RSC Medicinal Chemistry

Article	Citations
Covalent cannabinoid receptor ligands – structural insight and selectivity challenges	114
Exploring the potential of tamoxifen-based copper(ii) dichloride in breast cancer therapy	82
Recent advances of phenotypic screening strategies in the application of anti-influenza virus drug discovery	68
Expanding the chemical space of ester of quinoxaline-7-carboxylate 1,4-di-N-oxide derivatives as potential antitubercular agents	58
Structure–activity relationship study of PROTACs against hematopoietic prostaglandin D2 synthase	57
Synthesis and biological evaluation of novel D-ring fused steroidal N(2)-substituted-1,2,3-triazoles	57
New azole derivatives linked to indole/indoline moieties combined with FLC against drug-resistant Candida albicans	55
Metabolic labelling of cancer cells with glycodendrimers stimulate immune-mediated cytotoxicity	54
N-Arylsulfonamide-based adenosine analogues to target RNA cap N7-methyltransferase nsp14 of SARS-CoV-2	50
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Contents list	41
Inside front cover	38
Development of sulfonyl fluoride chemical probes to advance the discovery of cereblon modulators	37
In vivo demonstration of enhanced mRNA delivery by cyclic disulfide-containing lipid nanoparticles for facilitating endosomal escape	36
Exploration of hydrazine-based small molecules as metal chelators for KDM4 inhibition	33
Thiazole orange-carboplatin triplex-forming oligonucleotide (TFO) combination probes enhance targeted DNA crosslinking	31
4-Trifluoromethyl bithiazoles as broad-spectrum antimicrobial agents for virus-related bacterial infections or co-infections	29
Effect of mono-guanidine-like derivatives on platelet aggregation and tumour cell induced platelet aggregation	27
Biocompatible glycolipid derived from bhilawanol as an antibiofilm agent and a promising platform for drug delivery	27
Research progress of anticancer drugs targeting CDK12	27
Beta-cyclodextrin formulation of a disulfide-bond disrupting agent for improved systemic exposure	26
Integrating computational and experimental chemical biology revealed variable anticancer activities of phosphodiesterase isoenzyme 5 inhibitors (PDE5i) in lung cancer	26
Identification of the first structurally validated covalent ligands of the small GTPase RAB27A	26

ATP-competitive inhibitors for cancer treatment – kinases and the world beyond	24
Unveiling sultam in drug discovery: spotlight on the underexplored scaffold	24
Cytotoxicity of phosphoramidate, bis-amidate and cycloSal prodrug metabolites against tumour and normal cells	24
Design, synthesis, in vitro and in silico evaluation of indole-based tetrazole derivatives as putative anti-breast cancer agents	22
Unusual Ni⋯Ni interaction in Ni(ii) complexes as potential inhibitors for the development of new anti-SARS-CoV-2 Omicron drugs	22
Sirtuin 1-activating derivatives belonging to the anilinopyridine class displaying in vivo cardioprotective activities	21
Inside front cover	21
Natural product-inspired [3 + 2] cycloaddition-based spirooxindoles as dual anticancer agents: synthesis, characterization, and biological evaluation by in vitro and in silico methods	21
Contents list	21
Front cover	20
Tackling antimicrobial stewardship through synergy and antimicrobial peptides	20
Importance of photophosphatidylserine and Tim-3 in photoimmunotherapy	20
Simple accessible clemastine fumarate analogues as effective antileishmanials	20
Design, synthesis and biological evaluation of rhein–piperazine–furanone hybrids as potential anticancer agents	19
Design, quality and validation of the EU-OPENSCREEN fragment library poised to a high-throughput screening collection	19
Radiosynthesis of [18F]brequinar for in vivo PET imaging of hDHODH for potential studies of acute myeloid leukemia and cancers	19
Evolution of structure-guided drug design strategies targeting mutations in codon 12 of KRAS	19
Bioassay-guided isolation of hepatoprotective lignans from Vernonia cinerea: DeepSAT-driven structural elucidation and predictive mechanistic insights against drug-induced liver injury	19
Cornulacin: a new isoflavone fromCornulaca monacanthaand its isolation, structure elucidation and cytotoxicity through EGFR-mediated apoptosis	19
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	18
A ‘click’ chemistry approach to novel entinostat (MS-275) based class I histone deacetylase proteolysis targeting chimeras	18
Discovery of dibenzylbutane lignan LCA derivatives as potent anti-inflammatory agents	18
Diversely functionalized isoquinolines and their core-embedded heterocyclic frameworks: a privileged scaffold for medicinal chemistry	18
Exploration of cytotoxic potential and tubulin polymerization inhibition activity of cis-stilbene-1,2,3-triazole congeners	18
The relationship between cancer risk and cystic fibrosis: the role of CFTR in cell growth and cancer development	18
Back cover	18
Light-activatable photochemically targeting chimeras (PHOTACs) enable the optical control of targeted protein degradation of HDAC6	17
Recent advances from computer-aided drug design to artificial intelligence drug design	17
Structure-based design and evaluation of tyrosinase inhibitors targeting both human and mushroom isozymes	17
The physics-AI dialogue in drug design	17
Evolution of 3-(4-hydroxyphenyl)indoline-2-one as a scaffold for potent and selective anticancer activity	17
Design and development of sulfenylated 5-aminopyrazoles as inhibitors of acetylcholinesterase and butyrylcholinesterase: exploring the implication for Aβ1–42 aggregation inhibition in Alzhe	17
Prodrugs and their activation mechanisms for brain drug delivery	17
Trifluoroacetic acid-mediated synthesis of xanthene constructs and their extensive anti-tuberculosis evaluation	16
It's ok to be outnumbered – sub-stoichiometric modulation of homomeric protein complexes	16
A story of peptides, lipophilicity and chromatography – back and forth in time	16
Pretargeted imaging beyond the blood–brain barrier	16
Recent insights of PROTAC developments in inflammation-mediated and autoimmune targets: a critical review	16
Proximity-induced membrane protein degradation for cancer therapies	15
The allure of targets for novel drugs	15
Druggable targets for the immunopathy of Alzheimer's disease	15
Contents list	15
Hinokitiol potentiates antimicrobial activity of bismuth drugs: a combination therapy for overcoming antimicrobial resistance	15
Recent advancements in the development of next-generation dual-targeting antibacterial agents	14
On-resin synthesis of Lanreotide epimers and studies of their structure–activity relationships	14
Novel rhodanine–thiazole hybrids as potential antidiabetic agents: a structure-based drug design approach	14
Synthesis, biological evaluation and computational studies of pyrazole derivatives as Mycobacterium tuberculosis CYP121A1 inhibitors	14
Stachydrine, a pyrrole alkaloid with promising therapeutic potential against metabolic syndrome and associated organ dysfunction	13
Front cover	13
The importance of tyrosines in multimers of cyclic RGD nonapeptides: towards αvβ6-integrin targeted radiotherapeutics	13

Inhibition of transcription and antiproliferative effects in a cancer cell line using antigene oligonucleotides containing artificial nucleoside analogues	13
Correction: Design and synthesis of eugenol/isoeugenol glycoconjugates and other analogues as antifungal agents against Aspergillus fumigatus	13
Contents list	13
Minimising the payload solvent exposed hydrophobic surface area optimises the antibody-drug conjugate properties	13
Synthesis of novel rapanone derivatives via organocatalytic reductive C-alkylation: biological evaluation of antioxidant properties, in vivo zebrafish embryo toxicity, and docking studie	13
Front cover	13
Back cover	13
SETDB1 as a cancer target: challenges and perspectives in drug design	13
Stereochemical optimization of N,2-substituted cycloalkylamines as norepinephrine reuptake inhibitors	12
Development of Hsp90 C-terminal inhibitors with noviomimetics that manifest anti-proliferative activities	12
Insights into the modular design of kinase inhibitors and application to Abl and Axl	12
Design, synthesis and evaluation of 2-phenylpyrimidine derivatives as novel antifungal agents targeting CYP51	12
Discovery of a nasal spray steroid, tixocortol, as an inhibitor of SARS-CoV-2 main protease and viral replication	12
An allosteric inhibitor targeting the STAT3 coiled-coil domain selectively suppresses proliferation of breast cancer	12
Can large language models predict antimicrobial peptide activity and toxicity?	12
Pyridazinone-based derivatives as anticancer agents endowed with anti-microbial activity: molecular design, synthesis, and biological investigation	12
Scaffold hopping from indoles to indazoles yields dual MCL-1/BCL-2 inhibitors from MCL-1 selective leads	12
Rutaecarpine derivatives synthesized via skeletal reorganization alleviate inflammation-associated oxidative damage by inhibiting the MAPK/NF-κB signaling pathway	12
Design, synthesis and anti-proliferative activity of 3-aryl-evodiamine derivatives	11
NIR-II imaging of hepatocellular carcinoma based on a humanized anti-GPC3 antibody	11
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Exploration of piperidine 3D fragment chemical space: synthesis and 3D shape analysis of fragments derived from 20 regio- and diastereoisomers of methyl substituted pipecolinates	11
Enhanced inhibitory activity of compounds containing purine scaffolds compared to protein kinase CK2α considering crystalline water	11
Discovery of imidazo[1,2-b]pyridazine-containing TAK1 kinase inhibitors with excellent activities against multiple myeloma	11
Recent advancements in the therapeutic approaches for Alzheimer's disease treatment: current and future perspective	11
Back cover	11
Synthesis and biological evaluation of thiosemicarbazone-based antibody–drug conjugates	11
Geometric deep learning-guided Suzuki reaction conditions assessment for applications in medicinal chemistry	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
Inside front cover	11
Mycobacterium tuberculosis CitA activity is modulated by cysteine oxidation and pyruvate binding	10
Identification of novel phenylalanine derivatives bearing a hydroxamic acid moiety as potent quorum sensing inhibitors	10
Development of di-arylated 1,2,4-triazole-based derivatives as therapeutic agents against breast cancer: synthesis and biological evaluation	10
Site-specific molecular glues for the 14-3-3/Tau pS214 protein–protein interaction via reversible covalent imine tethering	10
Inside front cover	10
Quinazolinone-1,2,3-triazole-acetamide conjugates as potent α-glucosidase inhibitors: synthesis, enzyme inhibition, kinetic analysis, and molecular docking study	10
Progress in the discovery and development of small molecule methuosis inducers	10
Design and evaluation of poly-nitrogenous adjuvants capable of potentiating antibiotics in Gram-negative bacteria	10
Anticancer potential of copper(i) complexes based on isopropyl ester derivatives of bis(pyrazol-1-yl)acetate ligands	10
Evaluation of ketoclomazone and its analogues as inhibitors of 1-deoxy-d-xylulose 5-phosphate synthases and other thiamine diphosphate (ThDP)-dependent enzymes	10
Technical, preclinical, and clinical developments of Fc-glycan-specific antibody–drug conjugates	9
Research progress of metal–organic framework nanozymes in bacterial sensing, detection, and treatment	9
Design, synthesis, and biological evaluation of novel thiazole derivatives as PI3K/mTOR dual inhibitors	9
Discovery of 2,3-dihydro-1H-pyrrolo[3,4-b]quinolin-1-one derivatives as possible antileishmanial agents	9
Design and synthesis of novel cathepsin C inhibitors with anti-inflammatory activity	9
Thiazolidine-2,4-dione hybrids as dual alpha-amylase and alpha-glucosidase inhibitors: design, synthesis, in vitro and in vivo anti-diabetic evaluation	9
Five years of research on 2,4-thiazolidinediones as anticancer agents: medicinal chemistry insights (2020–2024)	9
Adjuvant strategies to tackle mcr-mediated polymyxin resistance	9
“Seasoning” antimalarial drugs' action: chloroquine bile salts as novel triple-stage antiplasmodial hits	9
Target 2035 – update on the quest for a probe for every protein	9
Semisynthetic blasticidin S ester derivatives show enhanced antibiotic activity	9
Development of thiazole-appended novel hydrazones as a new class of α-amylase inhibitors with anticancer assets: anin silicoandin vitroapproach	9
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Discovery of a potent and selective PROTAC degrader for STAT3	9
Novel tetrahydropyrimidinyl-substituted benzimidazoles and benzothiazoles: synthesis, antibacterial activity, DNA interactions and ADME profiling	9
SLL-1A-16 suppresses proliferation and induces autophagy in non-small-cell lung cancer cells via the AKT/mTOR signaling pathway	9
Inside front cover	9
Distinctive roles of aquaporins and novel therapeutic opportunities against cancer	9
Rational design and in vitro testing of new urease inhibitors to prevent urinary catheter blockage	9
EGFRAP: a predictive machine learning model for assessing small molecule activity against the epidermal growth factor receptor	8
Synthesis and Investigation of Thieno[2,3-b]pyridines that Restore Activity of Topotecan	8
Back cover	8
Outstanding Reviewers for RSC Medicinal Chemistry in 2024	8
Identification of SARS-CoV-2 Mpro inhibitors through deep reinforcement learning for de novo drug design and computational chemistry approaches	8
The synthesis and bioactivities of ROCK2 inhibitors with 1,2-dithiolan-3-yl motif	8
Recent developments in membrane targeting antifungal agents to mitigate antifungal resistance	8
Fragment-based discovery of dual ligand pharmacophores for lipid-sensing transcription factors for designed polypharmacology	8
Molecular understanding of the therapeutic potential of melanin inhibiting natural products	8
Ribosome-targeting antibiotics and resistance via ribosomal RNA methylation	8
Lysine targeting covalent inhibitors of malarial kinase PfCLK3	8
AlbiCDN: albumin-binding amphiphilic STING agonists augment the immune activity for cancer immunotherapy	8
Insights into the recent progress in the medicinal chemistry of pyranopyrimidine analogs	8
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	8
Inhibition of DXR in the MEP pathway with lipophilic N-alkoxyaryl FR900098 analogs	8
Design and synthesis of cyclic lipidated peptides derived from the C-terminus of Cx43 for hemichannel inhibition and cardiac endothelium targeting	8
Cyclometalated Complexes: Promising Metallodrugs in the Battle Against Cancer.	8
Synthesis and Antiplasmodial Activity of 6H,13H-Pyrazino[1,2-a;4,5-a′]diindole Analogues Substituted with Basic Side Chains	8
Integrating a quinone substructure into histone deacetylase inhibitors to cope with Alzheimer's disease and cancer	8
Stereoselective synthesis and antiproliferative activity of allo-gibberic acid-based 1,3-aminoalcohol regioisomers	7
Development of trisubstituted thiophene-3-arboxamide selenide derivatives as novel EGFR kinase inhibitors with cytotoxic activity	7

Correction: Minimising the payload solvent exposed hydrophobic surface area optimises the antibody–drug conjugate properties	7
Synthesis of full-length homodimer αD-VxXXB that targets human α7 nicotinic acetylcholine receptors	7
The Mycobacterium tuberculosis mycothiol S-transferase is divalent metal-dependent for mycothiol binding and transfer	7
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Complexity of αvβ6-integrin targeting RGD peptide trimers: emergence of non-specific binding by synergistic interaction	7
Inhibition of bacterial RNA polymerase function and protein–protein interactions: a promising approach for next-generation antibacterial therapeutics	7
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Novel pirfenidone derivatives: synthesis and biological evaluation	7
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Guggulsterone – a potent bioactive phytosteroid: synthesis, structural modification, and its improved bioactivities	7
Introduction to the themed collection in honour of Professor Christian Leumann	7
Applications of supramolecular assemblies in drug delivery and photodynamic therapy	7
QSAR, structure-based pharmacophore modelling and biological evaluation of novel platelet ADP receptor (P2Y12) antagonist	7
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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 light-driven on–off multitarget AChE and MAO-B inhibitors	6
Mannich reaction mediated derivatization of chromones and their biological evaluations as putative multipotent ligands for the treatment of Alzheimer's disease	6
Contents list	6
Front cover	6
Development of pharmacophore models for AcrB protein and the identification of potential adjuvant candidates for overcoming efflux-mediated colistin resistance	6
Synthesis and evaluation of tetrahydropyrrolo[1,2-a]quinolin-1(2H)-ones as new tubulin polymerization inhibitors	6
Design, synthesis, and evaluation of benzhydrylpiperazine-based novel dual COX-2/5-LOX inhibitors with anti-inflammatory and anti-cancer activity	6
Introduction to the themed collection on ‘Targeting RNA with small molecules’	6
Macrocyclic RGD-peptides with high selectivity for αvβ3 integrin in cancer imaging and therapy	6
Front cover	6
Expanding the chemical space for antiviral discovery: the potential of twistenediones	6
Design, synthesis and biological evaluation of novel β-caryophyllene derivatives as potential anti-cancer agents through the ROS-mediated apoptosis pathway	6
Copper selective 8-aminoquinoline based tetradentate chelators as anticancer agents	6
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
Front cover	6
Modulating polybasic character of galactose-based glycosylated antitumor ether lipids for enhanced cytotoxic response	6
Novel benzimidazole hybrids: design, synthesis, mechanistic studies, antifungal potential and molecular dynamics	6
Structure-guided design of a methyltransferase-like 3 (METTL3) proteolysis targeting chimera (PROTAC) incorporating an indole–nicotinamide chemotype	6
Expanding the structure–activity relationships of alkynyl diphenylurea scaffold as promising antibacterial agents	6
Front cover	6
Design, synthesis, and biological evaluation of new arjunolic acid derivatives as anticancer agents	6
Computer-aided discovery of triazolothiadiazoles as DYRK1A-targeted neuroprotective agents	6
Discovery of first-in-class PROTACs targeting maternal embryonic leucine zipper kinase (MELK) for the treatment of Burkitt lymphoma	6
Preventing SARS-CoV-2 infection using Fv-antibodies targeting the proprotein convertase (PPC) cleavage site	6
Contents list	6
Semisynthetic polymyxins with potent antibacterial activity and reduced kidney cell toxicity	6
Design, synthesis, antimicrobial activity, stability, and mechanism of action of bioresorbable ceragenins	6
Enhanced skin penetration of curcumin by a nanoemulsion-embedded oligopeptide hydrogel for psoriasis topical therapy	6
Development, biological evaluation, and molecular modelling of novel isocytosine and guanidine derivatives as BACE1 inhibitors using a fragment growing strategy	6
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism	6
Discovery of selective, metabolically stable pyrazole-based FLT3 inhibitors for the treatment of acute myeloid leukemia	6
Design, synthesis, molecular docking and anti-proliferative activity of novel phenothiazine containing imidazo[1,2-a]pyridine derivatives against MARK4 protein	6
Polysucrose hydrogel loaded with natural molecules/extracts for multiphase-directed sustainable wound healing	6
Design of Chitosan-Coated CeO₂-Doped ZnCr LDO Nanocomposites for Optimized Azithromycin Delivery: A Kinetic and Mechanistic Perspective	6
Contents list	6
A perspective on small molecules targeting the renin–angiotensin–aldosterone system and their utility in cardiovascular diseases: exploring the structural insights for rational drug discovery and deve	5
Front cover	5
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Discovery of benzoheterocyclic-substituted amide derivatives as apoptosis signal-regulating kinase 1 (ASK1) inhibitors	5
Antitubercular evaluation of dihydropyridine–triazole conjugates: design, synthesis, in vitro screening, SAR and in silico ADME predictions	5
Heterocyclic compounds as xanthine oxidase inhibitors for the management of hyperuricemia: synthetic strategies, structure–activity relationship and molecular docking studies (2018–2024)	5
An overview of the development of EED inhibitors to disable the PRC2 function	5
Synthesis and properties of the kojic acid dimer and its potential for the treatment of Alzheimer's disease	5
Expanding the scope of novel 1,2,3-triazole derivatives as new antiparasitic drug candidates	5
Discovery and computational studies of piperidine/piperazine-based compounds endowed with sigma receptor affinity	5
Overview of CFTR activators and their recent studies for dry eye disease: a review	5
Near-infrared photochemical internalization: design of a distorted zinc phthalocyanine for efficient intracellular delivery of immunotoxins	5
Discovery of pyrazolopyrimidines that selectively inhibit CSF-1R kinase by iterative design, synthesis and screening against glioblastoma cells	5
Inhibition of monoamine oxidases by heterocyclic derived conjugated dienones: synthesis and in vitro and in silico investigations	5
Prediction of synergistic gemcitabine-based combination treatment through a novel tumor stemness biomarker NANOG in pancreatic cancer	5
Chemical genetic approaches for the discovery of bacterial cell wall inhibitors	5
Back cover	5
NLRP3 inflammasome: structure, mechanism, drug-induced organ toxicity, therapeutic strategies, and future perspectives	5
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Novel benzimidazole-based pseudo-irreversible butyrylcholinesterase inhibitors with neuroprotective activity in an Alzheimer's disease mouse model	5
Ruthenium(ii)–arene complexes as anti-metastatic agents, and related techniques	5
The era of high-quality chemical probes	5
Design, synthesis, and SAR of antiproliferative activity of trioxatriangulene derivatives	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
Targeting host integrated stress response: lead discovery of flavonoid compounds active against coronaviruses PEDV and PDCoV	5
Design, synthesis and in vitro evaluations of new cyclotriphosphazenes as safe drug candidates	5
Back cover	5
Chromenochalcones: a comprehensive review on developments towards a medicinal perspective	5
In vitro biological evaluation and in silico studies of linear diarylheptanoids from Curcuma aromatica Salisb. as urease inhibitors	5
Armeniaspirol analogues with more potent Gram-positive antibiotic activity show enhanced inhibition of the ATP-dependent proteases ClpXP and ClpYQ	5
Design, synthesis, and biological evaluation of new thalidomide–donepezil hybrids as neuroprotective agents targeting cholinesterases and neuroinflammation	5
Coumarin–furo[2,3-d]pyrimidone hybrid molecules targeting human liver cancer cells: synthesis, anticancer effect, EGFR inhibition and molecular docking studies	5
From traditional medicine to nanomedicine: potential of Ginkgo biloba extracts in treating inflammatory skin diseases	5
Advances in the development of Wnt/β-catenin signaling inhibitors	5
In vitro evaluation of the immunogenic potential of gramicidin S and its photocontrolled analogues	5
Novel curcumin-based analogues as potential VEGFR2 inhibitors with promising metallic loading nanoparticles: synthesis, biological evaluation, and molecular modelling investigation	5
Benzenesulfonamide decorated dihydropyrimidin(thi)ones: carbonic anhydrase profiling and antiproliferative activity	5
Discovery and optimisation of pyrazolo[1,5-a]pyrimidines as aryl hydrocarbon receptor antagonists	5
Designed hybrid anticancer nuclear-localized peptide inhibits aggressive cancer cell proliferation	5
Synthetic 18F labeled biomolecules that are selective and promising for PET imaging: major advances and applications	5
Back cover	5
The development of a PET radiotracer for imaging alpha synuclein aggregates in Parkinson's disease	5
Photoswitchable Stat3 inhibitors: design, synthesis and anticancer activity study on 2D and 3D breast cancer cell cultures	5
Synthesis and bioactivity of psilocybin analogues containing a stable carbon–phosphorus bond	5