, synthesis and biological evaluation of cajanonic acid A analogues as potent PPAR γ antagonists12
Discovery of N-Ts-3-benzylidene-indolin-2-imines as potent anti-colorectal cancer agents through suppression of the PI3K-AKT pathway12
Phenyl urea based adjuvants for β-lactam antibiotics against methicillin resistant Staphylococcus aureus12
Graphical abstract TOC12
Editorial Board12
(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 depletion12
Design, synthesis, and antitumor activity study of novel oleanolic acid structural derivatives targeting c-Kit12
Neratinib derivative 7A induces apoptosis in colon cancer cells via the p53 pathway12
Contents continued12
Reinvestigation of clopidogrel bioactivation unveils new cytochrome P450-catalyzed thioester cleavage mechanism12
Graphical abstract TOC12
Structure–activity relationship of 2-aminodibenzothiophene pharmacophore and the discovery of aminobenzothiophenes as potent inhibitors of Mycobacterium smegmatis11
Enzymatic reconstitution of salicylate formation in promysalin biosynthesis11
Recent advances and perspectives in therapeutics for mpox11
Design, synthesis and activity evaluation of Hedgehog inhibitor Itraconazole derivatives in A549 cells11
Design, synthesis, and biological evaluation of polyphenol derivatives as DYRK1A inhibitors. The discovery of a potentially promising treatment for Multiple Sclerosis11
Discovery of novel N-(1-benzyl-1H-imidazol-2-yl)amide derivatives as melanocortin 1 receptor agonists11
Design, synthesis and evaluation of clickable photoaffinity probes for nuclear lamins11
Study of the reversal of metallo-β-lactamase-mediated resistance in Gram-negative bacteria by EDTMP11
Discovery and characterization a new collagenase from Hathewaya massiliensis for effective subcutaneous adipolysis11
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
Graphical Abstract Continued11
Syntheses and antitumor activities of neorautenol and shinpterocarpin analogs11
Editorial Board11
Discovery of triazenyl triazoles as Nav1.1 channel blockers for treatment of epilepsy11
A unified “top-down” approach for the synthesis of diverse lead-like molecular scaffolds11
Potent and selective carbonic anhydrase inhibition activities of pyrazolones bearing benzenesulfonamides10
Synthesis of a new series of quinoline/pyridine indole-3-sulfonamide hybrids as selective carbonic anhydrase IX inhibitors10
Investigation of the site 2 pocket of Grp94 with KUNG65 benzamide derivatives10
Design, synthesis, in silico studies, and antiproliferative evaluations of novel indolin-2-one derivatives containing 3-hydroxy-4-pyridinone fragment10
Harnessing dual-mode RIPK1 ligands for cross-species anti-necroptosis inhibitor compounds10
Contents continued10
The Pyrimidinyl Hydrazones: Selective for anti-Cancer cytotoxicity10
Discovery of a potent orally available pyrazolopyridone derivative as a novel selective bromodomain and extra-terminal domain (BET)-first bromodomain (BD1) inhibitor10
Synthesis of substrate peptides incorporating non-natural amino acids and screening study using BACE110
Discovery of novel 4-aminobenzamide derivatives as small molecule CBX2 inhibitors10
Structure-activity relationship of dibenzylideneacetone analogs against the neglected disease pathogen, Trypanosoma brucei10
Improving reactivity of naphthalimide-based GST probe by imparting TPP cation: Development and application for live cell imaging10
A dual aurora and lim kinase inhibitor reduces glioblastoma proliferation and invasion10
Discovery of sinomenine/8-Bis(benzylthio)octanoic acid hybrids as potential anti-leukemia drug candidate via mitochondrial pathway10
Graphical abstract TOC10
A small-molecule pretargeting approach for PSMA-targeted conjugates10
Design, synthesis and antitumor evaluation of a novel nectin-4 targeting bicyclic toxin conjugate10
Development of novel GI-centric prostaglandin E2 receptor type 4 (EP4) agonist prodrugs as treatment for ulcerative colitis and other intestinal inflammatory diseases10
Design, synthesis and evaluation of pterostilbene-indole hybrids as potential anticancer agents10
Design, synthesis and biological evaluation of novel cationic liposomes loaded with melphalan for the treatment of cancer10
Design, synthesis and anti-pneumonic activity evaluation of shikonin ester derivatives10
Direct-to-biology platform: From synthesis to biological evaluation of SHP2 allosteric inhibitors10
6-Aryl-quinazolines as novel GABAB receptor positive allosteric modulators10
Design, synthesis and biological evaluation of novel indole-piperazine derivatives as antibacterial agents10
Synthesis and functional evaluation of tetrahydroisoquinoline and polysubstituted benzylamine derivatives as sigma-2 receptor-targeted small-molecule probes10
Discovery of 3-acyl-2-anilino-1,4-dihydroquinolin-4-one derivatives as potential inhibitors of methicillin-resistant Staphylococcus aureus10
Contents continued10
Genipin derivative induced the apoptosis and inhibited the invasion and migration of A549 cancer cells via regulation of EGFR/JAK1/STAT3 signaling9
Graphical abstract TOC9
Permeation behavior of porphyrin derivatives with different functional group positions across cancer cell membranes9
A guanidinium group is an effective mimic of the tertiary carbocation formed by isopentenyl diphosphate isomerase9
PSMA-targeted SMART molecules outfitted with SN389
Hydrazinecarbonyl-thiazol-2-acetamides with pronounced apoptotic behavior: synthesis, in vitro/in vivo anti-proliferative activity and molecular modeling simulations9
Methyl N-(tert-butoxycarbonyl)pyridine-2-carbimidothioate: A new reagent for the synthesis of N-phenylpyridinecarboxamidine (“arylimidamide”) DNA-minor groove binders from poorly nucleophilic amines9
Editorial Board9
Synthesis of drimanyl indole fragments of drimentine alkaloids and their antibacterial activities9
A small molecule binding to TGGAA pentanucleotide repeats that cause spinocerebellar ataxia type 319
Iodophenyl-conjugated closo-dodecaborate as a promising small boron molecule that binds to serum albumin and accumulates in tumor9
Discovery of a proteolysis targeting chimera (PROTAC) as a potent regulator of FOXP39
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
Imidazo[2,1-b]thiazole based indoleamine-2,3-dioxygenase 1 (IDO1) inhibitor: Structure based design, synthesis, bio-evaluation and docking studies9
Graphical abstract TOC9
Design, synthesis, and biological evaluation of 2,4-diaminopyrimidine inhibitors of hematopoietic progenitor kinase 19
Synthesis, modeling, and biological evaluation of anti-tubulin indole-substituted furanones9
Further structural optimization and SAR study of sungsanpin derivatives as cell-invasion inhibitors9
PES derivative PESA is a potent tool to globally profile cellular targets of PES9
Corrigendum to “Discovery of 4-aminopyrimidine analogs as highly potent dual P70S6K/Akt inhibitors” [Bioorgan. Med. Chem. Lett. 50 (2021) 128352]9
Synthesis of mizoribine prodrugs and their in vivo evaluation as immunosuppressive agents9
Graphical abstract TOC9
Zinc-dependent deacetylases (HDACs) as potential targets for treating Alzheimer’s disease9
Discovery of BI-9787, a potent zwitterionic ketohexokinase inhibitor with oral bioavailability9
Editorial Board9
Synthesis, in vitro cytotoxicity evaluation and mechanism of 5′ monosubstituted chalcone derivatives as antitumor agents9
Cyano-Hydrol green derivatives: Expanding the 9-cyanopyronin-based resonance Raman vibrational palette9
Graphical abstract TOC9
Evaluation of an ester-linked immunosuppressive payload: A case study in understanding the stability and cleavability of ester-containing ADC linkers9
Highly potent anti-inflammatory, analgesic and antioxidant activities of 3,5-disubstituted tetrahydro-2H-1,3,5-thiadiazine thiones9
Synthesis and biological evaluation of biotinylated ZJ-1019
Discovery of a potent and subtype-selective TYK2 degrader based on an allosteric TYK2 inhibitor9
Conversion of oxadiazolo[3,4-b]pyrazines to imidazo[4,5-b]pyrazines via a tandem reduction-cyclization sequence generates new mitochondrial uncouplers9
Contents continued9
Discovery of an ellipticine derivative as TLR3 inhibitor against influenza A virus and SARS-CoV-29
Photo-regulated PROTACs: A novel tool for temporal control of targeted protein degradation9
New diarylpentanoids and chalcones as potential antimicrobial adjuvants9
Design, synthesis, and bioevaluation of SOS1 PROTACs derived from pyrido[2,3-d]pyrimidin-7-one-based SOS1 inhibitor9
Novel drug discovery approaches for MMP-13 inhibitors in the treatment of osteoarthritis9
Graphical Abstract TOC8
Short synthesis of a broadly Reactive, cell permeable serine hydrolase Fluorophosphonate-Alkyne probe8
4-Oxooctahydroquinoline-1(2H)-carboxamides as hepatitis B virus (HBV) capsid core protein assembly modulators8
Discovery of a DCAF11-dependent cyanoacrylamide-containing covalent degrader of BET-proteins8
Diamino variants of piperazine-based tissue transglutaminase inhibitors8
Azolo[5′,1′,2,3]pyrimido[5,4-e]tetrazolo[1,5-c]pyrimidines as dual-action antiglycators and α-glucosidase inhibitors8
The structural modification and biological evaluation of tetrahydrothienopyridine derivatives as selective BChE inhibitors8
Synthesis and preliminary immunologic properties of di-/trisaccharide-conjugates related to Bacillus anthracis8
An ascidian Polycarpa aurata-derived pan-inhibitor against coronaviruses targeting Mpro8
Graphical Abstract TOC8
Contents continued8
Synthesis and properties of PNA containing a dicationic nucleobase based on N4-benzoylated cytosine8
Exploration of inhibitors of the bacterial LexA repressor-protease8
Graphical abstract TOC8
Synthesis and evaluation of catecholamine derivatives as amyloid-beta aggregation inhibitors8
Sensitive and reliable gastric ulcer related MicroRNA detection by bridge catalytic hairpin assembly (bCHA) mediated primer exchange reaction8
Discovery of acyl ureas as highly selective small molecule CSF1R kinase inhibitors8
Novel imidazo[1,5-a]quinoxaline derivatives: SAR, selectivity and modeling challenges en route to the identification of an α5-GABAA receptor NAM8
Editorial Board8
Design, synthesis and antitumor activity of novel 4-oxobutanamide derivatives8
Graphical Abstract Contents Continued8
Graphical abstract TOC8
Synthesis and antitumor activity of a series of novel N-aryl-5-(2,2,2-trifluoroethoxy)-1,5-dihydro-2H-pyrrol-2-ones derivatives8
Design, synthesis and biological evaluation of sulfonylurea derivatives as NLRP3 inflammasome inhibitors8
Graphical abstract TOC8
Design of cyclic peptides as novel inhibitors of ICOS/ICOSL interaction8
Thiamine analogues featuring amino-oxetanes as potent and selective inhibitors of pyruvate dehydrogenase8
Synthesis of proposed structure of ledebourin A8
Multigram-scale total synthesis of (±)-ambreinolide by a diastereoselective polyene cyclization8
5-Fluoro-2′-deoxyuridine as an efficient 19F NMR reporter for G-quadruplex and i-motif structures8
SAR study of niclosamide derivatives for neuroprotective function in SH-SY5Y neuroblastoma8
Synthesis, radiolabeling, and evaluation of a potent β-site APP cleaving enzyme (BACE1) inhibitor for PET imaging of BACE1 in vivo7
Design of a ROS-responsive fluorescent probe for the diagnosis and imaging of breast cancer7
Editorial Board7
Expanded library of novel 2,3-pyrrolidinedione analogues exhibit anti-biofilm activity7
Inhibitors for metallo-β-lactamases from the B1 and B3 subgroups provide an avenue to combat a major mechanism of antibiotic resistance7
Design and synthesis of novel orexin 2 receptor agonists based on naphthalene skeleton7
Structure-activity relationship study of antitrypanosomal analogues of gibbilimbol B using multivariate analysis and computation-aided drug design7
Graphical abstract TOC7
Discovery of PFI-6, a small-molecule chemical probe for the YEATS domain of MLLT1 and MLLT37
Discovery of EP300/CBP histone acetyltransferase inhibitors through scaffold hopping of 1,4-oxazepane ring7
Rational design, synthesis, antiproliferative activity against MCF-7, MDA-MB-231 cells, estrogen receptors binding affinity, and computational study of indenopyrimidine-2,5-dione analogs for the treat7
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 novel aminopyrimidine derivatives as EGFR inhibitors7
Fragment-based discovery of novel phenyltriazolyl derivatives as allosteric type-I1/2 ALK inhibitors with promising antitumor effects7
The potential of Rhein's aromatic amines for Parkinson's disease prevention and treatment: α-Synuclein aggregation inhibition and disaggregation of preformed fibers7
Development of chromone-thiazolidine-2,4-dione Knoevenagel conjugates as apoptosis inducing agents7
Design, synthesis, and activity evaluation of Asiatic acid derivatives as Survivin inhibitors7
A FOXC2 inhibitor, MC-1-F2, as a therapeutic candidate for targeting EMT in castration-resistant prostate cancer7
Conformationally constrained potent inhibitors for enhancer of zeste homolog 2 (EZH2)7
Design, synthesis and antifungal activities of novel triazole derivatives with selenium-containing hydrophobic side chains7
Discovery of L15 as a novel Vif PROTAC degrader with antiviral activity against HIV-17
Synthesis and biological evaluation of novel 18F-labeled 2,4-diaminopyrimidine derivatives for detection of ghrelin receptor in the brain7
Siderophores: Chemical tools for precise antibiotic delivery7
Editorial Board7
Editorial Board7
Novel detection method for gallic acid: A water soluble boronic acid-based fluorescent sensor with double recognition sites7
Design, synthesis, and biological evaluation of novel HDAC inhibitors with a 3-(benzazol-2-yl)quinoxaline framework7
Graphical abstract TOC7
Graphical Abstract Contents Continued7
Editorial Board7
Discovery of benzimidazole-2-amide BNZ-111 as new tubulin inhibitor7
Identification of sugar-containing natural products that interact with i-motif DNA7
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