RSC Medicinal Chemistry

Article	Citations
Recent advances of phenotypic screening strategies in the application of anti-influenza virus drug discovery	145
Expanding the chemical space of ester of quinoxaline-7-carboxylate 1,4-di-N-oxide derivatives as potential antitubercular agents	101
Back cover	80
Back cover	75
Inside front cover	72
Designing halogen-free metal–phenolic imidazolium poly(ionic liquids) with multi-functional antibacterial, anti-inflammatory and cell proliferation properties for infected wounds	69
Metabolic labelling of cancer cells with glycodendrimers stimulate immune-mediated cytotoxicity	65
Contents list	65
Back cover	65
4-Trifluoromethyl bithiazoles as broad-spectrum antimicrobial agents for virus-related bacterial infections or co-infections	62
ATP-competitive inhibitors for cancer treatment – kinases and the world beyond	60
Exploration of hydrazine-based small molecules as metal chelators for KDM4 inhibition	58
Research progress of anticancer drugs targeting CDK12	53
Development of sulfonyl fluoride chemical probes to advance the discovery of cereblon modulators	52
Beta-cyclodextrin formulation of a disulfide-bond disrupting agent for improved systemic exposure	45
Cytotoxicity of phosphoramidate, bis-amidate and cycloSal prodrug metabolites against tumour and normal cells	43
In vivo demonstration of enhanced mRNA delivery by cyclic disulfide-containing lipid nanoparticles for facilitating endosomal escape	41
Effect of mono-guanidine-like derivatives on platelet aggregation and tumour cell induced platelet aggregation	40
N-Arylsulfonamide-based adenosine analogues to target RNA cap N7-methyltransferase nsp14 of SARS-CoV-2	40
Biocompatible glycolipid derived from bhilawanol as an antibiofilm agent and a promising platform for drug delivery	40
Emerging opportunities in the rewiring of biology through proximity inducing small molecules	36
Oxadiargyl analogs as potent inhibitors of Toxoplasma gondii protoporphyrinogen oxidase	34
Design, synthesis and structure–activity relationship analysis of dibenzodiazepinone derivatives against Osimertinib resistant NSCLC	34
Integrating computational and experimental chemical biology revealed variable anticancer activities of phosphodiesterase isoenzyme 5 inhibitors (PDE5i) in lung cancer	33
Structure–activity relationship study of PROTACs against hematopoietic prostaglandin D2 synthase	32

Exploring the potential of tamoxifen-based copper(ii) dichloride in breast cancer therapy	31
Unveiling sultam in drug discovery: spotlight on the underexplored scaffold	30
Thiazole orange-carboplatin triplex-forming oligonucleotide (TFO) combination probes enhance targeted DNA crosslinking	29
Design, synthesis, in vitro and in silico evaluation of indole-based tetrazole derivatives as putative anti-breast cancer agents	28
Unusual Ni⋯Ni interaction in Ni(ii) complexes as potential inhibitors for the development of new anti-SARS-CoV-2 Omicron drugs	28
Covalent cannabinoid receptor ligands – structural insight and selectivity challenges	28
Identification of the first structurally validated covalent ligands of the small GTPase RAB27A	28
Synthesis and biological evaluation of novel D-ring fused steroidal N(2)-substituted-1,2,3-triazoles	27
New azole derivatives linked to indole/indoline moieties combined with FLC against drug-resistant Candida albicans	26
Contents list	24
Back cover	24
Front cover	24
Inside front cover	24
Trifluoroacetic acid-mediated synthesis of xanthene constructs and their extensive anti-tuberculosis evaluation	24
Discovery of dibenzylbutane lignan LCA derivatives as potent anti-inflammatory agents	23
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	22
Evolution of structure-guided drug design strategies targeting mutations in codon 12 of KRAS	22
It's ok to be outnumbered – sub-stoichiometric modulation of homomeric protein complexes	22
Exploration of cytotoxic potential and tubulin polymerization inhibition activity of cis-stilbene-1,2,3-triazole congeners	22
Tackling antimicrobial stewardship through synergy and antimicrobial peptides	22
Light-activatable photochemically targeting chimeras (PHOTACs) enable the optical control of targeted protein degradation of HDAC6	21
Radiosynthesis of [ 18 F]brequinar for in vivo PET imaging of hDHODH for potential studies of acute my	21
Evolution of 3-(4-hydroxyphenyl)indoline-2-one as a scaffold for potent and selective anticancer activity	21
Simple accessible clemastine fumarate analogues as effective antileishmanials	21
Sirtuin 1-activating derivatives belonging to the anilinopyridine class displaying in vivo cardioprotective activities	21
Cornulacin: a new isoflavone from Cornulaca monacantha and its isolation, structure elucidation and cytotoxicity through EGFR-mediated apoptosis	20
Structure-based design and evaluation of tyrosinase inhibitors targeting both human and mushroom isozymes	20
Structure–activity relationships of fenarimol analogues with potent in vitro and in vivo activity against	20
Water-soluble cationic porphyrins with enhanced phototoxicity to cancer cell lines for G4-targeting photodynamic therapy	20
Design and development of sulfenylated 5-aminopyrazoles as inhibitors of acetylcholinesterase and butyrylcholinesterase: exploring the implication for Aβ 1–42	20
Diversely functionalized isoquinolines and their core-embedded heterocyclic frameworks: a privileged scaffold for medicinal chemistry	20
Prodrugs and their activation mechanisms for brain drug delivery	19
Recent advances from computer-aided drug design to artificial intelligence drug design	19
The physics-AI dialogue in drug design	19
Design, synthesis and biological evaluation of rhein–piperazine–furanone hybrids as potential anticancer agents	19
Bioassay-guided isolation of hepatoprotective lignans from Vernonia cinerea: DeepSAT-driven structural elucidation and predictive mechanistic insights against drug-induced liver injury	18
The relationship between cancer risk and cystic fibrosis: the role of CFTR in cell growth and cancer development	18
A story of peptides, lipophilicity and chromatography – back and forth in time	18
Recent insights of PROTAC developments in inflammation-mediated and autoimmune targets: a critical review	18
Importance of photophosphatidylserine and Tim-3 in photoimmunotherapy	17
Pretargeted imaging beyond the blood–brain barrier	17
Design, quality and validation of the EU-OPENSCREEN fragment library poised to a high-throughput screening collection	17
Natural product-inspired [3 + 2] cycloaddition-based spirooxindoles as dual anticancer agents: synthesis, characterization, and biological evaluation by in vitro and in silico methods	17
A ‘click’ chemistry approach to novel entinostat (MS-275) based class I histone deacetylase proteolysis targeting chimeras	17
Contents list	17
Discovery of imidazo[1,2-b]pyridazine-containing TAK1 kinase inhibitors with excellent activities against multiple myeloma	16
Correction: Design and synthesis of eugenol/isoeugenol glycoconjugates and other analogues as antifungal agents against Aspergillus fumigatus	16
On-resin synthesis of Lanreotide epimers and studies of their structure–activity relationships	16
Hinokitiol potentiates antimicrobial activity of bismuth drugs: a combination therapy for overcoming antimicrobial resistance	16
Front cover	16

Enhanced inhibitory activity of compounds containing purine scaffolds compared to protein kinase CK2α considering crystalline water	16
Front cover	16
Inhibition of transcription and antiproliferative effects in a cancer cell line using antigene oligonucleotides containing artificial nucleoside analogues	15
Design, synthesis and evaluation of 2-phenylpyrimidine derivatives as novel antifungal agents targeting CYP51	15
NIR-II imaging of hepatocellular carcinoma based on a humanized anti-GPC3 antibody	15
The importance of tyrosines in multimers of cyclic RGD nonapeptides: towards αvβ6-integrin targeted radiotherapeutics	15
Synthesis of novel rapanone derivatives via organocatalytic reductive C-alkylation: biological evaluation of antioxidant properties, in vivo zebrafish embryo toxicity, and docking studie	15
Recent advancements in the development of next-generation dual-targeting antibacterial agents	15
Development of Hsp90 C-terminal inhibitors with noviomimetics that manifest anti-proliferative activities	15
Back cover	15
Contents list	15
Rutaecarpine derivatives synthesized via skeletal reorganization alleviate inflammation-associated oxidative damage by inhibiting the MAPK/NF-κB signaling pathway	15
SETDB1 as a cancer target: challenges and perspectives in drug design	15
An allosteric inhibitor targeting the STAT3 coiled-coil domain selectively suppresses proliferation of breast cancer	15
Synthesis, biological evaluation and computational studies of pyrazole derivatives as Mycobacterium tuberculosis CYP121A1 inhibitors	14
Discovery of a nasal spray steroid, tixocortol, as an inhibitor of SARS-CoV-2 main protease and viral replication	14
The structural requirements of 3,5-substituted oxindoles that determine selective AMPK or GSK3β inhibition.	14
Can large language models predict antimicrobial peptide activity and toxicity?	14
Synthesis and biological evaluation of thiosemicarbazone-based antibody–drug conjugates	14
Geometric deep learning-guided Suzuki reaction conditions assessment for applications in medicinal chemistry	14
Stachydrine, a pyrrole alkaloid with promising therapeutic potential against metabolic syndrome and associated organ dysfunction	14
Stereochemical optimization of N ,2-substituted cycloalkylamines as norepinephrine reuptake inhibitors	14
Minimising the payload solvent exposed hydrophobic surface area optimises the antibody-drug conjugate properties	14
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	14
From fragments to follow-ups: rapid hit expansion by making use of EU-OPENSCREEN resources	14
Design, synthesis and anti-proliferative activity of 3-aryl-evodiamine derivatives	14
Druggable targets for the immunopathy of Alzheimer's disease	14
Exploration of piperidine 3D fragment chemical space: synthesis and 3D shape analysis of fragments derived from 20 regio- and diastereoisomers of methyl substituted pipecolinates	13
Proximity-induced membrane protein degradation for cancer therapies	13
Glioblastoma antitumoral activity of tetrahydroquinoline-derived triarylmethanes	13
Back cover	13
Synthesis and evaluation of HFIP bearing triazolo-amides as amyloid-β aggregation inhibitors and suppressors of aggregation induced neuroinflammation	13
Insights into the modular design of kinase inhibitors and application to Abl and Axl	13
The allure of targets for novel drugs	13
Inside front cover	13
Inside front cover	13
Design and evaluation of poly-nitrogenous adjuvants capable of potentiating antibiotics in Gram-negative bacteria	13
Scaffold hopping from indoles to indazoles yields dual MCL-1/BCL-2 inhibitors from MCL-1 selective leads	13
Pyridazinone-based derivatives as anticancer agents endowed with anti-microbial activity: molecular design, synthesis, and biological investigation	13
Novel rhodanine–thiazole hybrids as potential antidiabetic agents: a structure-based drug design approach	13
Contents list	13
“Seasoning” antimalarial drugs' action: chloroquine bile salts as novel triple-stage antiplasmodial hits	13
Recent advancements in the therapeutic approaches for Alzheimer's disease treatment: current and future perspective	13
Discovery of a potent and selective PROTAC degrader for STAT3	12
Quinazolinone-1,2,3-triazole-acetamide conjugates as potent α-glucosidase inhibitors: synthesis, enzyme inhibition, kinetic analysis, and molecular docking study	12
Anticancer potential of copper(i) complexes based on isopropyl ester derivatives of bis(pyrazol-1-yl)acetate ligands	12
Site-specific molecular glues for the 14-3-3/Tau pS214 protein–protein interaction via reversible covalent imine tethering	12
Contents list	12
Mycobacterium tuberculosis CitA activity is modulated by cysteine oxidation and pyruvate binding	12
Development of a nitric oxide-releasing cephalexin-based hybrid compound for enhanced antimicrobial efficacy and biofilm disruption	12
Novel tetrahydropyrimidinyl-substituted benzimidazoles and benzothiazoles: synthesis, antibacterial activity, DNA interactions and ADME profiling	12
Identification of novel phenylalanine derivatives bearing a hydroxamic acid moiety as potent quorum sensing inhibitors	12
Development of di-arylated 1,2,4-triazole-based derivatives as therapeutic agents against breast cancer: synthesis and biological evaluation	12
Target 2035 – update on the quest for a probe for every protein	12
Progress in the discovery and development of small molecule methuosis inducers	11
Evaluation of ketoclomazone and its analogues as inhibitors of 1-deoxy-d-xylulose 5-phosphate synthases and other thiamine diphosphate (ThDP)-dependent enzymes	11
Technical, preclinical, and clinical developments of Fc-glycan-specific antibody–drug conjugates	11
Integrating a quinone substructure into histone deacetylase inhibitors to cope with Alzheimer's disease and cancer	11
Distinctive roles of aquaporins and novel therapeutic opportunities against cancer	11
Research progress of metal–organic framework nanozymes in bacterial sensing, detection, and treatment	11
Adjuvant strategies to tackle mcr -mediated polymyxin resistance	11
Design, synthesis, and biological evaluation of novel thiazole derivatives as PI3K/mTOR dual inhibitors	11
Semisynthetic blasticidin S ester derivatives show enhanced antibiotic activity	11
Discovery of 2,3-dihydro-1H-pyrrolo[3,4-b]quinolin-1-one derivatives as possible antileishmanial agents	11
Five years of research on 2,4-thiazolidinediones as anticancer agents: medicinal chemistry insights (2020–2024)	11
SLL-1A-16 suppresses proliferation and induces autophagy in non-small-cell lung cancer cells via the AKT/mTOR signaling pathway	11
Contents list	11
Inside front cover	11
Synthesis and investigation of thieno[2,3-b]pyridines that restore activity of topotecan	10
Discovery and Optimization of Pyrrolopyrimidines as Highly Potent, Selective and Brain-Penetrant LRRK2 Inhibitors	10
Thiazolidine-2,4-dione hybrids as dual alpha-amylase and alpha-glucosidase inhibitors: design, synthesis, in vitro and in vivo anti-diabetic evaluation	10
Design and synthesis of cyclic lipidated peptides derived from the C-terminus of Cx43 for hemichannel inhibition and cardiac endothelium targeting	10
Fragment-based discovery of dual ligand pharmacophores for lipid-sensing transcription factors for designed polypharmacology	10
EGFR AP : a predictive machine learning model for assessing small molecule activity against the epidermal growth factor receptor	10
Development of trisubstituted thiophene-3-arboxamide selenide derivatives as novel EGFR kinase inhibitors with cytotoxic activity	10
Outstanding Reviewers for RSC Medicinal Chemistry in 2024	10
Back cover	10
Complexity of αvβ6-integrin targeting RGD peptide trimers: emergence of non-specific binding by synergistic interaction	10
Novel lithocholic acid-diindolylmethane hybrids as potent sialyltransferase inhibitors targeting triple-negative breast cancer: a molecular hybridization approach	10
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	10

Lysine targeting covalent inhibitors of malarial kinase PfCLK3	10
The synthesis and bioactivities of ROCK2 inhibitors with 1,2-dithiolan-3-yl motif	10
Diversifying the Triquinazine Scaffold of a Janus Kinase Inhibitor	10
AlbiCDN: albumin-binding amphiphilic STING agonists augment the immune activity for cancer immunotherapy	10
Design and synthesis of novel cathepsin C inhibitors with anti-inflammatory activity	10
Development of thiazole-appended novel hydrazones as a new class of α-amylase inhibitors with anticancer assets: anin silicoandin vitroapproach	10
Molecular understanding of the therapeutic potential of melanin inhibiting natural products	10
Recent developments in membrane targeting antifungal agents to mitigate antifungal resistance	9
Synthesis and antiplasmodial activity of 6H,13H-pyrazino[1,2-a;4,5-a′]diindole analogues substituted with basic side chains	9
QSAR, structure-based pharmacophore modelling and biological evaluation of novel platelet ADP receptor (P2Y12) antagonist	9
Insights into the recent progress in the medicinal chemistry of pyranopyrimidine analogs	9
Contents list	9
Correction: Minimising the payload solvent exposed hydrophobic surface area optimises the antibody–drug conjugate properties	9
Rational design and in vitro testing of new urease inhibitors to prevent urinary catheter blockage	9
Guggulsterone – a potent bioactive phytosteroid: synthesis, structural modification, and its improved bioactivities	9
Back cover	9
Synthesis of full-length homodimer αD-VxXXB that targets human α7 nicotinic acetylcholine receptors	9
Inhibition of DXR in the MEP pathway with lipophilic N-alkoxyaryl FR900098 analogs	9
Front cover	9
Cyclometalated complexes: promising metallodrugs in the battle against cancer	9
Introduction to the themed collection in honour of Professor Christian Leumann	9
Back cover	9
Identification of SARS-CoV-2 Mpro inhibitors through deep reinforcement learning for de novo drug design and computational chemistry approaches	9
Contents list	9
Ribosome-targeting antibiotics and resistance via ribosomal RNA methylation	9
Contents list	9
Novel pirfenidone derivatives: synthesis and biological evaluation	8
Stereoselective synthesis and antiproliferative activity of allo-gibberic acid-based 1,3-aminoalcohol regioisomers	8
Expanding the chemical space for antiviral discovery: the potential of twistenediones	8
Front cover	8
Design, synthesis, and biological evaluation of new arjunolic acid derivatives as anticancer agents	8
Design, synthesis, and biological evaluation of sulfonamide-functionalized pyridine carbothioamides as potent tubulin-targeting anticancer agents	8
Live cell screening to identify RNA-binding small molecule inhibitors of the pre-let-7–Lin28 RNA–protein interaction	8
Design, synthesis and biological evaluation of novel β-caryophyllene derivatives as potential anti-cancer agents through the ROS-mediated apoptosis pathway	8
Recent advances in structural modifications of natural products for anti-leishmaniasis therapy (2010–2024)	8
Macrocyclic RGD-peptides with high selectivity for αvβ3 integrin in cancer imaging and therapy	8
Applications of supramolecular assemblies in drug delivery and photodynamic therapy	8
Polysucrose hydrogel loaded with natural molecules/extracts for multiphase-directed sustainable wound healing	8
The rise of ultrashort cationic β-peptides as promising antimicrobial therapeutics	8
Analysis of the structural diversity of heterocycles amongst European medicines agency approved pharmaceuticals (2014–2023)	8
Design, synthesis, antimicrobial activity, stability, and mechanism of action of bioresorbable ceragenins	8
Design, synthesis and biological evaluation of light-driven on–off multitarget AChE and MAO-B inhibitors	8
Copper selective 8-aminoquinoline based tetradentate chelators as anticancer agents	8
Preventing SARS-CoV-2 infection using Fv-antibodies targeting the proprotein convertase (PPC) cleavage site	8
Computer-aided discovery of triazolothiadiazoles as DYRK1A-targeted neuroprotective agents	8
Contents list	8
The Mycobacterium tuberculosis mycothiol S-transferase is divalent metal-dependent for mycothiol binding and transfer	8
Introduction to the themed collection on ‘Targeting RNA with small molecules’	8
Inhibition of bacterial RNA polymerase function and protein–protein interactions: a promising approach for next-generation antibacterial therapeutics	8
Front cover	8
Design, synthesis, molecular docking and anti-proliferative activity of novel phenothiazine containing imidazo[1,2-a]pyridine derivatives against MARK4 protein	8
Design of chitosan-coated CeO 2 -doped ZnCr LDO nanocomposites for optimized azithromycin delivery: a kinetic and mechanistic perspective	8
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism	7
Heterocyclic compounds as xanthine oxidase inhibitors for the management of hyperuricemia: synthetic strategies, structure–activity relationship and molecular docking studies (2018–2024)	7
Front cover	7
Front cover	7
Discovery of novel dehydroabietylamine–pyrimidine hybrids: design, synthesis and anti-tumor evaluation	7
Back cover	7
Front cover	7
Synthesis and evaluation of tetrahydropyrrolo[1,2-a]quinolin-1(2H)-ones as new tubulin polymerization inhibitors	7
Expanding the structure–activity relationships of alkynyl diphenylurea scaffold as promising antibacterial agents	7
Identification of spirodioxolane nsP2 helicase inhibitors with antialphaviral activity	7
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	7
Mannich reaction mediated derivatization of chromones and their biological evaluations as putative multipotent ligands for the treatment of Alzheimer's disease	7
Semisynthetic polymyxins with potent antibacterial activity and reduced kidney cell toxicity	7
Modulating polybasic character of galactose-based glycosylated antitumor ether lipids for enhanced cytotoxic response	7
Design, synthesis, and evaluation of benzhydrylpiperazine-based novel dual COX-2/5-LOX inhibitors with anti-inflammatory and anti-cancer activity	7
Development of pharmacophore models for AcrB protein and the identification of potential adjuvant candidates for overcoming efflux-mediated colistin resistance	7
Contents list	7
Design, synthesis, inhibitory activity, and molecular simulations study for d-glucose-conjugated thioureas containing pyrimidine ring as multitarget inhibitors against α-amylase, α-glucosid	7
Novel benzimidazole-based pseudo-irreversible butyrylcholinesterase inhibitors with neuroprotective activity in an Alzheimer's disease mouse model	7
Design and synthesis of novel 8-(azaindolyl)-benzoazepinones as potent and selective ROCK inhibitors	7
Back cover	7
Design, synthesis and in vitro evaluations of new cyclotriphosphazenes as safe drug candidates	7
Tanshinones target drug-resistant tuberculosis: efficacy, selectivity, and potential mechanism of action	7
NLRP3 inflammasome: structure, mechanism, drug-induced organ toxicity, therapeutic strategies, and future perspectives	7
Synthesis and properties of the kojic acid dimer and its potential for the treatment of Alzheimer's disease	7
The era of high-quality chemical probes	7
Discovery of first-in-class PROTACs targeting maternal embryonic leucine zipper kinase (MELK) for the treatment of Burkitt lymphoma	7
Enhanced skin penetration of curcumin by a nanoemulsion-embedded oligopeptide hydrogel for psoriasis topical therapy	7
Discovery and computational studies of piperidine/piperazine-based compounds endowed with sigma receptor affinity	7
Novel benzimidazole hybrids: design, synthesis, mechanistic studies, antifungal potential and molecular dynamics	7
Discovery of selective, metabolically stable pyrazole-based FLT3 inhibitors for the treatment of acute myeloid leukemia	7
Benzenesulfonamide decorated dihydropyrimidin(thi)ones: carbonic anhydrase profiling and antiproliferative activity	7
News from RSC Medicinal Chemistry	7
Phenylthiazoles with potent & optimum selectivity toward Clostridium difficile	7
Discovery of benzoheterocyclic-substituted amide derivatives as apoptosis signal-regulating kinase 1 (ASK1) inhibitors	7
Novel flexible biphenyl PfDHFR inhibitors with improved antimalarial activity	7
Structure-guided design of a methyltransferase-like 3 (METTL3) proteolysis targeting chimera (PROTAC) incorporating an indole–nicotinamide chemotype	7
Machine learning prediction of acute toxicity with in vivo experiments on tetrazole derivatives	7
In vitro evaluation of the immunogenic potential of gramicidin S and its photocontrolled analogues	7
Development, biological evaluation, and molecular modelling of novel isocytosine and guanidine derivatives as BACE1 inhibitors using a fragment growing strategy	7
In vitro biological evaluation and in silico studies of linear diarylheptanoids from Curcuma aromatica Salisb. as urease inhibitors	6
Design and synthesis of isoxazole-functionalized benzene sulphonamides as novel inhibitors of Mycobacterium tuberculosis β-carbonic anhydrases	6
Inhibition of monoamine oxidases by heterocyclic derived conjugated dienones: synthesis and in vitro and in silico investigations	6