Bioorganic & Medicinal Chemistry

Article	Citations
Synthesis and antiproliferative activity of (−)-cleistenolide, (6S)-cleistenolide and 4-substituted cleistenolide analogues	110
Synthesis and biological evaluation of pyrazole-fused oleanolic acid derivatives as novel inhibitors of inflammatory and osteoclast differentiation	94
Production and synthesis of a novel 191Pt-labeled platinum complex and evaluation of its biodistribution in healthy mice	86
A DNA-encoded library special issue	81
Discovery of novel 2,8-diazaspiro[4.5]decan-1-one derivatives as potent RIPK1 kinase inhibitors	67
Discovery of 5-methylpyrimidopyridone analogues as selective antimycobacterial agents	62
Targeting prolidase. A survey of the literature data to depict a structure-activity relationship frame and to address future studies for drug development	47
Current Japanese pharmaceutical chemistry	45
Site-specific construction of triptolide-based antibody-drug conjugates	42
RNA-templated chemical synthesis of proapoptotic L- and d-peptides	39
Janus dendritic ionizable lipids with fine designed headgroup and tails to improve mRNA delivery efficiency	38
Contents continued	37
Graphical abstract TOC	37
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Editorial Board	35
Development of delivery carriers for plasmid DNA by conjugation of a helical template to oligoarginine	35
Diterpenoids from the whole plants of Croton yunnanensis and their bioactivities	35
Synthesis, bioevaluation and docking studies of new imidamide derivatives as nitric oxide synthase inhibitors	33
Exploring novel A2AAR antagonists: Design, synthesis, and evaluation of 2,6,9-trisubstituted purine derivatives as promising antifibrotic agents	33
Selective targeting of human TET1 by cyclic peptide inhibitors: Insights from biochemical profiling	32
Design, synthesis and antibacterial evaluation of oxazolidinone derivatives containing N-methylglycyl or quaternary ammonium salts	32
Crescent-shaped meta-substituted benzene derivatives as a new class of non-nucleoside ribonuclease A inhibitors	31
Targeting m6A binding protein YTHDFs for cancer therapy	30
Design, synthesis and evaluation the bioactivities of novel 1,3-dimethyl-6-amino-1H-indazole derivatives as anticancer agents	30
Research progress of STAT3-based dual inhibitors for cancer therapy	30

Synthesis and medicinal chemistry of tetronamides: Promising agrochemicals and antitumoral compounds	29
Sustainable electrochemical C(sp3) − H oxygenation using water as the oxygen source	29
Design, synthesis and validation of a new Crimped Head-Piece for DNA-Encoded libraries generation	29
Discovery of 3-hydroxymethyl-azetidine derivatives as potent polymerase theta inhibitors	28
Antimycobacterial and anti-inflammatory activities of thiourea derivatives focusing on treatment approaches for severe pulmonary tuberculosis	28
Graphical abstract TOC	27
Multiple approaches to repurposing drugs for neuroblastoma	27
More than forty years of nucleic acid structural science	27
Contents continued	27
Development of novel quinoline-NO donor hybrids inducing human breast cancer cells apoptosis via inhibition of topoisomerase I	27
Editorial Board	26
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Graphical Abstract Contents Continued	26
Design, synthesis, and antiviral activity of 1-aryl-4-arylmethylpiperazine derivatives as Zika virus inhibitors with broad antiviral spectrum	26
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Editorial Board	25
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Graphical Abstract Contents Continued	24
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A pharmacophore-based approach to demonstrating the scope of alcohol dehydrogenases	24
Discovery of tetracyclic 1,2,4-triazoline-fused dibenzo[b,f][1,4]oxazepine as a potent anti-colorectal cancer agent with good efficacy and low toxicity	24
Pentacyclic triterpene-amino acid derivatives induced apoptosis and autophagy in tumor cells, affected the JNK and PI3K/AKT/mTOR pathway	23
Design and evaluation of novel analogs of 2-amino-4-boronobutanoic acid (ABBA) as inhibitors of human gamma-glutamyl transpeptidase	23
Combining CuAAC reaction enables sialylated Bi- and triantennary pseudo mannose N-glycans for investigating Siglec-7 interactions	23
Corrigendum to “Discovery of 1,3,4-oxadiazole derivatives as potential antitumor agents inhibiting the programmed cell death-1/programmed cell death-ligand 1 interaction” [Bioorg. Med. Chem. 46 (2021)	22
CRBN ligand expansion for hematopoietic prostaglandin D2 synthase (H-PGDS) targeting PROTAC design and their in vitro ADME profiles	22
Design, synthesis, and analgesia evaluation of novel Transient Receptor Potential Vanilloid 1 (TRPV1) agonists modified from Cannabidiol (CBD)	22
Oligonucleotides containing 2′-O-methyl-5-(1-phenyl-1,2,3-triazol-4-yl)uridines demonstrate increased affinity for RNA and induce exon-skipping in vitro	22
Novel drug-like fluorenyl derivatives as selective butyrylcholinesterase and β-amyloid inhibitors for the treatment of Alzheimer’s disease	22
Graphical abstract TOC	21
1,3-Disubstituted-1,2,4-triazin-6-ones with potent activity against androgen receptor-dependent prostate cancer cells	21
Design, synthesis, and biological evaluation of novel Bcr-AblT315I inhibitors incorporating amino acids as flexible linker	21
Investigation on the solid-phase synthesis of silybin prodrugs and their timed-release	21
Concise synthesis of piperarborenine B	21
Chemical similarities and differences among inhibitors of nitric oxide synthase, arginase and dimethylarginine dimethylaminohydrolase-1: Implications for the design of novel enzyme inhibitors modulati	21
Harmine-inspired design and synthesis of benzo[d]imidazo[2,1-b]thiazole derivatives bearing 1,3,4-oxadiazole moiety as potential tumor suppressors	20
Design, synthesis and biological evaluation of novel indole derivatives as gut-selective NaPi2b inhibitors	20
Design and evaluation of achiral, non-atropisomeric 4-(aminomethyl)phthalazin-1(2H)-one derivatives as novel PRMT5/MTA inhibitors	20
Structure activity relationship and target prediction for ABX464 analogues in Caenorhabditis elegans	20
Synthesis, evaluation of anti-breast cancer activity in vitro of ICS II derivatives and summary of the structure-activity relationship	20
Peptide-based CE-SELEX enables convenient isolation of aptamers specifically recognizing CD20-expressing cells	20
Design, Synthesis, and biological evaluation of 7H-Pyrrolo[2,3-d]pyrimidines as potent HPK1 kinase inhibitors	19
In vivo imaging of fluorescent albumin modified with pyruvylated-human-type complex oligosaccharide reveals sialylation-like biodistribution and kinetics	19
Introduction of a carboxylic acid group into pyrazolylpyridine derivatives increased selectivity for inhibition of the 20-HETE synthase CYP4A11/4F2	19
Current development and structure–activity relationship study of berberine derivatives	19
Assessing the rigidity of cubanes and bicyclo(1.1.1)pentanes as benzene bioisosteres	19
Optimization of 1,4-bis(arylsulfonamido)naphthalene-N,N'-diacetic acids as inhibitors of Keap1-Nrf2 protein-protein interaction to suppress neuroinflammation	19
Synthesis and biological evaluation of O4′-benzyl-hispidol derivatives and analogs as dual monoamine oxidase-B inhibitors and anti-neuroinflammatory agents	19
Bioorthogonal strategies for the in vivo synthesis or release of drugs	19
Quinazoline-based hydroxamic acid derivatives as dual histone methylation and deacetylation inhibitors for potential anticancer agents	19

Discovery of SYD5115, a novel orally active small molecule TSH-R antagonist	19
Fatty acid binding protein 5 inhibitors as novel anticancer agents against metastatic castration-resistant prostate cancer	19
Ligand- and structure-based identification of novel CDK9 inhibitors for the potential treatment of leukemia	18
Structure-activity relationships of middle-size cyclic peptides, KRAS inhibitors derived from an mRNA display	18
A turn for the worse: Aβ β-hairpins in Alzheimer’s disease	18
A TNF-α blocking peptide that reduces NF-κB and MAPK activity for attenuating inflammation	18
Cytotoxicity of cinchona alkaloid organocatalysts against MES-SA and MES-SA/Dx5 multidrug-resistant uterine sarcoma cell lines	18
Di-indenopyridines as topoisomerase II-selective anticancer agents: Design, synthesis, and structure–activity relationships	17
Graphical abstract TOC	17
Two distinct rotations of bithiazole DNA intercalation revealed by direct comparison of crystal structures of Co(III)•bleomycin A2 and B2 bound to duplex 5′-TAGTT sites	17
Identification of benzothiazole derived monosaccharides as potent, selective, and orally bioavailable inhibitors of human and mouse galectin-3; a rare example of using a S···O binding interaction for	17
In Vivo Imaging of Tumor Hypoxia by Maintaining Green Fluorescence of 9-Aminoanthracene Under Hypoxic Conditions	17
High allele discrimination in the typing of single nucleotide polymorphisms of miRNA	17
4-Arylidene curcumin derivatives in vitro inhibit α-Synuclein aggregation and disaggregate the preformed fibril	17
Discovery of pyrazolo[3,4-d]pyrimidines as novel mitogen-activated protein kinase kinase 3 (MKK3) inhibitors	17
Synthesis and mammalian cell compatibility of light-released glycan precursors for controlled metabolic engineering	17
Editorial Board	16
Editorial Board	16
Hetero-aryl bromide precursor fluorine-18 radiosynthesis and preclinical evaluation of a novel positron emission tomography (PET) tracer [18F]GSK1482160	16
Design and identification of brain-penetrant, potent, and selective 1,3-oxazole-based cholesterol 24-hydroxylase (CH24H) inhibitors	16
The design of protozoan phosphoribosyltransferase inhibitors containing non-charged phosphate mimic residues	16
Structural optimization of naturally derived Ar-turmerone, as novel neuroinflammation suppressors effective in an Alzheimer mouse model	16
Design, synthesis and biological evaluation of arylpropylamine derivatives as potential multi-target antidepressants	16
Biphenyl-based small molecule inhibitors: Novel cancer immunotherapeutic agents targeting PD-1/PD-L1 interaction	16
Neopetrosidines A–D, pyridine alkaloids isolated from the marine sponge Neopetrosia chaliniformis and their cell cycle elongation activity	16
Graphical abstract TOC	16
3-Amino-5,6,7,8-tetrahydrothieno[2,3-b]quinoline-2-carbonitrile: A fluorescent molecule that induces differentiation in PC12 cells	16
Design and synthesis 1H-Pyrrolo[2,3-b]pyridine derivatives as FLT3 inhibitors for the treatment of Acute myeloid Leukemia	16
The 2022 Monkeypox outbreak: How the medicinal chemistry could help us?	16
Design, synthesis and biological evaluation of phosphoroxy quinazoline derivatives as potential EGFRT790M/C797S inhibitors	16
Discovery of polymethoxyphenyl-pyridines bearing amino side chains as tubulin colchicine-binding site inhibitors	15
Dihydroartemisinin improves hypercholesterolemia in ovariectomized mice via enhancing vectorial transport of cholesterol and bile acids from blood to bile	15
Design, synthesis and in vitro validation of bivalent binders of SARS-CoV-2 spike protein: Obeticholic, betulinic and glycyrrhetinic acids as building blocks	15
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Directly arylated oligonucleotides as fluorescent molecular rotors for probing DNA single-nucleotide polymorphisms	15
FDA-approved small molecule kinase inhibitors for cancer treatment (2001–2015): Medical indication, structural optimization, and binding mode Part I	15
Synthesis and antibacterial properties under blue LED light of conjugates between the siderophore desferrioxamine B (DFOB) and an Iridium(III) complex	15
Contents continued	15
Structure-activity relationships of 2-pyrimidinecarbohydrazides as utrophin modulators for the potential treatment of Duchenne muscular dystrophy	15
Design, synthesis and biological evaluation of EGFR kinase inhibitors that spans the orthosteric and allosteric sites	15
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Influence of N-arylsulfonamido d-valine N-substituents on the selectivity and potency of matrix metalloproteinase inhibitors	14
Fluorescent probes and degraders of the sterol transport protein Aster-A	14
Modulation of aryl hydrocarbon receptor activity by halogenated indoles	14
Discovery and structure-activity relationship of Morita-Baylis-Hillman adducts as larvicides against dengue mosquito vector, Aedes aegypti (Diptera: Culicidae)	14
Synthesis and biological evaluation of novel isobenzofuran-1(3H)-one derivatives as antidepressant agents	14
Design, synthesis, docking, and biochemical characterization of non-nucleoside SARS-CoV-2 RdRp inhibitors	14
Growth factors and their peptide mimetics for treatment of traumatic brain injury	14
Discovery of structurally diverse diazatricyclododecenes as lysosomotropic autophagy inhibitors	14
Discovery and optimization of orally bioavailable and potent plasma Kallikrein inhibitors bearing a quaternary carbon	14
Structure-Activity relationship of 1-(Furan-2ylmethyl)Pyrrolidine-Based Stimulation-2 (ST2) inhibitors for treating graft versus host disease	14
Editorial Board	14
An insight into the mechanistic role of (-)-Ampelopsin F from Vatica chinensis L. in inducing insulin secretion in pancreatic beta cells	14
Design, synthesis, and target identification of new hypoxia-inducible factor 1 (HIF-1) inhibitors containing 1-alkyl-1H-pyrazole-3-carboxamide moiety	14
Exploring novel pyrazole-nitroimidazole hybrids: Synthesis and antiprotozoal activity against the human pathogen trichomonas vaginalis	14
Recent advances on synthesis and biological activities of C-17 aza-heterocycle derived steroids	14
Design and synthesis of phenanthridinone and phenanthridine derivatives and their radiosensitizing activity	14
Exploring the interaction of N-(benzothiazol-2-yl)pyrrolamide DNA gyrase inhibitors with the GyrB ATP-binding site lipophilic floor: A medicinal chemistry and QTAIM study	14
Editorial Board	14
Graphical abstract TOC	14
C-terminal modified Enkephalin-like tetrapeptides with enhanced affinities at the kappa opioid receptor and monoamine transporters	14
Synthetic studies on the extracellular domain of the T cell immunoreceptor with immunoglobulin and immunoreceptor tyrosine-based inhibitory motif domain (TIGIT) using Trt-K10 solubilizing tags	14
PET imaging of VEGFR and integrins in glioma tumor xenografts using 89Zr labelled heterodimeric peptide	14
Discovery of novel hypoxia-activated, nitroimidazole constructed multi-target kinase inhibitors on the basis of AZD9291 for the treatment of human lung cancer	14
In vitro activity of N-phenyl-1,10-phenanthroline-2-amines against tachyzoites and bradyzoites of Toxoplasma gondii	13
Generation of an RNA aptamer against LipL32 of Leptospira isolated by Tripartite-hybrid SELEX coupled with in-house Python-aided unbiased data sorting	13
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From natural products to HDAC inhibitors: An overview of drug discovery and design strategy	13
Synthesis, biological activity and mechanism of action of novel allosecurinine derivatives as potential antitumor agents	13
Stereoisomers of cannabidiols and their pharmacological activities – A potentially novel direction for cannabinoids	13
Discovery of dual-targeted molecules based on Olaparib and Rigosertib for triple-negative breast cancer with wild-type BRCA	13
Design, synthesis and anti-tumor efficacy of novel phenyl thiazole/triazole derivatives as selective TrkA inhibitors	13
Graphical abstract TOC	13
Progress in the development of small molecular inhibitors of the Bruton’s tyrosine kinase (BTK) as a promising cancer therapy	13
Truxillic acid monoamides as fatty acid binding protein 5 inhibitors	13

Berberine improves liver injury induced glucose and lipid metabolic disorders via alleviating ER stress of hepatocytes and modulating gut microbiota in mice	13
Phenotypic screen identifies FOXO inhibitor to counteract maturation and promote expansion of human iPS cell-derived cardiomyocytes	13
Synthesis and biophysical properties of tetravalent PEG-conjugated antisense oligonucleotide	13
Identification of novel influenza polymerase PB2 inhibitors using virtual screening approach and molecular dynamics simulation analysis of active compounds	13
Chemical design of radioiodinated probes with a metabolizable linkage for target-selective imaging of systemic amyloidosis	13
Drug discovery targeting nicotinamide phosphoribosyltransferase (NAMPT): Updated progress and perspectives	13
Graphical abstract TOC	12
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Synthesis and biological evaluation of 4H-benzo[e][1,3]oxazin-4-ones analogues of TGX-221 as inhibitors of PI3Kβ	12
Discovery and optimization of anthraquinone derivatives containing substituted bisbenzyloxy groups as a novel scaffold damaged endoplasmic reticulum and against hepatocellular carcinoma cells	12
Editorial Board	12
Erratum to “De novo design with deep generative models based on 3D similarity scoring” [Bioorg. Med. Chem. 44 (2021) 116308]	12
Editorial Board	12
Design, synthesis, and biological evaluation of 2-arylamino-4-(piperidin-4-yloxy)pyrimidines as potent EGFRT790M/L858R inhibitors to treat non-small cell lung cancer	12
Synthesis and characterization of new acid-functionalized porphyrins displaying antimicrobial activity against gram positive bacteria, yeasts and filamentous fungi with or without ultra-high irradianc	12
Design of a potent and selective dual JAK1/TYK2 inhibitor	12
Corrigendum to “Discovery of novel Quinazoline-based KRAS G12C inhibitors as potential anticancer agents” [Bioorg. Med. Chem. 71 (2022) 116962]	12
Editorial Board	12
Editorial Board	12
Editorial Board	12
Biocompatible conjugated polymer nanoparticles labeled with 225Ac for tumor endoradiotherapy	12
Dual-responsive drug release and fluorescence imaging based on disulfide-pillar[4]arene aggregate in cancer cells	12
Discovery of evodiamine derivatives as potent insecticide candidates	12
Next generation Glucose-1-phosphate thymidylyltransferase (RmlA) inhibitors: An extended SAR study to direct future design	11
Structure-based lead optimization to improve potency and selectivity of a novel tetrahydroimidazo[1,2-a]pyridine-5-carboxylic acid series of heparanase-1 inhibitor	11
Selenoneine-inspired selenohydantoins with glutathione peroxidase-like activity	11
Elongation of N6-benzyladenosine scaffold via Pd-catalyzed C–C bond formation leads to derivatives with antiflaviviral activity	11
Rational design of AIEgens through π-bridge engineering for dual-modal photodynamic and photothermal therapy	11
Structure-activity relationship studies and biological properties evaluation of peptidic NRP-1 ligands: Investigation of N-terminal cysteine importance	11
Concise solid-phase synthesis enables derivatisation of YEATS domain cyclopeptide inhibitors for improved cellular uptake	11
Design, synthesis, and pharmacological evaluation of N-(3-carbamoyl-1H-pyrazol-4-yl)-1,3-oxazole-4-carboxamide derivatives as interleukin-1 receptor-associated kinase 4 inhibitors with reduced potenti	11
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A special issue on artificial intelligence for drug discovery	11
Synthesis and antimicrobial studies of cadasides analogues via on-resin esterification	11
Discovery and biological evaluation of novel dual PTP1B and ACP1 inhibitors for the treatment of insulin resistance	11
Discovery and development of small-molecule heparanase inhibitors	11
New phenylpiperazine-thiazolidine-2,4-dione hybrids targeting MAO inhibition: Synthesis, biological evaluation, kinetic study and in silico insights	11
Discovery of 1,8-naphthalidine derivatives as potent anti-hepatic fibrosis agents via repressing PI3K/AKT/Smad and JAK2/STAT3 pathways	11
Target discovery of bioactive natural products with native-compound-coupled CNBr-activated Sepharose 4B beads (NCCB): Applications, mechanisms and outlooks	11
An assessment of the mutational load caused by various reactions used in DNA encoded libraries	11
The most common linkers in bioactive molecules and their bioisosteric replacement network	11
Editorial Board	11
Thiazolidinedione-based structure modification of ergosterol peroxide provides thiazolidinedione-conjugated derivatives as potent agents against breast cancer cells through a PI3K/AKT/mTOR pathway	11
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Discovery of CN0 as a novel proteolysis-targeting chimera (PROTAC) degrader of PARP1 that can activate the cGAS/STING immunity pathway combined with daunorubicin	11
Exploration of 1,2,3-triazole linked benzenesulfonamide derivatives as isoform selective inhibitors of human carbonic anhydrase	11
Lead compound profiling for small molecule inhibitors of the REV1-CT/RIR Translesion synthesis Protein-Protein interaction	11
Potential COX-2 inhibitors modulating NF-κB/MAPK signaling pathways: Design, synthesis and evaluation of anti-inflammatory activity of Pterostilbene-carboxylic acid derivatives with an oxime ether moi	11
Structure-based screening combined with computational and biochemical analyses identified the inhibitor targeting the binding of DNA Ligase 1 to UHRF1	11
Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2	11
Graphical abstract TOC	11
Effect of helicity and hydrophobicity on cell-penetrating ability of arginine-rich peptides	11
Antitumor and toxicity study of mitochondria-targeted triptolide derivatives using triphenylphosphine (TPP+) as a carrier	11
Evaluation of potential anticonvulsant fluorinated N-benzamide enaminones as T-type Ca2+ channel blockers	11
Structure activity relationships leading to the identification of the indirect activator of AMPK, R419	11
Synthesis and biological evaluation of hybrids from optically active ring-opened 3-N-butylphthalide derivatives and 4-fluro-edaravone as potential anti-acute ischemic stroke agents	11
Design and synthesis of sulfonamides incorporating a biotin moiety: Carbonic anhydrase inhibitory effects, antiproliferative activity and molecular modeling studies	10
Discovery of 1,3,4-oxadiazole derivatives as potential antitumor agents inhibiting the programmed cell death-1/programmed cell death-ligand 1 interaction	10
Graphical Abstract TOC	10
Recent applications of seven-membered rings in drug design	10
Synthesis and biological evaluation of sulfonylpyridine derivatives as potential anti-chlamydia agents	10
Inhibition of the hERG potassium ion channel by different non-nucleoside human cytomegalovirus polymerase antiviral inhibitor series and the exploration of variations on a pyrroloquinoline core to red	10
Discovery of pyrido[4,3-d]pyrimidinone derivatives as novel Wee1 inhibitors	10
Identification of potent α-amylase inhibitors via dynamic combinatorial chemistry	10
Synthesis of sp3-rich chiral bicyclo[3.3.1]nonanes for chemical space expansion and study of biological activities	10
Design, synthesis, and bioactivity study on Lissodendrins B derivatives as PARP1 inhibitor	10
A critical update on the strategies towards small molecule inhibitors targeting Serine/arginine-rich (SR) proteins and Serine/arginine-rich proteins related kinases in alternative splicing	10
Harnessing polyhydroxylated pyrrolidines as a stabilizer of acid alpha-glucosidase (GAA) to enhance the efficacy of enzyme replacement therapy in Pompe disease	10
Targeting the PI3K/mTOR pathway in idiopathic pulmonary fibrosis: Advances and therapeutic potential	10
Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors	10
Discovery of acetohydroxyacid synthase inhibitors as anti-tuberculosis lead compounds from natural products	10
Discovery of Pyrazolo[1,5-a]pyrazin-4-ones as Potent and Brain Penetrant GluN2A-Selective Positive Allosteric Modulators Reducing AMPA Receptor Binding Activity	10
Discovery, Topo I inhibitory activity and mechanism evaluation of two novel cytisine-type alkaloid dimers from the seeds of Sophora alopecuroides L	10
Glutathione-responsive PROTAC for targeted degradation of ERα in breast cancer cells	10
Editorial Board	9
Contents continued	9
Editorial Board	9
Editorial Board	9
Iodoetherification as a strategy towards sp3-rich scaffolds for drug discovery	9
Design and synthesis of multivalent drug delivery system with CA IX inhibitors as ligands	9
Design, synthesis and anti-rheumatoid arthritis activity of target TLR4 inhibitors	9
A new small molecule DoNA binding to CAG repeat RNA	9
Silybins are stereospecific regulators of the 20S proteasome	9
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Editorial Board	9
Discovery of selective covalent cathepsin K inhibitors containing novel 4-cyanopyrimidine warhead based on quantum chemical calculations and binding mode analysis	9
Synthesis of PF-6870961, a major hydroxy metabolite of the novel ghrelin receptor inverse agonist PF-5190457	9
Design, synthesis and bioactivity evaluation of fisetin derivatives as potential anti-inflammatory agents against LPS-induced acute lung injury	9
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Contents continued	9
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Editorial Board	9
Structure activity relationship of pyrazinoic acid analogs as potential antimycobacterial agents	9