RSC Medicinal Chemistry

Article	Citations
Covalent cannabinoid receptor ligands – structural insight and selectivity challenges	103
Exploring the potential of tamoxifen-based copper(ii) dichloride in breast cancer therapy	63
Recent advances of phenotypic screening strategies in the application of anti-influenza virus drug discovery	59
N-Arylsulfonamide-based adenosine analogues to target RNA cap N7-methyltransferase nsp14 of SARS-CoV-2	55
Development of sulfonyl fluoride chemical probes to advance the discovery of cereblon modulators	51
Cytotoxicity of phosphoramidate, bis-amidate and cycloSal prodrug metabolites against tumour and normal cells	48
Expanding the chemical space of ester of quinoxaline-7-carboxylate 1,4-di-N-oxide derivatives as potential antitubercular agents	44
Integrating computational and experimental chemical biology revealed variable anticancer activities of phosphodiesterase isoenzyme 5 inhibitors (PDE5i) in lung cancer	43
Synthesis and biological evaluation of novel D-ring fused steroidal N(2)-substituted-1,2,3-triazoles	42
New azole derivatives linked to indole/indoline moieties combined with FLC against drug-resistant Candida albicans	34
Structure–activity relationship study of PROTACs against hematopoietic prostaglandin D2 synthase	34
Unveiling sultam in drug discovery: spotlight on the underexplored scaffold	33
Metabolic labelling of cancer cells with glycodendrimers stimulate immune-mediated cytotoxicity	33
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Contents list	32
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Inside front cover	25
Thiazole orange-carboplatin triplex-forming oligonucleotide (TFO) combination probes enhance targeted DNA crosslinking	24
Effect of mono-guanidine-like derivatives on platelet aggregation and tumour cell induced platelet aggregation	23
Biocompatible glycolipid derived from bhilawanol as an antibiofilm agent and a promising platform for drug delivery	23
4-Trifluoromethyl bithiazoles as broad-spectrum antimicrobial agents for virus-related bacterial infections or co-infections	23
Unusual Ni⋯Ni interaction in Ni(ii) complexes as potential inhibitors for the development of new anti-SARS-CoV-2 Omicron drugs	22
Design, synthesis, in vitro and in silico evaluation of indole-based tetrazole derivatives as putative anti-breast cancer agents	22
Identification of the first structurally validated covalent ligands of the small GTPase RAB27A	21

Contents list	20
Research progress of anticancer drugs targeting CDK12	20
Sirtuin 1-activating derivatives belonging to the anilinopyridine class displaying in vivo cardioprotective activities	19
Trifluoroacetic acid-mediated synthesis of xanthene constructs and their extensive anti-tuberculosis evaluation	19
Inside front cover	19
Front cover	18
Design, synthesis and biological evaluation of rhein–piperazine–furanone hybrids as potential anticancer agents	18
Tackling antimicrobial stewardship through synergy and antimicrobial peptides	18
Light-activatable photochemically targeting chimeras (PHOTACs) enable the optical control of targeted protein degradation of HDAC6	18
Natural product-inspired [3 + 2] cycloaddition-based spirooxindoles as dual anticancer agents: synthesis, characterization, and biological evaluation by in vitro and in silico methods	18
Recent advances from computer-aided drug design to artificial intelligence drug design	17
Simple accessible clemastine fumarate analogues as effective antileishmanials	17
A story of peptides, lipophilicity and chromatography – back and forth in time	17
Importance of photophosphatidylserine and Tim-3 in photoimmunotherapy	17
Pretargeted imaging beyond the blood–brain barrier	17
A ‘click’ chemistry approach to novel entinostat (MS-275) based class I histone deacetylase proteolysis targeting chimeras	16
Cornulacin: a new isoflavone fromCornulaca monacanthaand its isolation, structure elucidation and cytotoxicity through EGFR-mediated apoptosis	16
Diversely functionalized isoquinolines and their core-embedded heterocyclic frameworks: a privileged scaffold for medicinal chemistry	16
It's ok to be outnumbered – sub-stoichiometric modulation of homomeric protein complexes	16
Design and development of sulfenylated 5-aminopyrazoles as inhibitors of acetylcholinesterase and butyrylcholinesterase: exploring the implication for Aβ1–42 aggregation inhibition in Alzhe	16
Discovery of dibenzylbutane lignan LCA derivatives as potent anti-inflammatory agents	16
Prodrugs and their activation mechanisms for brain drug delivery	15
The physics-AI dialogue in drug design	15
Unravelling the potency of the 4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile scaffold with S-arylamide hybrids as PIM-1 kinase inhibitors: synthesis, biological activity and in	15
Back cover	15
Evolution of 3-(4-hydroxyphenyl)indoline-2-one as a scaffold for potent and selective anticancer activity	15
Exploration of cytotoxic potential and tubulin polymerization inhibition activity of cis-stilbene-1,2,3-triazole congeners	15
Recent insights of PROTAC developments in inflammation-mediated and autoimmune targets: a critical review	14
Design, quality and validation of the EU-OPENSCREEN fragment library poised to a high-throughput screening collection	14
Radiosynthesis of [18F]brequinar for in vivo PET imaging of hDHODH for potential studies of acute myeloid leukemia and cancers	14
Geometric deep learning-guided Suzuki reaction conditions assessment for applications in medicinal chemistry	13
The allure of targets for novel drugs	13
Discovery of imidazo[1,2-b]pyridazine-containing TAK1 kinase inhibitors with excellent activities against multiple myeloma	13
An allosteric inhibitor targeting the STAT3 coiled-coil domain selectively suppresses proliferation of breast cancer	13
Development of Hsp90 C-terminal inhibitors with noviomimetics that manifest anti-proliferative activities	13
Rutaecarpine derivatives synthesized via skeletal reorganization alleviate inflammation-associated oxidative damage by inhibiting the MAPK/NF-κB signaling pathway	13
Design, Synthesis and Anti-proliferative Activity of 3-Aryl-Evodiamines	13
Contents list	13
Hinokitiol potentiates antimicrobial activity of bismuth drugs: a combination therapy for overcoming antimicrobial resistance	13
Druggable targets for the immunopathy of Alzheimer's disease	13
Contents list	12
Correction: Design and synthesis of eugenol/isoeugenol glycoconjugates and other analogues as antifungal agents against Aspergillus fumigatus	12
The importance of tyrosines in multimers of cyclic RGD nonapeptides: towards αvβ6-integrin targeted radiotherapeutics	12
Front cover	12
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Minimising the payload solvent exposed hydrophobic surface area optimises the antibody-drug conjugate properties	11
Can large language models predict antimicrobial peptide activity and toxicity?	11
Enhanced inhibitory activity of compounds containing purine scaffolds compared to protein kinase CK2α considering crystalline water	11
Recent advancements in the development of next-generation dual-targeting antibacterial agents	11

SETDB1 as a cancer target: challenges and perspectives in drug design	11
On-resin synthesis of Lanreotide epimers and studies of their structure–activity relationships	11
Synthesis of novel rapanone derivatives via organocatalytic reductive C-alkylation: biological evaluation of antioxidant properties, in vivo zebrafish embryo toxicity, and docking studie	11
NMR 1H,19F-based screening of the four stem-looped structure 5_SL1–SL4 located in the 5′-untranslated region of SARS-CoV 2 RNA	11
Inhibition of transcription and antiproliferative effects in a cancer cell line using antigene oligonucleotides containing artificial nucleoside analogues	11
Novel rhodanine–thiazole hybrids as potential antidiabetic agents: a structure-based drug design approach	10
Stachydrine, a pyrrole alkaloid with promising therapeutic potential against metabolic syndrome and associated organ dysfunction	10
Insights into the modular design of kinase inhibitors and application to Abl and Axl	10
Recent advancements in the therapeutic approaches for Alzheimer's disease treatment: current and future perspective	10
Design, synthesis and evaluation of 2-phenylpyrimidine derivatives as novel antifungal agents targeting CYP51	10
Stereochemical optimization of N,2-substituted cycloalkylamines as norepinephrine reuptake inhibitors	10
Discovery of a nasal spray steroid, tixocortol, as an inhibitor of SARS-CoV-2 main protease and viral replication	10
Scaffold hopping from indoles to indazoles yields dual MCL-1/BCL-2 inhibitors from MCL-1 selective leads	10
Exploration of piperidine 3D fragment chemical space: synthesis and 3D shape analysis of fragments derived from 20 regio- and diastereoisomers of methyl substituted pipecolinates	10
Pyridazinone-based derivatives as anticancer agents endowed with anti-microbial activity: molecular design, synthesis, and biological investigation	10
NIR-II imaging of hepatocellular carcinoma based on a humanized anti-GPC3 antibody	10
Synthesis, biological evaluation and computational studies of pyrazole derivatives as Mycobacterium tuberculosis CYP121A1 inhibitors	10
Inside front cover	9
Anticancer potential of copper(i) complexes based on isopropyl ester derivatives of bis(pyrazol-1-yl)acetate ligands	9
Evaluation of ketoclomazone and its analogues as inhibitors of 1-deoxy-d-xylulose 5-phosphate synthases and other thiamine diphosphate (ThDP)-dependent enzymes	9
Mycobacterium tuberculosis CitA activity is modulated by cysteine oxidation and pyruvate binding	9
Design, synthesis, and biological evaluation of novel thiazole derivatives as PI3K/mTOR dual inhibitors	9
Back cover	9
Development of di-arylated 1,2,4-triazole-based derivatives as therapeutic agents against breast cancer: synthesis and biological evaluation	9
Identification of novel phenylalanine derivatives bearing a hydroxamic acid moiety as potent quorum sensing inhibitors	9
“Seasoning” antimalarial drugs' action: chloroquine bile salts as novel triple-stage antiplasmodial hits	9
Site-specific molecular glues for the 14-3-3/Tau pS214 protein–protein interaction via reversible covalent imine tethering	9
Inside front cover	9
Adjuvant strategies to tackle mcr-mediated polymyxin resistance	9
Design and evaluation of poly-nitrogenous adjuvants capable of potentiating antibiotics in Gram-negative bacteria	9
Progress in the discovery and development of small molecule methuosis inducers	9
Target 2035 – update on the quest for a probe for every protein	9
Contents list	9
Quinazolinone-1,2,3-triazole-acetamide conjugates as potent α-glucosidase inhibitors: synthesis, enzyme inhibition, kinetic analysis, and molecular docking study	8
Technical, preclinical, and clinical developments of Fc-glycan-specific antibody–drug conjugates	8
Discovery of 2,3-dihydro-1H-pyrrolo[3,4-b]quinolin-1-one derivatives as possible antileishmanial agents	8
Design and synthesis of novel cathepsin C inhibitors with anti-inflammatory activity	8
Contents list	8
Novel tetrahydropyrimidinyl-substituted benzimidazoles and benzothiazoles: synthesis, antibacterial activity, DNA interactions and ADME profiling	8
Inside front cover	8
Semisynthetic blasticidin S ester derivatives show enhanced antibiotic activity	8
Ribosome-targeting antibiotics and resistance via ribosomal RNA methylation	8
SLL-1A-16 suppresses proliferation and induces autophagy in non-small-cell lung cancer cells via the AKT/mTOR signaling pathway	8
Research progress of metal–organic framework nanozymes in bacterial sensing, detection, and treatment	8
Rational design and in vitro testing of new urease inhibitors to prevent urinary catheter blockage	8
Distinctive roles of aquaporins and novel therapeutic opportunities against cancer	8
Development of trisubstituted thiophene-3-arboxamide selenide derivatives as novel EGFR kinase inhibitors with cytotoxic activity	7
Insights into the recent progress in the medicinal chemistry of pyranopyrimidine analogs	7
The synthesis and bioactivities of ROCK2 inhibitors with 1,2-dithiolan-3-yl motif	7
Molecular understanding of the therapeutic potential of melanin inhibiting natural products	7
Synthesis and pharmacological evaluation of 1,3-diaryl substituted pyrazole based (thio)urea derivatives as potent antimicrobial agents against multi-drug resistant Staphylococcus aureus and	7
Identification of SARS-CoV-2 Mpro inhibitors through deep reinforcement learning for de novo drug design and computational chemistry approaches	7
AlbiCDN: albumin-binding amphiphilic STING agonists augment the immune activity for cancer immunotherapy	7
Design and synthesis of cyclic lipidated peptides derived from the C-terminus of Cx43 for hemichannel inhibition and cardiac endothelium targeting	7
Integrating a quinone substructure into histone deacetylase inhibitors to cope with Alzheimer's disease and cancer	7
Inhibition of DXR in the MEP pathway with lipophilic N-alkoxyaryl FR900098 analogs	7
Thiazolidine-2,4-dione hybrids as dual alpha-amylase and alpha-glucosidase inhibitors: design, synthesis, in vitro and in vivo anti-diabetic evaluation	7
Inhibition of bacterial RNA polymerase function and protein–protein interactions: a promising approach for next-generation antibacterial therapeutics	7
Guggulsterone – a potent bioactive phytosteroid: synthesis, structural modification, and its improved bioactivities	7
Synthesis and Antiplasmodial Activity of 6H,13H-Pyrazino[1,2-a;4,5-a′]diindole Analogues Substituted with Basic Side Chains	7
Recent developments in membrane targeting antifungal agents to mitigate antifungal resistance	7
Complexity of αvβ6-integrin targeting RGD peptide trimers: emergence of non-specific binding by synergistic interaction	7
Development of thiazole-appended novel hydrazones as a new class of α-amylase inhibitors with anticancer assets: anin silicoandin vitroapproach	7
Introduction to the themed collection in honour of Professor Christian Leumann	7
Correction: Minimising the payload solvent exposed hydrophobic surface area optimises the antibody–drug conjugate properties	6
Polysucrose hydrogel loaded with natural molecules/extracts for multiphase-directed sustainable wound healing	6
Stereoselective synthesis and antiproliferative activity of allo-gibberic acid-based 1,3-aminoalcohol regioisomers	6
Applications of supramolecular assemblies in drug delivery and photodynamic therapy	6
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Contents list	6
Front cover	6
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism	6
Design, synthesis, molecular docking and anti-proliferative activity of novel phenothiazine containing imidazo[1,2-a]pyridine derivatives against MARK4 protein	6
Novel pirfenidone derivatives: synthesis and biological evaluation	6
Synthesis of full-length homodimer αD-VxXXB that targets human α7 nicotinic acetylcholine receptors	6
Front cover	6
Contents list	6
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Synthesis and structure–activity relationship (SAR) studies of 1,2,3-triazole, amide, and ester-based benzothiazole derivatives as potential molecular probes for tau protein	6
Development, biological evaluation, and molecular modelling of novel isocytosine and guanidine derivatives as BACE1 inhibitors using a fragment growing strategy	6

Copper selective 8-aminoquinoline based tetradentate chelators as anticancer agents	6
Expanding the chemical space for antiviral discovery: the potential of twistenediones	6
The Mycobacterium tuberculosis mycothiol S-transferase is divalent metal-dependent for mycothiol binding and transfer	6
QSAR, structure-based pharmacophore modelling and biological evaluation of novel platelet ADP receptor (P2Y12) antagonist	6
Contents list	6
Introduction to the themed collection on ‘Targeting RNA with small molecules’	6
Preventing SARS-CoV-2 infection using Fv-antibodies targeting the proprotein convertase (PPC) cleavage site	6
Expanding the structure–activity relationships of alkynyl diphenylurea scaffold as promising antibacterial agents	6
Design, synthesis and biological evaluation of light-driven on–off multitarget AChE and MAO-B inhibitors	6
Live cell screening to identify RNA-binding small molecule inhibitors of the pre-let-7–Lin28 RNA–protein interaction	6
Design, synthesis, and biological evaluation of new arjunolic acid derivatives as anticancer agents	6
From traditional medicine to nanomedicine: potential of Ginkgo biloba extracts in treating inflammatory skin diseases	5
Discovery and computational studies of piperidine/piperazine-based compounds endowed with sigma receptor affinity	5
The era of high-quality chemical probes	5
Design, synthesis, inhibitory activity, and molecular simulations study for d-glucose-conjugated thioureas containing pyrimidine ring as multitarget inhibitors against α-amylase, α-glucosid	5
Near-infrared photochemical internalization: design of a distorted zinc phthalocyanine for efficient intracellular delivery of immunotoxins	5
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Designed hybrid anticancer nuclear-localized peptide inhibits aggressive cancer cell proliferation	5
Design, synthesis, and evaluation of benzhydrylpiperazine-based novel dual COX-2/5-LOX inhibitors with anti-inflammatory and anti-cancer activity	5
Targeting host integrated stress response: lead discovery of flavonoid compounds active against coronaviruses PEDV and PDCoV	5
Novel benzimidazole-based pseudo-irreversible butyrylcholinesterase inhibitors with neuroprotective activity in an Alzheimer's disease mouse model	5
Enhanced skin penetration of curcumin by a nanoemulsion-embedded oligopeptide hydrogel for psoriasis topical therapy	5
Front cover	5
Phenylthiazoles with potent & optimum selectivity toward Clostridium difficile	5
News from RSC Medicinal Chemistry	5
Mannich reaction mediated derivatization of chromones and their biological evaluations as putative multipotent ligands for the treatment of Alzheimer's disease	5
Synthetic 18F labeled biomolecules that are selective and promising for PET imaging: major advances and applications	5
Semisynthetic polymyxins with potent antibacterial activity and reduced kidney cell toxicity	5
Design, synthesis and in vitro evaluations of new cyclotriphosphazenes as safe drug candidates	5
Discovery of benzoheterocyclic-substituted amide derivatives as apoptosis signal-regulating kinase 1 (ASK1) inhibitors	5
Ruthenium(ii)–arene complexes as anti-metastatic agents, and related techniques	5
Design and synthesis of coumarin-based amphoteric antimicrobials with biofilm interference and immunoregulation effects	5
Heterocyclic compounds as xanthine oxidase inhibitors for the management of hyperuricemia: synthetic strategies, structure–activity relationship and molecular docking studies (2018–2024)	5
Design and synthesis of novel 8-(azaindolyl)-benzoazepinones as potent and selective ROCK inhibitors	5
Benzenesulfonamide decorated dihydropyrimidin(thi)ones: carbonic anhydrase profiling and antiproliferative activity	5
Discovery of selective, metabolically stable pyrazole-based FLT3 inhibitors for the treatment of acute myeloid leukemia	5
Front cover	5
Novel flexible biphenyl PfDHFR inhibitors with improved antimalarial activity	5
Contents list	5
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Modulating polybasic character of galactose-based glycosylated antitumor ether lipids for enhanced cytotoxic response	5
Repurposing of USFDA-approved drugs to identify leads for inhibition of acetylcholinesterase enzyme: a plausible utility as an anti-Alzheimer agent	5
Discovery of first-in-class PROTACs targeting maternal embryonic leucine zipper kinase (MELK) for the treatment of Burkitt lymphoma	5
Exploring medium and long arm extensions of 1,2,4-triazole derivatives as Candida albicans 14α-demethylase (CYP51) inhibitors	5
Design, synthesis, and SAR of antiproliferative activity of trioxatriangulene derivatives	5
The development of a PET radiotracer for imaging alpha synuclein aggregates in Parkinson's disease	5
An overview of the development of EED inhibitors to disable the PRC2 function	5
Design, synthesis, antimicrobial activity, stability, and mechanism of action of bioresorbable ceragenins	5
Discovery and optimisation of pyrazolo[1,5-a]pyrimidines as aryl hydrocarbon receptor antagonists	5
In vitro evaluation of the immunogenic potential of gramicidin S and its photocontrolled analogues	5
Development of pharmacophore models for AcrB protein and the identification of potential adjuvant candidates for overcoming efflux-mediated colistin resistance	5
Synthesis and evaluation of tetrahydropyrrolo[1,2-a]quinolin-1(2H)-ones as new tubulin polymerization inhibitors	5
PK 11195 derivatives: exploring the influence of amide and heterocyclic substitution on A147T TSPO discrimination	5
Contents list	5
Synthesis and properties of the kojic acid dimer and its potential for the treatment of Alzheimer's disease	5
The bench to bedside journey of tricyclo-DNA antisense oligonucleotides for the treatment of Duchenne muscular dystrophy	4
A concise review on hPXR ligand-recognizing residues and structure-based strategies to alleviate hPXR transactivation risk	4
Overview of the structure, side effects, and activity assays of l-asparaginase as a therapy drug of acute lymphoblastic leukemia	4
Front cover	4
Design, synthesis and preliminary biological evaluation of rivastigmine-INDY hybrids as multitarget ligands against Alzheimer's disease by targeting butyrylcholinesterase and DYRK1A/CLK1 kinases	4
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Asymmetric imidazole-4,5-dicarboxamide derivatives as SARS-CoV-2 main protease inhibitors: design, synthesis and biological evaluation	4
Systematic computational strategies for identifying protein targets and lead discovery	4
Expanding the scope of novel 1,2,3-triazole derivatives as new antiparasitic drug candidates	4
Contents list	4
Chromenochalcones: A Comprehensive Review on Developments Towards Medicinal Perspective	4
Identification of lysosomotropism using explainable machine learning and morphological profiling cell painting data	4
Evaluation of the effect of a cell penetrating peptide (TAT) towards tailoring the targeting efficacy and tumor uptake of porphyrin	4
Research status of indole-modified natural products	4
Bioorthogonal activation of prodrugs, for the potential treatment of breast cancer, using the Staudinger reaction	4
Concise synthesis and biological activity evaluation of novel pyrazinyl–aryl urea derivatives against several cancer cell lines, which can especially induce T24 apoptotic and necroptotic cell death	4
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Ebselen analogues with dual human neutrophil elastase (HNE) inhibitory and antiradical activity	4
Targeted protein degradation using the lysosomal pathway	4
Exploring 7β-amino-6-nitrocholestens as COVID-19 antivirals: in silico, synthesis, evaluation, and integration of artificial intelligence (AI) in drug design: assessing the cytotoxicity and ant	4
Antitubercular evaluation of dihydropyridine–triazole conjugates: design, synthesis, in vitro screening, SAR and in silico ADME predictions	4
Morpholine substituted quinazoline derivatives as anticancer agents against MCF-7, A549 and SHSY-5Y cancer cell lines and mechanistic studies	4
Armeniaspirol analogues with more potent Gram-positive antibiotic activity show enhanced inhibition of the ATP-dependent proteases ClpXP and ClpYQ	4
Design and synthesis of novel multi-target tetrabromophthalimides as CBS and Topo-II inhibitors and DNA intercalators	4
Phosphonodiamidate prodrugs of phosphoantigens (ProPAgens) exhibit potent Vγ9/Vδ2 T cell activation and eradication of cancer cells	4
Contents list	4
Visible and NIR light photoactivatableo-hydroxycinnamate system for efficient drug release with fluorescence monitoring	4
S-MGBs bearing amidine tail groups are potent, selective antiplasmodial agents	4
Correction: Concise synthesis and biological activity evaluation of novel pyrazinyl–aryl urea derivatives against several cancer cell lines, which can especially induce T24 apoptotic and necroptotic c	4
Back cover	4
Naphthylthiazoles: a class of broad-spectrum antifungals	4
Novel curcumin-based analogues as potential VEGFR2 inhibitors with promising metallic loading nanoparticles: synthesis, biological evaluation, and molecular modelling investigation	4
Fexinidazole optimization: enhancing anti-leishmanial profile, metabolic stability and hERG safety	4
Overview of CFTR activators and their recent studies for dry eye disease: a review	4
Prediction of synergistic gemcitabine-based combination treatment through a novel tumor stemness biomarker NANOG in pancreatic cancer	4
Covalent drugs targeting histidine – an unexploited opportunity?	4
Synthesis of tryptanthrin appended dispiropyrrolidine oxindoles and their antibacterial evaluation	4
Antiproliferative effects, mechanism of action and tumor reduction studies in a lung cancer xenograft mouse model of an organometallic gold(i) alkynyl complex	4