Bioorganic & Medicinal Chemistry Letters

Papers
(The TQCC of Bioorganic & Medicinal Chemistry Letters is 5. 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 2021-08-01 to 2025-08-01.)
ArticleCitations
Design, synthesis and biological evaluation of alginate oligosaccharide derivatives154
Amyloidogenic immunoglobulin light chain kinetic stabilizers comprising a simple urea linker module reveal a novel binding sub-site77
Design, synthesis and biological evaluation of tanshinone IIA derivatives as NLRP3 inflammasome inhibitors73
Enteroviral replication inhibition by N-Alkyl triazolopyrimidinone derivatives through a non-capsid binding mode58
Revisiting the dipeptidyl carboxypeptidase inhibitor captopril as a source of pan anti-trypanosomatid agents54
Novel carbohydrate-based sulfonamide derivatives as selective carbonic anhydrase II inhibitors: Synthesis, biological and molecular docking analysis46
Editorial Board45
Synthesis and biological evaluation of novel 1,2,3,4-tetrahydro-β-carboline derivatives as potential antibacterial agents43
Synthesis and SAR of novel GPR39 agonists and positive allosteric modulators40
Design of 99mTc-labeled zinc-chelating imaging probe for SPECT imaging of the pancreas39
Discovery of structural diverse reversible BTK inhibitors utilized to develop a novel in vivo CD69 and CD86 PK/PD mouse model38
Graphical Abstract TOC34
Studies on in vitro modulatory effects to base excision repair enzymes induced by small molecule binding to Deaminated CAG repeat hairpin32
Discovery of 3-amino-4-{(3S)-3-[(2-ethoxyethoxy)methyl]piperidin-1-yl}thieno[2,3-b]pyridine-2-carboxamide (DS96432529): A potent and orally active bone anabolic agent31
Editorial Board31
Editorial Board31
Non-alkylator anti-glioblastoma agents induced cell cycle G2/M arrest and apoptosis: Design, in silico physicochemical and SAR studies of 2-aminoquinoline-3-carboxamides30
Green synthesis and anti-biofilm activities of 3,5-disubstituted isoxazoline/isoxazole-linked secondary sulfonamide derivatives on Pseudomonas aeruginosa30
New class of fused [3,2-b][1,2,4]triazolothiazoles for targeting glioma in vitro30
Development of a highly potent and selective degrader of LRRK228
Phytochemical investigation of Asarum sieboldii var. seoulense and the phenotypic profiles of its constituents against a Parkinson’s Disease olfactory cell line27
A fluorescent molecular rotor for the selective detection of the hybrid-conformation 22AG G-Quadruplex26
Synthesis and characterization of chiral 6-azaspiro[2.5]octanes as potent and selective antagonists of the M4 muscarinic acetylcholine receptor25
Discovery of novel iminosydnone compounds with insecticidal activities based on the binding mode of triflumezopyrim25
Improved synthesis and anticancer activity of a potent neuronal nitric oxide synthase inhibitor24
Design and evaluation of anaplastic lymphoma kinase degraders using a covalent fumarate handle24
Contents continued23
Epigallocatechin and epigallocatechin-3-gallate are not inhibitors of tyrosinase23
Design, synthesis and characterizations of prodrugs of brexanolone22
Discovery of TNG-6132, a potent, selective, and orally bioavailable USP1 inhibitor22
Armeniaspirol analogues disrupt the electrical potential (ΔΨ) of the proton motive force22
Discovery of quinuclidine modulators of cellular progranulin22
The ester derivatives obtained by C-ring modification of podophyllotoxin induce apoptosis and inhibited proliferation in PC-3M cells via down-regulation of PI3K/Akt signaling pathway21
A PSMA-targeted doxorubicin small-molecule drug conjugate21
SARS-CoV-2 papain-like protease (PLpro) inhibitory and antiviral activity of small molecule derivatives for drug leads21
Pyrazolo-1-carbothioamides as EGR-1–DNA binding disruptors20
Neuropilin 1-targeted near-infrared fluorescence probes for tumor diagnosis20
Design and structural optimization of thiadiazole derivatives with potent GLS1 inhibitory activity20
New bis- and tetrakis-1,2,3-triazole derivatives: Synthesis, DNA cleavage, molecular docking, antimicrobial, antioxidant activity and acid dissociation constants19
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 inhibit19
A simple yet multifaceted 90 years old, evergreen enzyme: Carbonic anhydrase, its inhibition and activation19
Discovery of DS-1093a: An oral hypoxia-inducible factor prolyl hydroxylase inhibitor for the treatment of renal anemia19
Contents continued18
Contents continued18
Editorial Board18
Topoisomerase IIα inhibitory and antiproliferative activity of dihydroxylated 2,6-diphenyl-4-fluorophenylpyridines: Design, synthesis, and structure-activity relationships17
Graphical abstract TOC17
Graphical abstract TOC17
Pharmacokinetic analysis of 6-O-[18F]FEE for PET imaging of EGFR mutation17
Photocrosslinking and capture for the analysis of carbohydrate-dependent interactions17
Exploratory study of oxatomide derivatives with high P2X7 receptor inhibitory activity17
pH-responsive aggregates consisted of oligodeoxynucleotides bearing nitrophenol group that deliver drugs into acidic cells17
Graphical abstract TOC17
Design, synthesis, and biological evaluation of 5ʹ-deoxy (N)-methanocarbanucleoside derivatives as A3 adenosine receptor ligands17
Graphical abstract TOC17
Graphical abstract TOC17
Design, synthesis and biological evaluation of pteridine-7(8H)-one derivatives as potent and selective CDK4/6 inhibitors17
Discovery of arylsulfonamides as a novel class of allosteric integrase inhibitors with antiviral activity16
Identification and evaluation of 4-anilinoquin(az)olines as potent inhibitors of both dengue virus (DENV) and Venezuelan equine encephalitis virus (VEEV)16
DDD-028: A potent, neuroprotective, non-opioid compound for the treatment of diabetic neuropathy16
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
High-yield and high-purity amide bond formation using DMTMM PF6 for DNA-encoded libraries16
Design and discovery of C2-fluoroalkyl iminothiazine dioxides as BACE inhibitors16
α-Fluorination of tropane compounds and its impact on physicochemical and ADME properties16
Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia16
Design and activity evaluation of new EGFR tyrosine kinase inhibitors containing cyclic polyamines16
Discovery and optimization of (2-naphthylthio)acetic acid derivative as selective Bfl-1 inhibitor16
Biological evaluation of newly synthesized α-benzil monoxime thiocarbohydrazide derivatives as an antimicrobial and anticancer agent: In vitro screening and ADMET predictions16
Optimisation of momelotinib with improved potency and efficacy as pan-JAK inhibitor16
Contents continued16
nTZDpa (non-thiazolidinedione PPARγ partial agonist) derivatives retain antimicrobial activity without improving renal toxicity15
Design, synthesis and biological evaluation of novel cyano-cinnamate derivatives as mitochondrial pyruvate carrier inhibitors15
Ultrasound-dependent RNAi using TatU1A-rose bengal conjugate15
Design, synthesis and properties of peptide inhibitors based on BRCA1856-87115
Biocatalytic synthesis and evaluation of antioxidant and antibacterial activities of hydroxyequols15
An overview of cyclopropenone derivatives as promising bioactive molecules15
PEG-lipid-modified agonistic antibody against tumor necrosis factor receptor family elicits superior apoptosis-inducing activity against human carcinoma15
(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 depletion14
Design and synthesis of novel fluorene derivatives as inhibitors of pyruvate dehydrogenase kinase14
Novel pyridinium-type fullerene derivatives as multitargeting inhibitors of HIV-1 reverse transcriptase, HIV-1 protease, and HCV NS5B polymerase14
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 variants14
Stereochemical inversion at a 1,4-cyclohexyl PROTAC linker fine-tunes conformation and binding affinity14
Synthesis of a new series of quinoline/pyridine indole-3-sulfonamide hybrids as selective carbonic anhydrase IX inhibitors14
Design, synthesis and activity evaluation of Hedgehog inhibitor Itraconazole derivatives in A549 cells14
Design, synthesis and biological evaluation of pyrimidine base hydroxamic acid derivatives as dual JMJD3 and HDAC inhibitors14
Comparative analysis of p-terphenylquinone and seriniquinone derivatives as reactive oxygen species-modulating agents14
Synthesis and evaluation of lipoic acid – donepezil hybrids for Alzheimer’s disease using a straightforward strategy14
Synthesis and evaluation of potent novel inhibitors of human sulfide:quinone oxidoreductase14
Editorial Board14
Improving reactivity of naphthalimide-based GST probe by imparting TPP cation: Development and application for live cell imaging14
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 dipeptide14
Synthesis and evaluation of 3-hydroxyquinolin-2(1H)-one derivatives as inhibitors of tyrosinase14
Synthesis and pharmacological characterization of multiply substituted 2H-chromene derivatives as P2Y6 receptor antagonists14
A photoactivatable self-localizing ligand with improved photosensitivity for chemo-optogenetic control of protein localization in living cells14
Synthesis of dolutegravir derivatives modified by 1,2,3-triazole structure and their anti-inflammatory activity in LPS-induced BV2 cells14
Design and synthesis of a series of OFF-ON near infrared fluorescent probes for nucleic acid in aqueous solution14
Editorial Board13
Graphical Abstract Continued13
Design, synthesis and biological evaluation of cajanonic acid A analogues as potent PPAR γ antagonists13
Reinvestigation of clopidogrel bioactivation unveils new cytochrome P450-catalyzed thioester cleavage mechanism13
Graphical Abstract Contents Continued13
Discovery of novel N-(1-benzyl-1H-imidazol-2-yl)amide derivatives as melanocortin 1 receptor agonists13
Synthesis and biological evaluation of substituted amide derivatives of C4-ageratochromene dimer analog13
Discovery of triazenyl triazoles as Nav1.1 channel blockers for treatment of epilepsy13
6-Aryl-quinazolines as novel GABAB receptor positive allosteric modulators13
Editorial Board13
Graphical abstract TOC13
Structure–activity relationship of 2-aminodibenzothiophene pharmacophore and the discovery of aminobenzothiophenes as potent inhibitors of Mycobacterium smegmatis13
Graphical abstract TOC13
Editorial Board13
Contents continued12
Structure-activity relationship of dual inhibitors containing maleimide and imidazole motifs against glutaminyl cyclase and glycogen synthase kinase-3β12
Design, synthesis, and biological evaluation of polyphenol derivatives as DYRK1A inhibitors. The discovery of a potentially promising treatment for Multiple Sclerosis12
Antibacterial activity of β-sitosterol isolated from the leaves of Odontonema strictum (Acanthaceae)12
Phenyl urea based adjuvants for β-lactam antibiotics against methicillin resistant Staphylococcus aureus12
Neratinib derivative 7A induces apoptosis in colon cancer cells via the p53 pathway12
Discovery of dronedarone and its analogues as NLRP3 inflammasome inhibitors with potent anti-inflammation activity12
A unified “top-down” approach for the synthesis of diverse lead-like molecular scaffolds12
A dual aurora and lim kinase inhibitor reduces glioblastoma proliferation and invasion12
Structure-activity relationship of dibenzylideneacetone analogs against the neglected disease pathogen, Trypanosoma brucei12
Design, synthesis, in silico studies, and antiproliferative evaluations of novel indolin-2-one derivatives containing 3-hydroxy-4-pyridinone fragment12
Graphical abstract TOC12
Enzymatic reconstitution of salicylate formation in promysalin biosynthesis12
Discovery of sinomenine/8-Bis(benzylthio)octanoic acid hybrids as potential anti-leukemia drug candidate via mitochondrial pathway12
Graphical abstract TOC12
Design, synthesis and biological evaluation of novel cationic liposomes loaded with melphalan for the treatment of cancer12
Identification of potent and selective inhibitors of PKR via virtual screening and traditional design12
Contents continued11
Synthesis of mizoribine prodrugs and their in vivo evaluation as immunosuppressive agents11
Contents continued11
Syntheses and antitumor activities of neorautenol and shinpterocarpin analogs11
Direct-to-biology platform: From synthesis to biological evaluation of SHP2 allosteric inhibitors11
Editorial Board11
PSMA-targeted SMART molecules outfitted with SN3811
Synthesis and evaluation of antimycobacterial activity of riboflavin derivatives11
Graphical abstract TOC11
Corrigendum to “Discovery of 4-aminopyrimidine analogs as highly potent dual P70S6K/Akt inhibitors” [Bioorgan. Med. Chem. Lett. 50 (2021) 128352]11
Graphical abstract TOC11
Rationalizing the binding and α subtype selectivity of synthesized imidazodiazepines and benzodiazepines at GABAA receptors by using molecular docking studies11
Methyl N-(tert-butoxycarbonyl)pyridine-2-carbimidothioate: A new reagent for the synthesis of N-phenylpyridinecarboxamidine (“arylimidamide”) DNA-minor groove binders from poorly nucleophilic amines11
Discovery of 3-acyl-2-anilino-1,4-dihydroquinolin-4-one derivatives as potential inhibitors of methicillin-resistant Staphylococcus aureus11
A guanidinium group is an effective mimic of the tertiary carbocation formed by isopentenyl diphosphate isomerase11
Graphical abstract TOC11
Investigation of the site 2 pocket of Grp94 with KUNG65 benzamide derivatives11
Graphical abstract TOC11
SAR towards indoline and 3-azaindoline classes of IDO1 inhibitors11
Potent and selective carbonic anhydrase inhibition activities of pyrazolones bearing benzenesulfonamides11
Graphical abstract TOC11
Development of novel GI-centric prostaglandin E2 receptor type 4 (EP4) agonist prodrugs as treatment for ulcerative colitis and other intestinal inflammatory diseases11
Conversion of oxadiazolo[3,4-b]pyrazines to imidazo[4,5-b]pyrazines via a tandem reduction-cyclization sequence generates new mitochondrial uncouplers10
Highly potent anti-inflammatory, analgesic and antioxidant activities of 3,5-disubstituted tetrahydro-2H-1,3,5-thiadiazine thiones10
Photo-regulated PROTACs: A novel tool for temporal control of targeted protein degradation10
Novel drug discovery approaches for MMP-13 inhibitors in the treatment of osteoarthritis10
Hydrazinecarbonyl-thiazol-2-acetamides with pronounced apoptotic behavior: synthesis, in vitro/in vivo anti-proliferative activity and molecular modeling simulations10
A small-molecule pretargeting approach for PSMA-targeted conjugates10
Design, synthesis and biological evaluation of novel indole-piperazine derivatives as antibacterial agents10
Discovery of BI-9787, a potent zwitterionic ketohexokinase inhibitor with oral bioavailability10
A small molecule binding to TGGAA pentanucleotide repeats that cause spinocerebellar ataxia type 3110
Further structural optimization and SAR study of sungsanpin derivatives as cell-invasion inhibitors10
Permeation behavior of porphyrin derivatives with different functional group positions across cancer cell membranes10
Designing a novel photoinduced electron transfer-based small-molecule fluorescent probe specific for CYP3A isozymes10
Discovery of an ellipticine derivative as TLR3 inhibitor against influenza A virus and SARS-CoV-210
Discovery of a potent orally available pyrazolopyridone derivative as a novel selective bromodomain and extra-terminal domain (BET)-first bromodomain (BD1) inhibitor10
Evaluation of an ester-linked immunosuppressive payload: A case study in understanding the stability and cleavability of ester-containing ADC linkers10
New diarylpentanoids and chalcones as potential antimicrobial adjuvants10
PES derivative PESA is a potent tool to globally profile cellular targets of PES10
Cyano-Hydrol green derivatives: Expanding the 9-cyanopyronin-based resonance Raman vibrational palette10
Harnessing dual-mode RIPK1 ligands for cross-species anti-necroptosis inhibitor compounds10
Design, synthesis, and bioevaluation of SOS1 PROTACs derived from pyrido[2,3-d]pyrimidin-7-one-based SOS1 inhibitor10
Synthesis, in vitro cytotoxicity evaluation and mechanism of 5′ monosubstituted chalcone derivatives as antitumor agents10
Discovery of a proteolysis targeting chimera (PROTAC) as a potent regulator of FOXP310
Zinc-dependent deacetylases (HDACs) as potential targets for treating Alzheimer’s disease10
Synthesis, modeling, and biological evaluation of anti-tubulin indole-substituted furanones10
Synthesis and biological evaluation of biotinylated ZJ-10110
Design, synthesis, and biological evaluation of 2,4-diaminopyrimidine inhibitors of hematopoietic progenitor kinase 110
Iodophenyl-conjugated closo-dodecaborate as a promising small boron molecule that binds to serum albumin and accumulates in tumor10
Synthesis and biological activity of conformationally restricted indole-based inhibitors of neurotropic alphavirus replication: Generation of a three-dimensional pharmacophore10
Discovery of a potent and subtype-selective TYK2 degrader based on an allosteric TYK2 inhibitor10
Retraction notice to “Synthesis and bioevaluation of aryl-guanidino polyamine conjugates targeting the polyamine transporter” [Bioorg. Med. Chem. Lett. 20 (2010) 6421–6425]9
Graphical abstract TOC9
Graphical Abstract Contents Continued9
Multigram-scale total synthesis of (±)-ambreinolide by a diastereoselective polyene cyclization9
Discovery of a DCAF11-dependent cyanoacrylamide-containing covalent degrader of BET-proteins9
Activation of 8–17 DNAzyme with extra functional group at conserved residues is related to catalytic metal ion9
Editorial Board9
Synthesis of drimanyl indole fragments of drimentine alkaloids and their antibacterial activities9
Discovery of aryl aminothiazole γ-secretase modulators with novel effects on amyloid β-peptide production9
Discovery of IDO1 inhibitors containing a decahydroquinoline, decahydro-1,6-naphthyridine, or octahydro-1H-pyrrolo[3,2-c]pyridine scaffold9
Graphical abstract TOC9
Contents continued9
Graphical Abstract TOC9
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
Synthesis of proposed structure of ledebourin A9
Contents continued9
Thiamine analogues featuring amino-oxetanes as potent and selective inhibitors of pyruvate dehydrogenase9
5-Fluoro-2′-deoxyuridine as an efficient 19F NMR reporter for G-quadruplex and i-motif structures9
Diamino variants of piperazine-based tissue transglutaminase inhibitors9
Discovery of acyl ureas as highly selective small molecule CSF1R kinase inhibitors9
Graphical abstract TOC9
Novel imidazo[1,5-a]quinoxaline derivatives: SAR, selectivity and modeling challenges en route to the identification of an α5-GABAA receptor NAM9
Graphical Abstract TOC9
Imidazo[2,1-b]thiazole based indoleamine-2,3-dioxygenase 1 (IDO1) inhibitor: Structure based design, synthesis, bio-evaluation and docking studies9
Synthesis and antitumor activity of a series of novel N-aryl-5-(2,2,2-trifluoroethoxy)-1,5-dihydro-2H-pyrrol-2-ones derivatives9
Synthesis and properties of PNA containing a dicationic nucleobase based on N4-benzoylated cytosine9
Pyrimidine-2,4-dione targets STAT3 signaling pathway to induce cytotoxicity in hepatocellular carcinoma cells9
Design, synthesis and antiproliferative activity of novel 2,4-diamino-5-methyleneaminopyrimidine derivatives as potential anticancer agents9
Synthesis and evaluation of catecholamine derivatives as amyloid-beta aggregation inhibitors9
An ascidian Polycarpa aurata-derived pan-inhibitor against coronaviruses targeting Mpro9
Editorial Board9
Recent developments of benzimidazole based analogs as potential tubulin polymerization inhibitors: A critical review8
Graphical abstract TOC8
Editorial Board8
Graphical abstract TOC8
Identification of (−)-Epigallocateshin gallate derivatives promoting innate immune activation via 2′,3′-cyclic GMP-AMP-stimulator of interferon genes pathway8
Discovery of cinnoline derivatives as potent PI3K inhibitors with antiproliferative activity8
Inhibition of glutathione S-transferases by photoactive calix[4]arene α-ketophosphonic acids8
Design, synthesis and antitumor activity of novel 4-oxobutanamide derivatives8
Editorial Board8
4-Oxooctahydroquinoline-1(2H)-carboxamides as hepatitis B virus (HBV) capsid core protein assembly modulators8
Graphical abstract TOC8
Design of cyclic peptides as novel inhibitors of ICOS/ICOSL interaction8
Inhibitors for metallo-β-lactamases from the B1 and B3 subgroups provide an avenue to combat a major mechanism of antibiotic resistance8
Synthesis and preliminary immunologic properties of di-/trisaccharide-conjugates related to Bacillus anthracis8
The lipidation and glycosylation enabling bioactivity enhancement and structural change of antibacterial peptide G38
Design, synthesis and biological evaluation of sulfonylurea derivatives as NLRP3 inflammasome inhibitors8
Graphical Abstract Contents Continued8
Novel detection method for gallic acid: A water soluble boronic acid-based fluorescent sensor with double recognition sites8
Expanded library of novel 2,3-pyrrolidinedione analogues exhibit anti-biofilm activity8
Strategic structure–activity relationship study on a follistatin-derived myostatin inhibitory peptide8
The structural modification and biological evaluation of tetrahydrothienopyridine derivatives as selective BChE inhibitors8
l-Hypaphorine and d-hypaphorine: Specific antiacetylcholinesterase activity in rat brain tissue8
Development of chromone-thiazolidine-2,4-dione Knoevenagel conjugates as apoptosis inducing agents8
Graphical abstract TOC8
SAR study of niclosamide derivatives for neuroprotective function in SH-SY5Y neuroblastoma8
Editorial Board8
Estimation of the lipophilicity of purine-2,6-dione-based TRPA1 antagonists and PDE4/7 inhibitors with analgesic activity8
Sensitive and reliable gastric ulcer related MicroRNA detection by bridge catalytic hairpin assembly (bCHA) mediated primer exchange reaction8
Design, synthesis and evaluation of the Brigatinib analogues as potent inhibitors against tertiary EGFR mutants (EGFRdel19/T790M/C797S and EGFRL858R/T790M/C797S)8
Retraction notice to “Corrigendum to “Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities” [Bioorg. Med. Chem. Lett. 228
Thermal treatment affects aptamers’ structural profiles8
The association between oxidized low-density lipoprotein and cancer: An emerging targeted therapeutic approach?8
Synthesis and biological evaluation of novel 18F-labeled 2,4-diaminopyrimidine derivatives for detection of ghrelin receptor in the brain8
Discovery of the potent covalent inhibitor with an acrylate warhead for SARS-CoV-2 3CL protease8
Exploration of inhibitors of the bacterial LexA repressor-protease8
Aiming to improve binding of porphyrin diphenyl guanidinium conjugates to guanine-quadruplexes: When size matters8
Design, synthesis, and biological evaluation of novel HDAC inhibitors with a 3-(benzazol-2-yl)quinoxaline framework8
Editorial Board8
Synthesis, antiproliferative activity, and biological profiling of C-19 trityl and silyl ether andrographolide analogs in colon cancer and breast cancer cells8
Editorial Board8
Identification of Plasmodium falciparum falcilysin inhibitors by a virtual screen8
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