RSC Medicinal Chemistry

Article	Citations
Covalent cannabinoid receptor ligands – structural insight and selectivity challenges	126
Synthesis and biological evaluation of novel D-ring fused steroidal N(2)-substituted-1,2,3-triazoles	94
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	62
Back cover	61
Metabolic labelling of cancer cells with glycodendrimers stimulate immune-mediated cytotoxicity	61
New azole derivatives linked to indole/indoline moieties combined with FLC against drug-resistant Candida albicans	61
Inside front cover	59
Back cover	59
ATP-competitive inhibitors for cancer treatment – kinases and the world beyond	55
In vivo demonstration of enhanced mRNA delivery by cyclic disulfide-containing lipid nanoparticles for facilitating endosomal escape	52
Exploration of hydrazine-based small molecules as metal chelators for KDM4 inhibition	49
Integrating computational and experimental chemical biology revealed variable anticancer activities of phosphodiesterase isoenzyme 5 inhibitors (PDE5i) in lung cancer	48
Unusual Ni⋯Ni interaction in Ni(ii) complexes as potential inhibitors for the development of new anti-SARS-CoV-2 Omicron drugs	46
Structure–activity relationship study of PROTACs against hematopoietic prostaglandin D2 synthase	40
Research progress of anticancer drugs targeting CDK12	39
Design, synthesis, in vitro and in silico evaluation of indole-based tetrazole derivatives as putative anti-breast cancer agents	39
Cytotoxicity of phosphoramidate, bis-amidate and cycloSal prodrug metabolites against tumour and normal cells	39
Emerging opportunities in the rewiring of biology through proximity inducing small molecules	35
N-Arylsulfonamide-based adenosine analogues to target RNA cap N7-methyltransferase nsp14 of SARS-CoV-2	32
Designing Halogen-free Metal-phenolic Imidazolium Poly(Ionic Liquids) with Muti-functional Antibacterial, Anti-inflammatory and Cell Proliferation Properties for Infected Wounds	32
4-Trifluoromethyl bithiazoles as broad-spectrum antimicrobial agents for virus-related bacterial infections or co-infections	31
Back cover	29
Biocompatible glycolipid derived from bhilawanol as an antibiofilm agent and a promising platform for drug delivery	27
Contents list	27

Thiazole orange-carboplatin triplex-forming oligonucleotide (TFO) combination probes enhance targeted DNA crosslinking	27
Identification of the first structurally validated covalent ligands of the small GTPase RAB27A	27
Beta-cyclodextrin formulation of a disulfide-bond disrupting agent for improved systemic exposure	26
Development of sulfonyl fluoride chemical probes to advance the discovery of cereblon modulators	26
Unveiling sultam in drug discovery: spotlight on the underexplored scaffold	26
Effect of mono-guanidine-like derivatives on platelet aggregation and tumour cell induced platelet aggregation	26
Exploring the potential of tamoxifen-based copper(ii) dichloride in breast cancer therapy	25
Natural product-inspired [3 + 2] cycloaddition-based spirooxindoles as dual anticancer agents: synthesis, characterization, and biological evaluation by in vitro and in silico methods	23
Tackling antimicrobial stewardship through synergy and antimicrobial peptides	23
Sirtuin 1-activating derivatives belonging to the anilinopyridine class displaying in vivo cardioprotective activities	22
Contents list	22
Inside front cover	22
Design and development of sulfenylated 5-aminopyrazoles as inhibitors of acetylcholinesterase and butyrylcholinesterase: exploring the implication for Aβ1–42 aggregation inhibition in Alzhe	21
Diversely functionalized isoquinolines and their core-embedded heterocyclic frameworks: a privileged scaffold for medicinal chemistry	21
Evolution of structure-guided drug design strategies targeting mutations in codon 12 of KRAS	21
Bioassay-guided isolation of hepatoprotective lignans from Vernonia cinerea: DeepSAT-driven structural elucidation and predictive mechanistic insights against drug-induced liver injury	21
Back cover	21
The relationship between cancer risk and cystic fibrosis: the role of CFTR in cell growth and cancer development	21
Structure–activity relationships of fenarimol analogues with potent in vitro and in vivo activity against Madurella mycetomatis, the main causative agent of eumycetoma.	21
Trifluoroacetic acid-mediated synthesis of xanthene constructs and their extensive anti-tuberculosis evaluation	20
Design, synthesis and biological evaluation of rhein–piperazine–furanone hybrids as potential anticancer agents	20
Evolution of 3-(4-hydroxyphenyl)indoline-2-one as a scaffold for potent and selective anticancer activity	20
Pretargeted imaging beyond the blood–brain barrier	20
Radiosynthesis of [18F]brequinar for in vivo PET imaging of hDHODH for potential studies of acute myeloid leukemia and cancers	19
Simple accessible clemastine fumarate analogues as effective antileishmanials	19
Importance of photophosphatidylserine and Tim-3 in photoimmunotherapy	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
Recent advances from computer-aided drug design to artificial intelligence drug design	18
It's ok to be outnumbered – sub-stoichiometric modulation of homomeric protein complexes	18
Front cover	18
Structure-based design and evaluation of tyrosinase inhibitors targeting both human and mushroom isozymes	18
Exploration of cytotoxic potential and tubulin polymerization inhibition activity of cis-stilbene-1,2,3-triazole congeners	18
Discovery of dibenzylbutane lignan LCA derivatives as potent anti-inflammatory agents	18
Prodrugs and their activation mechanisms for brain drug delivery	18
The physics-AI dialogue in drug design	18
Recent insights of PROTAC developments in inflammation-mediated and autoimmune targets: a critical review	17
Design, quality and validation of the EU-OPENSCREEN fragment library poised to a high-throughput screening collection	17
Water-soluble cationic porphyrins with enhanced phototoxicity to cancer cell lines for G4-targeting photodynamic therapy	17
Light-activatable photochemically targeting chimeras (PHOTACs) enable the optical control of targeted protein degradation of HDAC6	17
Druggable targets for the immunopathy of Alzheimer's disease	16
Recent advancements in the therapeutic approaches for Alzheimer's disease treatment: current and future perspective	16
A ‘click’ chemistry approach to novel entinostat (MS-275) based class I histone deacetylase proteolysis targeting chimeras	16
Contents list	16
A story of peptides, lipophilicity and chromatography – back and forth in time	16
NIR-II imaging of hepatocellular carcinoma based on a humanized anti-GPC3 antibody	15
Design, synthesis and anti-proliferative activity of 3-aryl-evodiamine derivatives	15
On-resin synthesis of Lanreotide epimers and studies of their structure–activity relationships	15
Front cover	15
Front cover	14

Enhanced inhibitory activity of compounds containing purine scaffolds compared to protein kinase CK2α considering crystalline water	14
Back cover	14
Correction: Design and synthesis of eugenol/isoeugenol glycoconjugates and other analogues as antifungal agents against Aspergillus fumigatus	14
Proximity-induced membrane protein degradation for cancer therapies	14
Contents list	14
Can large language models predict antimicrobial peptide activity and toxicity?	14
The importance of tyrosines in multimers of cyclic RGD nonapeptides: towards αvβ6-integrin targeted radiotherapeutics	14
Scaffold hopping from indoles to indazoles yields dual MCL-1/BCL-2 inhibitors from MCL-1 selective leads	14
Rutaecarpine derivatives synthesized via skeletal reorganization alleviate inflammation-associated oxidative damage by inhibiting the MAPK/NF-κB signaling pathway	13
Stereochemical optimization of N,2-substituted cycloalkylamines as norepinephrine reuptake inhibitors	13
An allosteric inhibitor targeting the STAT3 coiled-coil domain selectively suppresses proliferation of breast cancer	13
SETDB1 as a cancer target: challenges and perspectives in drug design	13
Development of Hsp90 C-terminal inhibitors with noviomimetics that manifest anti-proliferative activities	13
Synthesis and biological evaluation of thiosemicarbazone-based antibody–drug conjugates	13
Discovery of a nasal spray steroid, tixocortol, as an inhibitor of SARS-CoV-2 main protease and viral replication	13
Synthesis, biological evaluation and computational studies of pyrazole derivatives as Mycobacterium tuberculosis CYP121A1 inhibitors	13
Design, synthesis and evaluation of 2-phenylpyrimidine derivatives as novel antifungal agents targeting CYP51	13
Stachydrine, a pyrrole alkaloid with promising therapeutic potential against metabolic syndrome and associated organ dysfunction	13
Inhibition of transcription and antiproliferative effects in a cancer cell line using antigene oligonucleotides containing artificial nucleoside analogues	13
Minimising the payload solvent exposed hydrophobic surface area optimises the antibody-drug conjugate properties	13
Insights into the modular design of kinase inhibitors and application to Abl and Axl	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
Discovery of imidazo[1,2-b]pyridazine-containing TAK1 kinase inhibitors with excellent activities against multiple myeloma	12
Novel rhodanine–thiazole hybrids as potential antidiabetic agents: a structure-based drug design approach	12
Inside front cover	12
Back cover	12
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	12
Recent advancements in the development of next-generation dual-targeting antibacterial agents	12
Hinokitiol potentiates antimicrobial activity of bismuth drugs: a combination therapy for overcoming antimicrobial resistance	12
Inside front cover	12
Geometric deep learning-guided Suzuki reaction conditions assessment for applications in medicinal chemistry	12
Pyridazinone-based derivatives as anticancer agents endowed with anti-microbial activity: molecular design, synthesis, and biological investigation	12
Exploration of piperidine 3D fragment chemical space: synthesis and 3D shape analysis of fragments derived from 20 regio- and diastereoisomers of methyl substituted pipecolinates	12
Contents list	12
The allure of targets for novel drugs	12
Research progress of metal–organic framework nanozymes in bacterial sensing, detection, and treatment	11
Development of di-arylated 1,2,4-triazole-based derivatives as therapeutic agents against breast cancer: synthesis and biological evaluation	11
Discovery of a potent and selective PROTAC degrader for STAT3	11
Anticancer potential of copper(i) complexes based on isopropyl ester derivatives of bis(pyrazol-1-yl)acetate ligands	11
Novel tetrahydropyrimidinyl-substituted benzimidazoles and benzothiazoles: synthesis, antibacterial activity, DNA interactions and ADME profiling	11
Mycobacterium tuberculosis CitA activity is modulated by cysteine oxidation and pyruvate binding	11
“Seasoning” antimalarial drugs' action: chloroquine bile salts as novel triple-stage antiplasmodial hits	11
Contents list	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
Design and evaluation of poly-nitrogenous adjuvants capable of potentiating antibiotics in Gram-negative bacteria	11
Target 2035 – update on the quest for a probe for every protein	11
Site-specific molecular glues for the 14-3-3/Tau pS214 protein–protein interaction via reversible covalent imine tethering	11
Technical, preclinical, and clinical developments of Fc-glycan-specific antibody–drug conjugates	11
Progress in the discovery and development of small molecule methuosis inducers	11
SLL-1A-16 suppresses proliferation and induces autophagy in non-small-cell lung cancer cells via the AKT/mTOR signaling pathway	11
Adjuvant strategies to tackle mcr-mediated polymyxin resistance	11
Identification of novel phenylalanine derivatives bearing a hydroxamic acid moiety as potent quorum sensing inhibitors	11
Quinazolinone-1,2,3-triazole-acetamide conjugates as potent α-glucosidase inhibitors: synthesis, enzyme inhibition, kinetic analysis, and molecular docking study	11
Development of a nitric oxide-releasing cephalexin-based hybrid compound for enhanced antimicrobial efficacy and biofilm disruption	11
Five years of research on 2,4-thiazolidinediones as anticancer agents: medicinal chemistry insights (2020–2024)	10
Distinctive roles of aquaporins and novel therapeutic opportunities against cancer	10
Inside front cover	10
Design and synthesis of novel cathepsin C inhibitors with anti-inflammatory activity	10
Design, synthesis, and biological evaluation of novel thiazole derivatives as PI3K/mTOR dual inhibitors	10
Contents list	10
Discovery of 2,3-dihydro-1H-pyrrolo[3,4-b]quinolin-1-one derivatives as possible antileishmanial agents	10
Development of thiazole-appended novel hydrazones as a new class of α-amylase inhibitors with anticancer assets: anin silicoandin vitroapproach	9
Outstanding Reviewers for RSC Medicinal Chemistry in 2024	9
Inhibition of DXR in the MEP pathway with lipophilic N-alkoxyaryl FR900098 analogs	9
Cyclometalated complexes: promising metallodrugs in the battle against cancer	9
Development of trisubstituted thiophene-3-arboxamide selenide derivatives as novel EGFR kinase inhibitors with cytotoxic activity	9
Fragment-based discovery of dual ligand pharmacophores for lipid-sensing transcription factors for designed polypharmacology	9
Integrating a quinone substructure into histone deacetylase inhibitors to cope with Alzheimer's disease and cancer	9
Recent developments in membrane targeting antifungal agents to mitigate antifungal resistance	9
Rational design and in vitro testing of new urease inhibitors to prevent urinary catheter blockage	9
Design and synthesis of cyclic lipidated peptides derived from the C-terminus of Cx43 for hemichannel inhibition and cardiac endothelium targeting	9
Ribosome-targeting antibiotics and resistance via ribosomal RNA methylation	9
EGFRAP: a predictive machine learning model for assessing small molecule activity against the epidermal growth factor receptor	9
Back cover	9
Insights into the recent progress in the medicinal chemistry of pyranopyrimidine analogs	9
Molecular understanding of the therapeutic potential of melanin inhibiting natural products	9
Guggulsterone – a potent bioactive phytosteroid: synthesis, structural modification, and its improved bioactivities	9
Synthesis and antiplasmodial activity of 6H,13H-pyrazino[1,2-a;4,5-a′]diindole analogues substituted with basic side chains	9
The synthesis and bioactivities of ROCK2 inhibitors with 1,2-dithiolan-3-yl motif	9
Identification of SARS-CoV-2 Mpro inhibitors through deep reinforcement learning for de novo drug design and computational chemistry approaches	9

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	9
Novel lithocholic acid-diindolylmethane hybrids as potent sialyltransferase inhibitors targeting triple-negative breast cancer: a molecular hybridization approach	9
Correction: Minimising the payload solvent exposed hydrophobic surface area optimises the antibody–drug conjugate properties	8
Introduction to the themed collection in honour of Professor Christian Leumann	8
Complexity of αvβ6-integrin targeting RGD peptide trimers: emergence of non-specific binding by synergistic interaction	8
Back cover	8
Contents list	8
Contents list	8
Contents list	8
Synthesis of full-length homodimer αD-VxXXB that targets human α7 nicotinic acetylcholine receptors	8
Thiazolidine-2,4-dione hybrids as dual alpha-amylase and alpha-glucosidase inhibitors: design, synthesis, in vitro and in vivo anti-diabetic evaluation	8
Lysine targeting covalent inhibitors of malarial kinase PfCLK3	8
Semisynthetic blasticidin S ester derivatives show enhanced antibiotic activity	8
Stereoselective synthesis and antiproliferative activity of allo-gibberic acid-based 1,3-aminoalcohol regioisomers	8
Front cover	8
Macrocyclic RGD-peptides with high selectivity for αvβ3 integrin in cancer imaging and therapy	8
Back cover	8
AlbiCDN: albumin-binding amphiphilic STING agonists augment the immune activity for cancer immunotherapy	8
Synthesis and investigation of thieno[2,3-b]pyridines that restore activity of topotecan	8
QSAR, structure-based pharmacophore modelling and biological evaluation of novel platelet ADP receptor (P2Y12) antagonist	8
Applications of supramolecular assemblies in drug delivery and photodynamic therapy	8
Analysis of the structural diversity of heterocycles amongst European medicines agency approved pharmaceuticals (2014–2023)	8
Live cell screening to identify RNA-binding small molecule inhibitors of the pre-let-7–Lin28 RNA–protein interaction	8
Design, synthesis, antimicrobial activity, stability, and mechanism of action of bioresorbable ceragenins	7
Discovery of first-in-class PROTACs targeting maternal embryonic leucine zipper kinase (MELK) for the treatment of Burkitt lymphoma	7
Introduction to the themed collection on ‘Targeting RNA with small molecules’	7
The Mycobacterium tuberculosis mycothiol S-transferase is divalent metal-dependent for mycothiol binding and transfer	7
Copper selective 8-aminoquinoline based tetradentate chelators as anticancer agents	7
Computer-aided discovery of triazolothiadiazoles as DYRK1A-targeted neuroprotective agents	7
Design, synthesis and biological evaluation of light-driven on–off multitarget AChE and MAO-B inhibitors	7
Front cover	7
Development of pharmacophore models for AcrB protein and the identification of potential adjuvant candidates for overcoming efflux-mediated colistin resistance	7
NLRP3 inflammasome: structure, mechanism, drug-induced organ toxicity, therapeutic strategies, and future perspectives	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
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
Discovery of selective, metabolically stable pyrazole-based FLT3 inhibitors for the treatment of acute myeloid leukemia	7
Recent advances in structural modifications of natural products for anti-leishmaniasis therapy (2010–2024)	7
Polysucrose hydrogel loaded with natural molecules/extracts for multiphase-directed sustainable wound healing	7
Inhibition of bacterial RNA polymerase function and protein–protein interactions: a promising approach for next-generation antibacterial therapeutics	7
Design, synthesis and biological evaluation of novel β-caryophyllene derivatives as potential anti-cancer agents through the ROS-mediated apoptosis pathway	7
Novel pirfenidone derivatives: synthesis and biological evaluation	7
Design, synthesis, molecular docking and anti-proliferative activity of novel phenothiazine containing imidazo[1,2-a]pyridine derivatives against MARK4 protein	7
Design, synthesis, and biological evaluation of new arjunolic acid derivatives as anticancer agents	7
Front cover	7
Synthesis and properties of the kojic acid dimer and its potential for the treatment of Alzheimer's disease	7
Front cover	7
Modulating polybasic character of galactose-based glycosylated antitumor ether lipids for enhanced cytotoxic response	7
Contents list	7
Expanding the chemical space for antiviral discovery: the potential of twistenediones	7
The rise of ultrashort cationic β-peptides as promising antimicrobial therapeutics	7
Design of chitosan-coated CeO2-doped ZnCr LDO nanocomposites for optimized azithromycin delivery: a kinetic and mechanistic perspective	7
Front cover	7
Preventing SARS-CoV-2 infection using Fv-antibodies targeting the proprotein convertase (PPC) cleavage site	7
Design, synthesis and in vitro evaluations of new cyclotriphosphazenes as safe drug candidates	7
Contents list	7
Design, synthesis, and evaluation of benzhydrylpiperazine-based novel dual COX-2/5-LOX inhibitors with anti-inflammatory and anti-cancer activity	7
Novel benzimidazole-based pseudo-irreversible butyrylcholinesterase inhibitors with neuroprotective activity in an Alzheimer's disease mouse model	6
Back cover	6
Tanshinones Target Drug-Resistant Tuberculosis: Efficacy, Selectivity, and Potential Mechanism of Action	6
Targeting host integrated stress response: lead discovery of flavonoid compounds active against coronaviruses PEDV and PDCoV	6
In vitro evaluation of the immunogenic potential of gramicidin S and its photocontrolled analogues	6
Structure-guided design of a methyltransferase-like 3 (METTL3) proteolysis targeting chimera (PROTAC) incorporating an indole–nicotinamide chemotype	6
Semisynthetic polymyxins with potent antibacterial activity and reduced kidney cell toxicity	6
Back cover	6
Front cover	6
Design, synthesis, and SAR of antiproliferative activity of trioxatriangulene derivatives	6
A review on small molecular mimics of antimicrobial peptides with an emphasis on the structure–activity relationship perspective	6
Designed hybrid anticancer nuclear-localized peptide inhibits aggressive cancer cell proliferation	6
Enhanced skin penetration of curcumin by a nanoemulsion-embedded oligopeptide hydrogel for psoriasis topical therapy	6
Contents list	6
Novel benzimidazole hybrids: design, synthesis, mechanistic studies, antifungal potential and molecular dynamics	6
Design and synthesis of novel 8-(azaindolyl)-benzoazepinones as potent and selective ROCK inhibitors	6
Heterocyclic compounds as xanthine oxidase inhibitors for the management of hyperuricemia: synthetic strategies, structure–activity relationship and molecular docking studies (2018–2024)	6
Development, biological evaluation, and molecular modelling of novel isocytosine and guanidine derivatives as BACE1 inhibitors using a fragment growing strategy	6
Synthesis and evaluation of tetrahydropyrrolo[1,2-a]quinolin-1(2H)-ones as new tubulin polymerization inhibitors	6
From traditional medicine to nanomedicine: potential of Ginkgo biloba extracts in treating inflammatory skin diseases	6
Discovery of novel dehydroabietylamine–pyrimidine hybrids: design, synthesis and anti-tumor evaluation	6
Synthetic 18F labeled biomolecules that are selective and promising for PET imaging: major advances and applications	6
Optimizing linker rigidity to improve intracellular behavior of PROTACs targeting hematopoietic prostaglandin D synthase	6
Exploring medium and long arm extensions of 1,2,4-triazole derivatives as Candida albicans 14α-demethylase (CYP51) inhibitors	6
Structural insights into the nirmatrelvir-resistant SARS-CoV-2 Mpro L50F/E166A/L167F triple mutant-inhibitor-complex reveal strategies for next generation coronaviral inhibitor design	6
Expanding the structure–activity relationships of alkynyl diphenylurea scaffold as promising antibacterial agents	6
News from RSC Medicinal Chemistry	6
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism	6
Novel flexible biphenyl PfDHFR inhibitors with improved antimalarial activity	6
Discovery and computational studies of piperidine/piperazine-based compounds endowed with sigma receptor affinity	6
The era of high-quality chemical probes	6
Benzenesulfonamide decorated dihydropyrimidin(thi)ones: carbonic anhydrase profiling and antiproliferative activity	6
Mannich reaction mediated derivatization of chromones and their biological evaluations as putative multipotent ligands for the treatment of Alzheimer's disease	6
Phenylthiazoles with potent & optimum selectivity toward Clostridium difficile	6
Near-infrared photochemical internalization: design of a distorted zinc phthalocyanine for efficient intracellular delivery of immunotoxins	6
Contents list	6
PK 11195 derivatives: exploring the influence of amide and heterocyclic substitution on A147T TSPO discrimination	6
Discovery of benzoheterocyclic-substituted amide derivatives as apoptosis signal-regulating kinase 1 (ASK1) inhibitors	6
Design and synthesis of coumarin-based amphoteric antimicrobials with biofilm interference and immunoregulation effects	6