Bioorganic & Medicinal Chemistry

Article	Citations
Editorial Board	329
Design and synthesis of multivalent drug delivery system with CA IX inhibitors as ligands	80
Steroidal alkaloids isolated from Veratrum grandiflorum Loes. as novel Smoothened inhibitors with anti-proliferation effects on DAOY medulloblastoma cells	75
Discovery of novel indazole derivatives as SOS1 agonists that activate KRAS signaling	71
Systematic assessment of structure-promiscuity relationships between different types of kinase inhibitors	68
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Discovery of novel tripeptide propylene oxide proteasome inhibitors for the treatment of multiple myeloma	60
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Graphical abstract TOC	49
A gemcitabine-based conjugate with enhanced antitumor efficacy by suppressing HIF-1α expression under hypoxia	42
Discovery of fluorinated 2‑Styryl 4(3H)-quinazolinone as potential therapeutic hit for oral cancer	38
Production and synthesis of a novel 191Pt-labeled platinum complex and evaluation of its biodistribution in healthy mice	38
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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	36
Graphical Abstract Contents Continued	35
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Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists	33
Synthesis, anticancer activity and molecular docking studies of N-deacetylthiocolchicine and 4-iodo-N-deacetylthiocolchicine derivatives	32
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Daphnanes diterpenes from the latex of Hura crepitans L. and their PKCζ-dependent anti-proliferative activity on colorectal cancer cells	30
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Contents continued	29
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Which boronic acids are used most frequently for synthesis of bioactive molecules?	26

Contents continued	26
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Design, synthesis and evaluation of 1-benzyl-1H-imidazole-5-carboxamide derivatives as potent TGR5 agonists	26
Aromatic oligoesters as novel helix mimetic scaffolds	26
There’s more to enzyme antagonism than inhibition	25
Structure activity relationship of pyrazinoic acid analogs as potential antimycobacterial agents	25
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	25
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	25
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Discovery of selective covalent cathepsin K inhibitors containing novel 4-cyanopyrimidine warhead based on quantum chemical calculations and binding mode analysis	25
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Synthesis and biological evaluation of 3-styrylchromone derivatives as selective monoamine oxidase B inhibitors	24
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Design, synthesis and biological evaluation of double fatty chain-modified glucagon-like peptide-1 conjugates	24
Graphical Abstract Contents Continued	24
Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis	23
Impact of α-modifications on the activity of triazole bisphosphonates as geranylgeranyl diphosphate synthase inhibitors	23
Design, synthesis and validation of a new Crimped Head-Piece for DNA-Encoded libraries generation	23
Design, synthesis and evaluate of indazolylaminoquinazoline derivatives as potent Tropomyosin receptor kinase (TRK) inhibitors	22
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SAR study of N′-(Salicylidene)heteroarenecarbohydrazides as promising antifungal agents	22
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Design and synthesis of a DNA-encoded combinatorial library of bicyclic peptoids	21
Synthesis of PF-6870961, a major hydroxy metabolite of the novel ghrelin receptor inverse agonist PF-5190457	21
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Discovery of novel 2,8-diazaspiro[4.5]decan-1-one derivatives as potent RIPK1 kinase inhibitors	21
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Design, synthesis, evaluation and optimization of novel azole analogues as potent antifungal agents	21
Iodoetherification as a strategy towards sp3-rich scaffolds for drug discovery	20
Structure-based drug design of novel and highly potent pyruvate dehydrogenase kinase inhibitors	20
Graphical Abstract Contents Continued	20
Design, synthesis and bioactivity evaluation of fisetin derivatives as potential anti-inflammatory agents against LPS-induced acute lung injury	20
Design, synthesis and antitumor activity of 2-substituted quinazoline-4-amine derivatives	20
A DNA-encoded library special issue	20
Rational design of prodrug-type apoB-targeted siRNA for nuclease resistance improvement without compromising gene silencing potency	19
Novel ferrocenylbisphosphonate hybrid compounds: Synthesis, characterization and potent activity against cancer cell lines	19
Synthesis and evaluation of dual fatty acid amide hydrolase-monoacylglycerol lipase inhibition and antinociceptive activities of 4-methylsulfonylaniline-derived semicarbazones	19
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	19
Graphical abstract TOC	18
Synthesis and biological evaluation of 1H-pyrrolo[3,2–g]isoquinolines	18
Mechanism-based inhibition of GH127/146 cysteine glycosidases by stereospecifically functionalized l-arabinofuranosides	18
Graphical abstract TOC	18
Discovery of 5-methylpyrimidopyridone analogues as selective antimycobacterial agents	18
Scope of on-DNA nucleophilic aromatic substitution on weakly-activated heterocyclic substrates for the synthesis of DNA-encoded libraries	18
Design and synthesis of boron-containing ALK inhibitor with favorable in vivo efficacy	18
Editorial Board	17
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	17
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Repurposing primaquine as a polyamine conjugate to become an antibiotic adjuvant	17
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Editorial Board	17
Design, synthesis and biological evaluation studies of novel anti-fibrosis agents bearing sulfoxide moiety	17
Discovery of chiral 1,4-diarylazetidin-2-one-based hydroxamic acid derivatives as novel tubulin polymerization inhibitors with histone deacetylase inhibitory activity	17
Graphical abstract TOC	16
Linker optimization and activity validation of a cell surface vimentin targeted homo-dimeric peptoid antagonist for lung cancer stem cells	16
Synthesis of lathyrane diterpenoid nitrogen-containing heterocyclic derivatives and evaluation of their anti-inflammatory activities	16
Structural optimization of a lysine demethylase 5 inhibitor for improvement of its cellular activity	16
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Synthesis and antiviral activity of formycin derivatives with anti-influenza virus activity	15
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Graphical Abstract Continued	15
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	15
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10-Alkoxy-anthracenyl-isoxazole analogs have sub-micromolar activity against a Glioblastoma multiforme cell line	15
Discovery of potent dual ligands for dopamine D4 and σ1 receptors	15
Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor	15
Editorial Board	14
Editorial Board	14
Graphical Abstract Contents Continued	14
Development of delivery carriers for plasmid DNA by conjugation of a helical template to oligoarginine	14
Polyguluronate simulations shed light onto the therapeutic action of OligoG CF-5/20	14
Editorial Board	14
Crescent-shaped meta-substituted benzene derivatives as a new class of non-nucleoside ribonuclease A inhibitors	14
A simplified analog of debromoaplysiatoxin lacking the B-ring of spiroketal moiety retains protein kinase C-binding and antiproliferative activities	14
Synthesis and physical and biological properties of 1,3-diaza-2-oxophenoxazine-conjugated oligonucleotides	14
Editorial Board	14
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Synthetic approaches to FDA approved drugs for asthma and COPD from 1969 to 2020	14
DNA-encoded C H functionality via photoredox-mediated hydrogen atom transformation catalysis	14
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Design, synthesis, and biological evaluation of stapled ascaphin-8 peptides	13
Targeting m6A binding protein YTHDFs for cancer therapy	13
Discovery of a new class of valosine containing protein (VCP/P97) inhibitors for the treatment of colorectal cancer	13
Rational design of cannabinoid type-1 receptor allosteric modulators: Org27569 and PSNCBAM-1 hybrids	13
Medicinal chemistry perspectives on the development of piperazine-containing HIV-1 inhibitors	13
New substituted benzoxazine derivatives as potent inducers of membrane permeability and cell death	13
A bleomycin-mimicking manganese-porphyrin-conjugated mitochondria-targeting peptoid for cancer therapy	13
A review of MMP-2 structures and binding mode analysis of its inhibitors to strategize structure-based drug design	13
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	13
A kind of HIV-1 protease inhibitors containing phenols with antiviral activity against DRV-resistant variants	13
Bioisoteres for carboxylic acids: From ionized isosteres to novel unionized replacements	13
Anti-HER2 monoclonal antibody based-radioimmunoconjugates: Assessment of the chelating agent influence	13
Synthesis and biological evaluation of lappaconitine analogues as potential anti-neuroinflammatory agents by side chain modification and scaffold hopping strategy	13
Modulation of proteasome subunit selectivity of syringolins	13
Editorial Board	13
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	13
Design and synthesis of proteolysis-targeting chimeras (PROTACs) as degraders of glutathione peroxidase 4	13
Skin- and airway-deliverable TRPA1 inhibitor	12
SAR evolution towards potent C-terminal carboxamide peptide inhibitors of Zika virus NS2B-NS3 protease	12
Synthesis and biological evaluation of pyrazole-fused oleanolic acid derivatives as novel inhibitors of inflammatory and osteoclast differentiation	12
Synthesis and structural optimization of oncolytic peptide LTX-315	12
Design, synthesis, and molecular simulation studies of N-phenyltetrahydroquinazolinones as protoporphyrinogen IX oxidase inhibitors	12
Discovery of novel pyrimidine molecules containing boronic acid as VCP/p97 Inhibitors	12
Small molecule inhibitor E-64 exhibiting the activity against African swine fever virus pS273R	12
Sustainable electrochemical C(sp3) − H oxygenation using water as the oxygen source	12
A novel selective estrogen receptor degrader induces cell cycle arrest in breast cancer via ERα degradation and the autophagy-lysosome pathway	12
Design, synthesis and evaluation of novel prostate-specific membrane antigen-targeted aryl [18F]fluorosulfate PET tracers	12
Amine-bearing hydrocarbon cross-links: Tailoring helix stability, hydrophilicity, and synthetic adaptability in peptides	12
Structure-activity relationship studies on divalent naphthalene diimide G quadruplex ligands with anticancer and antiparasitic activity	12
Dipyridyl-substituted thiosemicarbazone as a potent broad-spectrum inhibitor of metallo-β-lactamases	12
Auranofin inhibits virulence pathways in Pseudomonas aeruginosa	12
Multi-target potential of newly designed tacrine-derived cholinesterase inhibitors: Synthesis, computational and pharmacological study	12
Novel hybrid conjugates with dual estrogen receptor α degradation and histone deacetylase inhibitory activities for breast cancer therapy	12
Design, synthesis and biological evaluation of naphthyl amide derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors	12
Directed evolution of an amine transaminase for the synthesis of an Apremilast intermediate via kinetic resolution	12
N3-Methyluridine and 2′-O-Alkyl/2′-Fluoro-N3-methyluridine functionalized nucleic acids improve nuclease resistance while maintaining duplex geometry	12
Design, synthesis and anticancer activity evaluation of 4-(3-1H-indazolyl)amino quinazoline derivatives as PAK4 inhibitors	12
Synthesis and biological evaluation of orally active anti-Trypanosoma agents	12
Selective targeting of human TET1 by cyclic peptide inhibitors: Insights from biochemical profiling	12
Ionization and lipophilicity in nonpolar media mimicking the cell membrane interior	12
Design, synthesis and biological evaluation of novel 9-N-substituted-13-alkylberberine derivatives from Chinese medicine as anti-hepatocellular carcinoma agents	12

RNA-templated chemical synthesis of proapoptotic L- and d-peptides	12
Oropouche virus – The “Newest” invisible public enemy?	11
Inhibition of amyloid formation of amyloid β (1–42), amylin and insulin by 1,5-diazacyclooctanes, a spermine-acrolein conjugate	11
Design, Synthesis, and Biological Evaluation of New 1H-Imidazole-2-Carboxylic Acid Derivatives as Metallo-β-Lactamase Inhibitors	11
Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy	11
Pentafluorosulfanyl-substituted biaryl derivatives as MATE-type transporter inhibitors targeting drug-resistant bacteria	11
Discovery of benzo[f]pyrido[4,3-b][1,4]oxazepin-10-one derivatives as orally available bromodomain and extra-terminal domain (BET) inhibitors with efficacy in an in vivo psoriatic animal model	11
Structure-based design and optimization of a new class of small molecule inhibitors targeting the P-stalk binding pocket of ricin	11
How kelch domain-containing protein 3 distinguishes between the C-end degron of herpesviral protein UL49.5 and its mutants – Insights from molecular dynamics	11
Exploring novel A2AAR antagonists: Design, synthesis, and evaluation of 2,6,9-trisubstituted purine derivatives as promising antifibrotic agents	11
A novel tricyclic β-lactam exhibiting potent antibacterial activities against carbapenem-resistant Enterobacterales: Synthesis and structure-activity-relationships	11
A comprehensive review on the biological interest of quinoline and its derivatives	11
Targeting prolidase. A survey of the literature data to depict a structure-activity relationship frame and to address future studies for drug development	11
Targeting glioma with heteroaromatic alkaloids: A review of potential therapeutics	11
Identification of benzamides derivatives of norfloxacin as promising microRNA-21 inhibitors via repressing its transcription	11
Design and synthesis of efficient fluororethylene-peptidomimetic inhibitors of dipeptidyl peptidase III (DPP3)	11
Discovery of benzimidazole derivatives as potent and selective aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors with glucose consumption improving activity	11
Efficient synthesis of indole-chalcones based glycohybrids and their anticancer activity	11
From triazolophthalazines to triazoloquinazolines: A bioisosterism-guided approach toward the identification of novel PCAF inhibitors with potential anticancer activity	11
Discovery of 3-hydroxymethyl-azetidine derivatives as potent polymerase theta inhibitors	11
Antimycobacterial and anti-inflammatory activities of thiourea derivatives focusing on treatment approaches for severe pulmonary tuberculosis	11
Withaferin A, a polyfunctional pharmacophore that includes covalent engagement of IPO5, is an inhibitor of influenza A replication	11
Design, synthesis, and antiviral activity of a series of CD4-mimetic small-molecule HIV-1 entry inhibitors	11
Self-assembly of photosensitive and radiotherapeutic peptide for combined photodynamic-radio cancer therapy with intracellular delivery of miRNA-139-5p	11
Research progress of multi-target HDAC inhibitors blocking the BRD4-LIFR-JAK1-STAT3 signaling pathway in the treatment of cancer	11
Histone deacetylase (HDAC) inhibitor specificity determinants are preserved in a class of dual HDAC/non-covalent proteasome inhibitors	11
Research progress of STAT3-based dual inhibitors for cancer therapy	10
Fragment-based lead discovery to identify novel inhibitors that target the ATP binding site of pyruvate dehydrogenase kinases	10
Design, synthesis and biological evaluation of the tumor hypoxia-activated PROTACs bearing caged CRBN E3 ligase ligands	10
Synthesis and evaluation of sulfonamide derivatives targeting EGFR790M/L858R mutations and ALK rearrangement as anticancer agents	10
Junctions in DNA: underexplored targets for therapeutic intervention	10
Design, synthesis, kinetic, molecular dynamics, and hypoglycemic effect characterization of new and potential selective benzimidazole derivatives as Protein Tyrosine Phosphatase 1B inhibitors	10
A trio of quinoline-isoniazid-phthalimide with promising antiplasmodial potential: Synthesis, in-vitro evaluation and heme-polymerization inhibition studies	10
DeepAS – Chemical language model for the extension of active analogue series	10
Substituents of life: The most common substituent patterns present in natural products	10
SAR insights into TET2 catalytic domain inhibition: Synthesis of 2-Hydroxy-4-Methylene-pentanedicarboxylates	10
Design, synthesis and biological evaluation of colchicine glycoconjugates as tubulin polymerization inhibitors	10
A computer-aided drug design approach to discover tumour suppressor p53 protein activators for colorectal cancer therapy	10
Iodinated 1,2-diacylhydrazines, benzohydrazide-hydrazones and their analogues as dual antimicrobial and cytotoxic agents	10
Synthesis and evaluation of trypanocidal activity of derivatives of naturally occurring 2,5-diphenyloxazoles	10
Indolylarylsulfones bearing phenylboronic acid and phenylboronate ester functionalities as potent HIV‑1 non-nucleoside reverse transcriptase inhibitors	10
18F-Labeled o‑aminopyridyl alkynyl radioligands targeting colony-stimulating factor 1 receptor for neuroinflammation imaging	10
Discovery of novel macrocyclic derivatives as potent and selective cyclin-dependent kinase 2 inhibitors	10
Novel methyllycaconitine analogues selective for the α4β2 over α7 nicotinic acetylcholine receptors	10
Multiple approaches to repurposing drugs for neuroblastoma	10
Structure-activity relationship and mechanistic study on guggulsterone derivatives; Discovery of new anti-pancreatic cancer candidate	10
Effects of β-lapachone and β-nor-lapachone on multidrug efflux transporters and biofilms of Candida glabrata	10
A new small molecule DoNA binding to CAG repeat RNA	10
Improving the solubility of anti-proliferative thieno[2,3-b]quinoline-2-carboxamides	10
Axial chirality and affinity at the GABAA receptor of triazolobenzodiazepines	10
Synthesis and biological evaluation of novel 1,4-benzodiazepin-3-one derivatives as potential antitumor agents against prostate cancer	10
Short peptide pharmacophores developed from protein phosphatase-1 disrupting peptides (PDPs)	10
Current and emerging therapies for Achondroplasia: The dawn of precision medicine	10
Synthesis and medicinal chemistry of tetronamides: Promising agrochemicals and antitumoral compounds	10
Synthesis and antiproliferative activity of (−)-cleistenolide, (6S)-cleistenolide and 4-substituted cleistenolide analogues	10
Diterpenoids from the whole plants of Croton yunnanensis and their bioactivities	9
Antiviral strategies targeting host factors and mechanisms obliging +ssRNA viral pathogens	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
Revisiting recent unusual drug-DNA complex structures: Implications for cancer and neurological disease diagnostics and therapeutics	9
Fused chromeno and quinolino[1,8]naphthyridines: Synthesis and biological evaluation as topoisomerase I inhibitors and antiproliferative agents	9
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	9
Synthesis and evaluation of curcumin-based near-infrared fluorescent probes for detection of amyloid β peptide in Alzheimer mouse models	9
Endothelial cell spreading on lipid bilayers with combined integrin and cadherin binding ligands	9
Synthesis of kanamycin-azole hybrids and investigation of their antifungal activities	9
Editorial Board	9
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	9
Cathepsin D inhibitors based on tasiamide B derivatives with cell membrane permeability	9
Expedient discovery for novel antifungal leads: 1,3,4-Oxadiazole derivatives bearing a quinazolin-4(3H)-one fragment	9
Design, synthesis and biological evaluation of salicylanilides as novel allosteric inhibitors of human pancreatic lipase	9
Synthesis of alpha-Gal C-disaccharides	9
Facile incorporation of non-canonical heme ligands in myoglobin through chemical protein synthesis	9
Design and synthesis of a fluorescent probe to develop a fluorescence polarization assay for the E3 ligase FEM1C	9
Benzobis(imidazole) derivatives as STAT3 signal inhibitors with antitumor activity	9
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	9
Site-specific construction of triptolide-based antibody-drug conjugates	9
An insight into the medicinal attributes of berberine derivatives: A review	9
Discovery of a novel photoswitchable PI3K inhibitor toward optically-controlled anticancer activity	9
Synthesis, bioevaluation and docking studies of new imidamide derivatives as nitric oxide synthase inhibitors	9
Triple branched RGD modification on liposomes: A prospective strategy to enhance the glioma targeting efficiency	9
Synthesis, microbiological evaluation and structure activity relationship analysis of linezolid analogues with different C5-acylamino substituents	9
Probing for optimal photoaffinity linkers of benzophenone-based photoaffinity probes for adenylating enzymes	9
Integrated lipidomics and network pharmacology analysis of the protective effects and mechanism of Yuanzhi San on rats with cognitive impairment	9
Development of flavonoid probes and the binding mode of the target protein and quercetin derivatives	9
Discovery of cyanoguanidine derivatives as biased μ-opioid receptor agonists	9
Discovery of selective platelet-derived growth factor receptor-beta (PDGFR-β) bifunctional small-molecule degraders	9
Development of QTMP: A promising anticancer agent through NP-Privileged Motif-Driven structural modulation	9
Janus dendritic ionizable lipids with fine designed headgroup and tails to improve mRNA delivery efficiency	8
Editorial Board	8
De novo design with deep generative models based on 3D similarity scoring	8
Current Japanese pharmaceutical chemistry	8
Sulfonamide-derivatized galactosides selectively target an unexplored binding site in the galectin-9N-terminal domain	8
An overview of GPX4-targeting TPDs for cancer therapy	8
Proteolysis targeting chimera of BI-2536 induces potent dual degradation of PLK1 and BET proteins	8
The application of PROTACs in immune-inflammation diseases	8
Synthesis and evaluation of 1,2,3-dithiazole inhibitors of the nucleocapsid protein of feline immunodeficiency virus (FIV) as a model for HIV infection	8