Bioorganic & Medicinal Chemistry

Article	Citations
Editorial Board	93
Discovery of novel indazole derivatives as SOS1 agonists that activate KRAS signaling	91
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A gemcitabine-based conjugate with enhanced antitumor efficacy by suppressing HIF-1α expression under hypoxia	73
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LC-MS/MS analysis of elastin crosslinker desmosines and microscopic evaluation in clinical samples of patients with hypertrophy of ligamentum flavum	56
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Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists	44
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Editorial Board	38
Which boronic acids are used most frequently for synthesis of bioactive molecules?	34
Targeting osteoarthritis-associated galectins and an induced effector class by a ditopic bifunctional reagent: Impact of its glycan part on binding measured in the tissue context	33
Aromatic oligoesters as novel helix mimetic scaffolds	33
There’s more to enzyme antagonism than inhibition	33
Contents continued	33
Editorial Board	32
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Synthesis and biological evaluation of 3-styrylchromone derivatives as selective monoamine oxidase B inhibitors	30
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Design, synthesis and validation of a new Crimped Head-Piece for DNA-Encoded libraries generation	30

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Design, synthesis and evaluate of indazolylaminoquinazoline derivatives as potent Tropomyosin receptor kinase (TRK) inhibitors	29
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Design and synthesis of a DNA-encoded combinatorial library of bicyclic peptoids	28
Synthesis of PF-6870961, a major hydroxy metabolite of the novel ghrelin receptor inverse agonist PF-5190457	28
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Novel ferrocenylbisphosphonate hybrid compounds: Synthesis, characterization and potent activity against cancer cell lines	27
In vitro, ex vivo and in vivo short-term screening of DHEA nitrate derivatives activity over Trypanosoma cruzi Ninoa and TH strains from Oaxaca State, México	27
Scope of on-DNA nucleophilic aromatic substitution on weakly-activated heterocyclic substrates for the synthesis of DNA-encoded libraries	26
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Design and synthesis of boron-containing ALK inhibitor with favorable in vivo efficacy	25
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Design, synthesis and biological evaluation studies of novel anti-fibrosis agents bearing sulfoxide moiety	23
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Early potential evaluation of lead compounds from a DNA-encoded library by the determination of their thermodynamics through a chromatographic method based on immobilized β2-adrenoceptor	22
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Synthesis and antiviral activity of formycin derivatives with anti-influenza virus activity	22
Discovery of potent dual ligands for dopamine D4 and σ1 receptors	21
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Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor	21
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Polyguluronate simulations shed light onto the therapeutic action of OligoG CF-5/20	20
Development of delivery carriers for plasmid DNA by conjugation of a helical template to oligoarginine	20
Editorial Board	20
Graphical abstract TOC	20
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Aspirin-based PROTACs as COX-2 degraders for anti-inflammation	19
Synthesis and biological evaluation of lappaconitine analogues as potential anti-neuroinflammatory agents by side chain modification and scaffold hopping strategy	19
Proteolysis targeting chimera of BI-2536 induces potent dual degradation of PLK1 and BET proteins	19
Design, synthesis, and biological evaluation of novel azaspirooxindolinone derivatives as potent inhibitors of ITK and BTK-dependent cancers	19
Graphical Abstract Contents Continued	19
De novo discovery of cyclic peptide inhibitors of IL-11 signaling	19
Fine-tuning probes for fluorescence polarization binding assays of bivalent ligands against polo-like kinase 1 using full-length protein	19

Identification and optimization of a small molecule inhibitor of the ovarian tumor protease of the Crimean-Congo hemorrhagic fever virus	19
Editorial Board	19
Janus dendritic ionizable lipids with fine designed headgroup and tails to improve mRNA delivery efficiency	19
Fatty acid conjugated BimBH3 analogues with d‑amino acid substitution as PTPN1 inhibitors with enhanced activity, biostability and orally available potency for the treatment of diabetes	19
Targeting glioma with heteroaromatic alkaloids: A review of potential therapeutics	18
Design and synthesis of proteolysis-targeting chimeras (PROTACs) as degraders of glutathione peroxidase 4	18
SAR study of N′-(Salicylidene)heteroarenecarbohydrazides as promising antifungal agents	18
10-Alkoxy-anthracenyl-isoxazole analogs have sub-micromolar activity against a Glioblastoma multiforme cell line	18
Anti-HBV activity of (R)-gentiandiol, a metabolite of Swertiamarin, in transgenic mice: Insights from non-targeted serum metabolomics	18
Synthesis and structural optimization of oncolytic peptide LTX-315	18
Discovery of a new class of valosine containing protein (VCP/P97) inhibitors for the treatment of colorectal cancer	18
Structure-activity relationship studies on divalent naphthalene diimide G quadruplex ligands with anticancer and antiparasitic activity	17
H2S-releasing oridonin derivatives with improved antitumor activity by inhibiting the PI3K/AKT pathway	17
Synthesis of α-fluorocinnamate derivatives as novel cathepsin S inhibitors with in vitro antiproliferative activity against pancreatic cancer cells	17
Editorial Board	17
Unraveling the mechanism of alkaloids from Sophora alopecuroides Linn combined with immune checkpoint blockade in the treatment of non-small cell lung cancer based on systems pharmacology	16
Design, synthesis and biological evaluation of colchicine glycoconjugates as tubulin polymerization inhibitors	16
Discovery of novel pyrimidine molecules containing boronic acid as VCP/p97 Inhibitors	16
Discovery of a novel photoswitchable PI3K inhibitor toward optically-controlled anticancer activity	16
Graphical abstract TOC	16
Targeting m6A binding protein YTHDFs for cancer therapy	16
Ionization and lipophilicity in nonpolar media mimicking the cell membrane interior	16
Bioisoteres for carboxylic acids: From ionized isosteres to novel unionized replacements	16
Editorial Board	16
Multi-target potential of newly designed tacrine-derived cholinesterase inhibitors: Synthesis, computational and pharmacological study	16
Skin- and airway-deliverable TRPA1 inhibitor	15
Efficient synthesis of indole-chalcones based glycohybrids and their anticancer activity	15
Diterpenoids from the whole plants of Croton yunnanensis and their bioactivities	15
Design, synthesis and biological evaluation of novel 9-N-substituted-13-alkylberberine derivatives from Chinese medicine as anti-hepatocellular carcinoma agents	15
Exploring novel A2AAR antagonists: Design, synthesis, and evaluation of 2,6,9-trisubstituted purine derivatives as promising antifibrotic agents	15
Design, synthesis, and molecular simulation studies of N-phenyltetrahydroquinazolinones as protoporphyrinogen IX oxidase inhibitors	15
Targeting prolidase. A survey of the literature data to depict a structure-activity relationship frame and to address future studies for drug development	15
SAR evolution towards potent C-terminal carboxamide peptide inhibitors of Zika virus NS2B-NS3 protease	15
Oropouche virus – The “Newest” invisible public enemy?	15
Discovery of cyanoguanidine derivatives as biased μ-opioid receptor agonists	15
How kelch domain-containing protein 3 distinguishes between the C-end degron of herpesviral protein UL49.5 and its mutants – Insights from molecular dynamics	15
Indolylarylsulfones bearing phenylboronic acid and phenylboronate ester functionalities as potent HIV‑1 non-nucleoside reverse transcriptase inhibitors	14
Synthesis of lathyrane diterpenoid nitrogen-containing heterocyclic derivatives and evaluation of their anti-inflammatory activities	14
Current Japanese pharmaceutical chemistry	14
Design and synthesis of efficient fluororethylene-peptidomimetic inhibitors of dipeptidyl peptidase III (DPP3)	14
Photocaging of N-pyridinyl amide scaffold-based PIM inhibitors for spatiotemporal controlled anticancer bioactivity	14
Current and emerging therapies for Achondroplasia: The dawn of precision medicine	14
Synthesis and evaluation of trypanocidal activity of derivatives of naturally occurring 2,5-diphenyloxazoles	14
Editorial Board	14
Discovery of 3-hydroxymethyl-azetidine derivatives as potent polymerase theta inhibitors	14
Discovery of benzimidazole derivatives as potent and selective aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors with glucose consumption improving activity	14
Synthesis, bioevaluation and docking studies of new imidamide derivatives as nitric oxide synthase inhibitors	14
Discovery of novel macrocyclic derivatives as potent and selective cyclin-dependent kinase 2 inhibitors	14
Multiple approaches to repurposing drugs for neuroblastoma	14
Editorial Board	14
Research progress of multi-target HDAC inhibitors blocking the BRD4-LIFR-JAK1-STAT3 signaling pathway in the treatment of cancer	14
Discovery of fluorinated 2‑Styryl 4(3H)-quinazolinone as potential therapeutic hit for oral cancer	14
DeepAS – Chemical language model for the extension of active analogue series	14
Structure-activity relationship and mechanistic study on guggulsterone derivatives; Discovery of new anti-pancreatic cancer candidate	13
Development of QTMP: A promising anticancer agent through NP-Privileged Motif-Driven structural modulation	13
Integrated lipidomics and network pharmacology analysis of the protective effects and mechanism of Yuanzhi San on rats with cognitive impairment	13
Site-specific construction of triptolide-based antibody-drug conjugates	13
A review of MMP-2 structures and binding mode analysis of its inhibitors to strategize structure-based drug design	13
Facile incorporation of non-canonical heme ligands in myoglobin through chemical protein synthesis	13
Synthesis and evaluation of curcumin-based near-infrared fluorescent probes for detection of amyloid β peptide in Alzheimer mouse models	13
Editorial Board	13
Development of flavonoid probes and the binding mode of the target protein and quercetin derivatives	13
Discovery of selective platelet-derived growth factor receptor-beta (PDGFR-β) bifunctional small-molecule degraders	13
Synthetic approaches to FDA approved drugs for asthma and COPD from 1969 to 2020	13
Triple branched RGD modification on liposomes: A prospective strategy to enhance the glioma targeting efficiency	13
Design, synthesis and biological evaluation of the tumor hypoxia-activated PROTACs bearing caged CRBN E3 ligase ligands	13
Design, synthesis, and biological evaluation of a novel series of 1,2,4-oxadiazole inhibitors of SLACK potassium channels: Identification of in vitro tool VU0935685	13
Probing for optimal photoaffinity linkers of benzophenone-based photoaffinity probes for adenylating enzymes	13
Discovery of ASP5878: Synthesis and structure–activity relationships of pyrimidine derivatives as pan-FGFRs inhibitors with improved metabolic stability and suppressed hERG channel inhibitory activity	13
Substituents of life: The most common substituent patterns present in natural products	13
Design, synthesis and biological evaluation of salicylanilides as novel allosteric inhibitors of human pancreatic lipase	13
Modulation of proteasome subunit selectivity of syringolins	12
Antimycobacterial and anti-inflammatory activities of thiourea derivatives focusing on treatment approaches for severe pulmonary tuberculosis	12
Amine-bearing hydrocarbon cross-links: Tailoring helix stability, hydrophilicity, and synthetic adaptability in peptides	12
Structure activity relationship of pyrazinoic acid analogs as potential antimycobacterial agents	12
Withaferin A, a polyfunctional pharmacophore that includes covalent engagement of IPO5, is an inhibitor of influenza A replication	12
Medicinal chemistry perspectives on the development of piperazine-containing HIV-1 inhibitors	12
Identification of benzamides derivatives of norfloxacin as promising microRNA-21 inhibitors via repressing its transcription	12
Design, synthesis and anticancer activity evaluation of 4-(3-1H-indazolyl)amino quinazoline derivatives as PAK4 inhibitors	12
DNA-encoded C H functionality via photoredox-mediated hydrogen atom transformation catalysis	12

Silybins are stereospecific regulators of the 20S proteasome	12
Design, synthesis and biological evaluation of imidazopyridazine derivatives containing isoquinoline group as potent MNK1/2 inhibitors	12
A new small molecule DoNA binding to CAG repeat RNA	12
Production and synthesis of a novel 191Pt-labeled platinum complex and evaluation of its biodistribution in healthy mice	12
A computer-aided drug design approach to discover tumour suppressor p53 protein activators for colorectal cancer therapy	12
Cathepsin D inhibitors based on tasiamide B derivatives with cell membrane permeability	12
Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis	12
Synthesis and physical and biological properties of 1,3-diaza-2-oxophenoxazine-conjugated oligonucleotides	12
Design and synthesis of a fluorescent probe to develop a fluorescence polarization assay for the E3 ligase FEM1C	12
Short peptide pharmacophores developed from protein phosphatase-1 disrupting peptides (PDPs)	12
Synthesis of alpha-Gal C-disaccharides	12
Iodoetherification as a strategy towards sp3-rich scaffolds for drug discovery	12
Structural optimization of a lysine demethylase 5 inhibitor for improvement of its cellular activity	12
Synthesis and medicinal chemistry of tetronamides: Promising agrochemicals and antitumoral compounds	12
Synthesis and evaluation of dual fatty acid amide hydrolase-monoacylglycerol lipase inhibition and antinociceptive activities of 4-methylsulfonylaniline-derived semicarbazones	12
Novel hybrid conjugates with dual estrogen receptor α degradation and histone deacetylase inhibitory activities for breast cancer therapy	12
Junctions in DNA: underexplored targets for therapeutic intervention	12
Endothelial cell spreading on lipid bilayers with combined integrin and cadherin binding ligands	12
A bleomycin-mimicking manganese-porphyrin-conjugated mitochondria-targeting peptoid for cancer therapy	11
Improving the solubility of anti-proliferative thieno[2,3-b]quinoline-2-carboxamides	11
Systematic assessment of structure-promiscuity relationships between different types of kinase inhibitors	11
Pentafluorosulfanyl-substituted biaryl derivatives as MATE-type transporter inhibitors targeting drug-resistant bacteria	11
Crescent-shaped meta-substituted benzene derivatives as a new class of non-nucleoside ribonuclease A inhibitors	11
Novel methyllycaconitine analogues selective for the α4β2 over α7 nicotinic acetylcholine receptors	11
Iodinated 1,2-diacylhydrazines, benzohydrazide-hydrazones and their analogues as dual antimicrobial and cytotoxic agents	11
Discovery of chiral 1,4-diarylazetidin-2-one-based hydroxamic acid derivatives as novel tubulin polymerization inhibitors with histone deacetylase inhibitory activity	11
Detection of N,N-diacetyllactosamine (LacdiNAc) containing free prostate-specific antigen for early stage prostate cancer diagnostics and for identification of castration-resistant prostate cancer pat	11
Repurposing primaquine as a polyamine conjugate to become an antibiotic adjuvant	11
Dipyridyl-substituted thiosemicarbazone as a potent broad-spectrum inhibitor of metallo-β-lactamases	11
Design, synthesis, kinetic, molecular dynamics, and hypoglycemic effect characterization of new and potential selective benzimidazole derivatives as Protein Tyrosine Phosphatase 1B inhibitors	11
Synthesis and biological evaluation of novel 1,4-benzodiazepin-3-one derivatives as potential antitumor agents against prostate cancer	11
Synthesis and antiproliferative activity of (−)-cleistenolide, (6S)-cleistenolide and 4-substituted cleistenolide analogues	11
Sulfonamide-derivatized galactosides selectively target an unexplored binding site in the galectin-9N-terminal domain	11
Fused chromeno and quinolino[1,8]naphthyridines: Synthesis and biological evaluation as topoisomerase I inhibitors and antiproliferative agents	11
Rational design of cannabinoid type-1 receptor allosteric modulators: Org27569 and PSNCBAM-1 hybrids	11
Design, synthesis and evaluation of novel prostate-specific membrane antigen-targeted aryl [18F]fluorosulfate PET tracers	11
Synthesis and biological evaluation of orally active anti-Trypanosoma agents	11
Effects of β-lapachone and β-nor-lapachone on multidrug efflux transporters and biofilms of Candida glabrata	11
A DNA-encoded library special issue	11
The application of PROTACs in immune-inflammation diseases	11
Discovery of novel tripeptide propylene oxide proteasome inhibitors for the treatment of multiple myeloma	10
N3-Methyluridine and 2′-O-Alkyl/2′-Fluoro-N3-methyluridine functionalized nucleic acids improve nuclease resistance while maintaining duplex geometry	10
Discovery and mechanistic study of thiazole-4-acylsulfonamide derivatives as potent and orally active ChemR23 inhibitors with a long-acting effect in cynomolgus monkeys	10
Design, synthesis, and biological evaluation of stapled ascaphin-8 peptides	10
Synthesis and biological evaluation of novel photo-clickable adenosine and cyclic ADP-ribose analogs: 8-N3-2′-O-propargyladenosine and 8-N3-2′-O-propargyl-cADPR	10
Synthesis, microbiological evaluation and structure activity relationship analysis of linezolid analogues with different C5-acylamino substituents	10
Sustainable electrochemical C(sp3) − H oxygenation using water as the oxygen source	10
Design, synthesis and antitumor activity of 2-substituted quinazoline-4-amine derivatives	10
Synthesis and biological evaluation of pyrazole-fused oleanolic acid derivatives as novel inhibitors of inflammatory and osteoclast differentiation	10
Inhibition of amyloid formation of amyloid β (1–42), amylin and insulin by 1,5-diazacyclooctanes, a spermine-acrolein conjugate	10
RNA-templated chemical synthesis of proapoptotic L- and d-peptides	10
Directed evolution of an amine transaminase for the synthesis of an Apremilast intermediate via kinetic resolution	10
Axial chirality and affinity at the GABAA receptor of triazolobenzodiazepines	10
A simplified analog of debromoaplysiatoxin lacking the B-ring of spiroketal moiety retains protein kinase C-binding and antiproliferative activities	10
Design, synthesis and biological evaluation of naphthyl amide derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors	10
New substituted benzoxazine derivatives as potent inducers of membrane permeability and cell death	10
Mechanism-based inhibition of GH127/146 cysteine glycosidases by stereospecifically functionalized l-arabinofuranosides	10
Auranofin inhibits virulence pathways in Pseudomonas aeruginosa	10
Benzobis(imidazole) derivatives as STAT3 signal inhibitors with antitumor activity	10
Discovery of 5-methylpyrimidopyridone analogues as selective antimycobacterial agents	10
Linker optimization and activity validation of a cell surface vimentin targeted homo-dimeric peptoid antagonist for lung cancer stem cells	10
Rational design of prodrug-type apoB-targeted siRNA for nuclease resistance improvement without compromising gene silencing potency	10
Discovery of novel 2,8-diazaspiro[4.5]decan-1-one derivatives as potent RIPK1 kinase inhibitors	10
A kind of HIV-1 protease inhibitors containing phenols with antiviral activity against DRV-resistant variants	10
From triazolophthalazines to triazoloquinazolines: A bioisosterism-guided approach toward the identification of novel PCAF inhibitors with potential anticancer activity	9
Small molecule inhibitor E-64 exhibiting the activity against African swine fever virus pS273R	9
A novel tricyclic β-lactam exhibiting potent antibacterial activities against carbapenem-resistant Enterobacterales: Synthesis and structure-activity-relationships	9
Daphnanes diterpenes from the latex of Hura crepitans L. and their PKCζ-dependent anti-proliferative activity on colorectal cancer cells	9
Non-fused imidazole-biphenyl analogs repress triple-negative breast cancer growth by mainly stabilizing the c-MYC G-quadruplex via a multi-site binding mode	9
An overview of GPX4-targeting TPDs for cancer therapy	9
Discovery of 4-oxo-4,5-dihydropyrazolo[1,5-a]quinoxaline-7-carboxamide derivatives as PI3Kα inhibitors via virtual screening and docking-based structure optimization	9
Novel 3-benzylidene/benzylphthalide Mannich base derivatives as potential multifunctional agents for the treatment of Alzheimer’s disease	9
Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy	9
Structure-based design and optimization of a new class of small molecule inhibitors targeting the P-stalk binding pocket of ricin	9
Design, synthesis and biological evaluation of double fatty chain-modified glucagon-like peptide-1 conjugates	9
Expedient discovery for novel antifungal leads: 1,3,4-Oxadiazole derivatives bearing a quinazolin-4(3H)-one fragment	9
Synthesis and evaluation of sulfonamide derivatives targeting EGFR790M/L858R mutations and ALK rearrangement as anticancer agents	9
Fragment-based lead discovery to identify novel inhibitors that target the ATP binding site of pyruvate dehydrogenase kinases	9
Versatile anti-infective properties of pyrido- and dihydropyrido[2,3-d]pyrimidine-based compounds	9
Editorial Board	9
Selective targeting of human TET1 by cyclic peptide inhibitors: Insights from biochemical profiling	9
Structure-based drug design of novel and highly potent pyruvate dehydrogenase kinase inhibitors	9
Revisiting recent unusual drug-DNA complex structures: Implications for cancer and neurological disease diagnostics and therapeutics	9
Design, synthesis, evaluation and optimization of novel azole analogues as potent antifungal agents	9
Impact of α-modifications on the activity of triazole bisphosphonates as geranylgeranyl diphosphate synthase inhibitors	9
A trio of quinoline-isoniazid-phthalimide with promising antiplasmodial potential: Synthesis, in-vitro evaluation and heme-polymerization inhibition studies	9
18F-Labeled o‑aminopyridyl alkynyl radioligands targeting colony-stimulating factor 1 receptor for neuroinflammation imaging	9
Synthesis and biological evaluation of 1H-pyrrolo[3,2–g]isoquinolines	9
Design, Synthesis, and Biological Evaluation of New 1H-Imidazole-2-Carboxylic Acid Derivatives as Metallo-β-Lactamase Inhibitors	9
Homopurine guanine-rich sequences in complex with N-methyl mesoporphyrin IX form parallel G-quadruplex dimers and display a unique symmetry tetrad	9
Discovery of selective covalent cathepsin K inhibitors containing novel 4-cyanopyrimidine warhead based on quantum chemical calculations and binding mode analysis	9
In vivo organic synthesis by metal catalysts	9
Design, synthesis, anti-tumor activity and mechanism of novel PROTACs as degraders of PD-L1 and inhibitors of PD-1/PD-L1 interaction	9
Steroidal alkaloids isolated from Veratrum grandiflorum Loes. as novel Smoothened inhibitors with anti-proliferation effects on DAOY medulloblastoma cells	9
An insight into the medicinal attributes of berberine derivatives: A review	9