RSC Medicinal Chemistry

Article	Citations
Covalent cannabinoid receptor ligands – structural insight and selectivity challenges	134
Recent advances of phenotypic screening strategies in the application of anti-influenza virus drug discovery	97
Expanding the chemical space of ester of quinoxaline-7-carboxylate 1,4-di-N-oxide derivatives as potential antitubercular agents	74
Back cover	72
Inside front cover	68
Back cover	68
Back cover	63
Contents list	63
Emerging opportunities in the rewiring of biology through proximity inducing small molecules	59
Design, synthesis and structure-activity relationship analysis of the dibenzodiazepinone derivatives against osimertinib resistant NSCLC	59
4-Trifluoromethyl bithiazoles as broad-spectrum antimicrobial agents for virus-related bacterial infections or co-infections	57
N-Arylsulfonamide-based adenosine analogues to target RNA cap N7-methyltransferase nsp14 of SARS-CoV-2	55
Research progress of anticancer drugs targeting CDK12	50
New azole derivatives linked to indole/indoline moieties combined with FLC against drug-resistant Candida albicans	50
Thiazole orange-carboplatin triplex-forming oligonucleotide (TFO) combination probes enhance targeted DNA crosslinking	43
Unveiling sultam in drug discovery: spotlight on the underexplored scaffold	41
ATP-competitive inhibitors for cancer treatment – kinases and the world beyond	41
In vivo demonstration of enhanced mRNA delivery by cyclic disulfide-containing lipid nanoparticles for facilitating endosomal escape	40
Exploration of hydrazine-based small molecules as metal chelators for KDM4 inhibition	36
Integrating computational and experimental chemical biology revealed variable anticancer activities of phosphodiesterase isoenzyme 5 inhibitors (PDE5i) in lung cancer	34
Cytotoxicity of phosphoramidate, bis-amidate and cycloSal prodrug metabolites against tumour and normal cells	33
Biocompatible glycolipid derived from bhilawanol as an antibiofilm agent and a promising platform for drug delivery	32
Structure–activity relationship study of PROTACs against hematopoietic prostaglandin D2 synthase	32
Development of sulfonyl fluoride chemical probes to advance the discovery of cereblon modulators	29
Effect of mono-guanidine-like derivatives on platelet aggregation and tumour cell induced platelet aggregation	29

Beta-cyclodextrin formulation of a disulfide-bond disrupting agent for improved systemic exposure	29
Unusual Ni⋯Ni interaction in Ni(ii) complexes as potential inhibitors for the development of new anti-SARS-CoV-2 Omicron drugs	27
Designing halogen-free metal–phenolic imidazolium poly(ionic liquids) with multi-functional antibacterial, anti-inflammatory and cell proliferation properties for infected wounds	27
Identification of the first structurally validated covalent ligands of the small GTPase RAB27A	27
Design, synthesis, in vitro and in silico evaluation of indole-based tetrazole derivatives as putative anti-breast cancer agents	26
Exploring the potential of tamoxifen-based copper(ii) dichloride in breast cancer therapy	26
Metabolic labelling of cancer cells with glycodendrimers stimulate immune-mediated cytotoxicity	26
Synthesis and biological evaluation of novel D-ring fused steroidal N(2)-substituted-1,2,3-triazoles	26
Inside front cover	24
Natural product-inspired [3 + 2] cycloaddition-based spirooxindoles as dual anticancer agents: synthesis, characterization, and biological evaluation by in vitro and in silico methods	24
Sirtuin 1-activating derivatives belonging to the anilinopyridine class displaying in vivo cardioprotective activities	23
Contents list	23
Design and development of sulfenylated 5-aminopyrazoles as inhibitors of acetylcholinesterase and butyrylcholinesterase: exploring the implication for Aβ1–42 aggregation inhibition in Alzhe	22
Cornulacin: a new isoflavone fromCornulaca monacanthaand its isolation, structure elucidation and cytotoxicity through EGFR-mediated apoptosis	22
Back cover	22
Trifluoroacetic acid-mediated synthesis of xanthene constructs and their extensive anti-tuberculosis evaluation	22
Importance of photophosphatidylserine and Tim-3 in photoimmunotherapy	21
Front cover	21
Radiosynthesis of [18F]brequinar for in vivo PET imaging of hDHODH for potential studies of acute myeloid leukemia and cancers	21
Simple accessible clemastine fumarate analogues as effective antileishmanials	21
Discovery of dibenzylbutane lignan LCA derivatives as potent anti-inflammatory agents	21
Structure–activity relationships of fenarimol analogues with potent in vitro and in vivo activity against Madurella mycetomatis, the main causative agent of mycetoma	20
It's ok to be outnumbered – sub-stoichiometric modulation of homomeric protein complexes	20
Evolution of 3-(4-hydroxyphenyl)indoline-2-one as a scaffold for potent and selective anticancer activity	20
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	20
Structure-based design and evaluation of tyrosinase inhibitors targeting both human and mushroom isozymes	20
A story of peptides, lipophilicity and chromatography – back and forth in time	20
Prodrugs and their activation mechanisms for brain drug delivery	19
Recent advances from computer-aided drug design to artificial intelligence drug design	19
Design, quality and validation of the EU-OPENSCREEN fragment library poised to a high-throughput screening collection	19
Evolution of structure-guided drug design strategies targeting mutations in codon 12 of KRAS	19
The relationship between cancer risk and cystic fibrosis: the role of CFTR in cell growth and cancer development	19
Light-activatable photochemically targeting chimeras (PHOTACs) enable the optical control of targeted protein degradation of HDAC6	19
Tackling antimicrobial stewardship through synergy and antimicrobial peptides	19
Exploration of cytotoxic potential and tubulin polymerization inhibition activity of cis-stilbene-1,2,3-triazole congeners	19
Recent insights of PROTAC developments in inflammation-mediated and autoimmune targets: a critical review	19
A ‘click’ chemistry approach to novel entinostat (MS-275) based class I histone deacetylase proteolysis targeting chimeras	18
Pretargeted imaging beyond the blood–brain barrier	18
Design, synthesis and biological evaluation of rhein–piperazine–furanone hybrids as potential anticancer agents	17
The physics-AI dialogue in drug design	17
Water-soluble cationic porphyrins with enhanced phototoxicity to cancer cell lines for G4-targeting photodynamic therapy	17
Diversely functionalized isoquinolines and their core-embedded heterocyclic frameworks: a privileged scaffold for medicinal chemistry	16
On-resin synthesis of Lanreotide epimers and studies of their structure–activity relationships	16
Bioassay-guided isolation of hepatoprotective lignans from Vernonia cinerea: DeepSAT-driven structural elucidation and predictive mechanistic insights against drug-induced liver injury	16
Druggable targets for the immunopathy of Alzheimer's disease	16
Front cover	16
Design, synthesis and anti-proliferative activity of 3-aryl-evodiamine derivatives	16
Contents list	16
Front cover	16
The importance of tyrosines in multimers of cyclic RGD nonapeptides: towards αvβ6-integrin targeted radiotherapeutics	15

Discovery of imidazo[1,2-b]pyridazine-containing TAK1 kinase inhibitors with excellent activities against multiple myeloma	15
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	15
Proximity-induced membrane protein degradation for cancer therapies	15
Enhanced inhibitory activity of compounds containing purine scaffolds compared to protein kinase CK2α considering crystalline water	15
Hinokitiol potentiates antimicrobial activity of bismuth drugs: a combination therapy for overcoming antimicrobial resistance	15
Correction: Design and synthesis of eugenol/isoeugenol glycoconjugates and other analogues as antifungal agents against Aspergillus fumigatus	15
Discovery of a nasal spray steroid, tixocortol, as an inhibitor of SARS-CoV-2 main protease and viral replication	14
Contents list	14
Design, synthesis and evaluation of 2-phenylpyrimidine derivatives as novel antifungal agents targeting CYP51	14
Minimising the payload solvent exposed hydrophobic surface area optimises the antibody-drug conjugate properties	14
SETDB1 as a cancer target: challenges and perspectives in drug design	14
Stereochemical optimization of N,2-substituted cycloalkylamines as norepinephrine reuptake inhibitors	14
Inhibition of transcription and antiproliferative effects in a cancer cell line using antigene oligonucleotides containing artificial nucleoside analogues	14
Development of Hsp90 C-terminal inhibitors with noviomimetics that manifest anti-proliferative activities	14
Back cover	14
Recent advancements in the development of next-generation dual-targeting antibacterial agents	13
The allure of targets for novel drugs	13
Synthesis and biological evaluation of thiosemicarbazone-based antibody–drug conjugates	13
Novel rhodanine–thiazole hybrids as potential antidiabetic agents: a structure-based drug design approach	13
Stachydrine, a pyrrole alkaloid with promising therapeutic potential against metabolic syndrome and associated organ dysfunction	13
Geometric deep learning-guided Suzuki reaction conditions assessment for applications in medicinal chemistry	13
Insights into the modular design of kinase inhibitors and application to Abl and Axl	13
Recent advancements in the therapeutic approaches for Alzheimer's disease treatment: current and future perspective	13
Rutaecarpine derivatives synthesized via skeletal reorganization alleviate inflammation-associated oxidative damage by inhibiting the MAPK/NF-κB signaling pathway	13
Synthesis, biological evaluation and computational studies of pyrazole derivatives as Mycobacterium tuberculosis CYP121A1 inhibitors	13
From fragments to follow-ups: rapid hit expansion by making use of EU-OPENSCREEN resources	13
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
Scaffold hopping from indoles to indazoles yields dual MCL-1/BCL-2 inhibitors from MCL-1 selective leads	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
An allosteric inhibitor targeting the STAT3 coiled-coil domain selectively suppresses proliferation of breast cancer	13
Glioblastoma Antitumoral Activity of Tetrahydroquinoline-derived Triarylmethanes	13
Can large language models predict antimicrobial peptide activity and toxicity?	13
Contents list	12
Inside front cover	12
NIR-II imaging of hepatocellular carcinoma based on a humanized anti-GPC3 antibody	12
Discovery of a potent and selective PROTAC degrader for STAT3	12
Identification of novel phenylalanine derivatives bearing a hydroxamic acid moiety as potent quorum sensing inhibitors	12
Back cover	12
Mycobacterium tuberculosis CitA activity is modulated by cysteine oxidation and pyruvate binding	12
Design and evaluation of poly-nitrogenous adjuvants capable of potentiating antibiotics in Gram-negative bacteria	12
Contents list	12
“Seasoning” antimalarial drugs' action: chloroquine bile salts as novel triple-stage antiplasmodial hits	12
Pyridazinone-based derivatives as anticancer agents endowed with anti-microbial activity: molecular design, synthesis, and biological investigation	12
Inside front cover	12
Development of a nitric oxide-releasing cephalexin-based hybrid compound for enhanced antimicrobial efficacy and biofilm disruption	12
Technical, preclinical, and clinical developments of Fc-glycan-specific antibody–drug conjugates	12
Development of di-arylated 1,2,4-triazole-based derivatives as therapeutic agents against breast cancer: synthesis and biological evaluation	12
Novel tetrahydropyrimidinyl-substituted benzimidazoles and benzothiazoles: synthesis, antibacterial activity, DNA interactions and ADME profiling	11
Inside front cover	11
Progress in the discovery and development of small molecule methuosis inducers	11
Site-specific molecular glues for the 14-3-3/Tau pS214 protein–protein interaction via reversible covalent imine tethering	11
Five years of research on 2,4-thiazolidinediones as anticancer agents: medicinal chemistry insights (2020–2024)	11
Anticancer potential of copper(i) complexes based on isopropyl ester derivatives of bis(pyrazol-1-yl)acetate ligands	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
SLL-1A-16 suppresses proliferation and induces autophagy in non-small-cell lung cancer cells via the AKT/mTOR signaling pathway	11
Synthesis and evaluation of HFIP bearing triazolo-amides as amyloid-β aggregation inhibitor and suppressor of aggregation induced neuroinflammation	11
Target 2035 – update on the quest for a probe for every protein	11
Design, synthesis, and biological evaluation of novel thiazole derivatives as PI3K/mTOR dual inhibitors	11
Research progress of metal–organic framework nanozymes in bacterial sensing, detection, and treatment	11
Quinazolinone-1,2,3-triazole-acetamide conjugates as potent α-glucosidase inhibitors: synthesis, enzyme inhibition, kinetic analysis, and molecular docking study	11
Adjuvant strategies to tackle mcr-mediated polymyxin resistance	11
Outstanding Reviewers for RSC Medicinal Chemistry in 2024	10
Semisynthetic blasticidin S ester derivatives show enhanced antibiotic activity	10
Back cover	10
Rational design and in vitro testing of new urease inhibitors to prevent urinary catheter blockage	10
The synthesis and bioactivities of ROCK2 inhibitors with 1,2-dithiolan-3-yl motif	10
Distinctive roles of aquaporins and novel therapeutic opportunities against cancer	10
Guggulsterone – a potent bioactive phytosteroid: synthesis, structural modification, and its improved bioactivities	10
Cyclometalated complexes: promising metallodrugs in the battle against cancer	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
Discovery of 2,3-dihydro-1H-pyrrolo[3,4-b]quinolin-1-one derivatives as possible antileishmanial agents	10
Integrating a quinone substructure into histone deacetylase inhibitors to cope with Alzheimer's disease and cancer	10
Development of thiazole-appended novel hydrazones as a new class of α-amylase inhibitors with anticancer assets: anin silicoandin vitroapproach	10
Identification of SARS-CoV-2 Mpro inhibitors through deep reinforcement learning for de novo drug design and computational chemistry approaches	10
Synthesis of full-length homodimer αD-VxXXB that targets human α7 nicotinic acetylcholine receptors	9
Contents list	9
Inhibition of DXR in the MEP pathway with lipophilic N-alkoxyaryl FR900098 analogs	9
Design and synthesis of novel cathepsin C inhibitors with anti-inflammatory activity	9
Lysine targeting covalent inhibitors of malarial kinase PfCLK3	9

EGFRAP: a predictive machine learning model for assessing small molecule activity against the epidermal growth factor receptor	9
Synthesis and antiplasmodial activity of 6H,13H-pyrazino[1,2-a;4,5-a′]diindole analogues substituted with basic side chains	9
Recent developments in membrane targeting antifungal agents to mitigate antifungal resistance	9
QSAR, structure-based pharmacophore modelling and biological evaluation of novel platelet ADP receptor (P2Y12) antagonist	9
Correction: Minimising the payload solvent exposed hydrophobic surface area optimises the antibody–drug conjugate properties	9
Insights into the recent progress in the medicinal chemistry of pyranopyrimidine analogs	9
Novel lithocholic acid-diindolylmethane hybrids as potent sialyltransferase inhibitors targeting triple-negative breast cancer: a molecular hybridization approach	9
Design and synthesis of cyclic lipidated peptides derived from the C-terminus of Cx43 for hemichannel inhibition and cardiac endothelium targeting	9
AlbiCDN: albumin-binding amphiphilic STING agonists augment the immune activity for cancer immunotherapy	9
Molecular understanding of the therapeutic potential of melanin inhibiting natural products	9
Synthesis and investigation of thieno[2,3-b]pyridines that restore activity of topotecan	9
Contents list	9
Back cover	9
Introduction to the themed collection in honour of Professor Christian Leumann	9
Back cover	9
Fragment-based discovery of dual ligand pharmacophores for lipid-sensing transcription factors for designed polypharmacology	9
Ribosome-targeting antibiotics and resistance via ribosomal RNA methylation	9
Development of trisubstituted thiophene-3-arboxamide selenide derivatives as novel EGFR kinase inhibitors with cytotoxic activity	9
Complexity of αvβ6-integrin targeting RGD peptide trimers: emergence of non-specific binding by synergistic interaction	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
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
Inhibition of bacterial RNA polymerase function and protein–protein interactions: a promising approach for next-generation antibacterial therapeutics	8
Macrocyclic RGD-peptides with high selectivity for αvβ3 integrin in cancer imaging and therapy	8
Design, synthesis and biological evaluation of novel β-caryophyllene derivatives as potential anti-cancer agents through the ROS-mediated apoptosis pathway	8
Preventing SARS-CoV-2 infection using Fv-antibodies targeting the proprotein convertase (PPC) cleavage site	8
Novel pirfenidone derivatives: synthesis and biological evaluation	8
Front cover	8
Front cover	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
Applications of supramolecular assemblies in drug delivery and photodynamic therapy	8
Contents list	8
The rise of ultrashort cationic β-peptides as promising antimicrobial therapeutics	8
Polysucrose hydrogel loaded with natural molecules/extracts for multiphase-directed sustainable wound healing	8
Contents list	8
NLRP3 inflammasome: structure, mechanism, drug-induced organ toxicity, therapeutic strategies, and future perspectives	7
Discovery and computational studies of piperidine/piperazine-based compounds endowed with sigma receptor affinity	7
Benzenesulfonamide decorated dihydropyrimidin(thi)ones: carbonic anhydrase profiling and antiproliferative activity	7
Identification of Spirodioxolane nsP2 Helicase Inhibitors with Antialphaviral Activity	7
Discovery of novel dehydroabietylamine–pyrimidine hybrids: design, synthesis and anti-tumor evaluation	7
Front cover	7
Synthesis and evaluation of tetrahydropyrrolo[1,2-a]quinolin-1(2H)-ones as new tubulin polymerization inhibitors	7
Design, synthesis, antimicrobial activity, stability, and mechanism of action of bioresorbable ceragenins	7
Design, synthesis, and biological evaluation of new arjunolic acid derivatives as anticancer agents	7
Copper selective 8-aminoquinoline based tetradentate chelators as anticancer agents	7
Design of chitosan-coated CeO2-doped ZnCr LDO nanocomposites for optimized azithromycin delivery: a kinetic and mechanistic perspective	7
Design, synthesis, molecular docking and anti-proliferative activity of novel phenothiazine containing imidazo[1,2-a]pyridine derivatives against MARK4 protein	7
Tanshinones target drug-resistant tuberculosis: efficacy, selectivity, and potential mechanism of action	7
Mannich reaction mediated derivatization of chromones and their biological evaluations as putative multipotent ligands for the treatment of Alzheimer's disease	7
Heterocyclic compounds as xanthine oxidase inhibitors for the management of hyperuricemia: synthetic strategies, structure–activity relationship and molecular docking studies (2018–2024)	7
Enhanced skin penetration of curcumin by a nanoemulsion-embedded oligopeptide hydrogel for psoriasis topical therapy	7
Design, synthesis and in vitro evaluations of new cyclotriphosphazenes as safe drug candidates	7
Discovery of selective, metabolically stable pyrazole-based FLT3 inhibitors for the treatment of acute myeloid leukemia	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
Modulating polybasic character of galactose-based glycosylated antitumor ether lipids for enhanced cytotoxic response	7
Recent advances in structural modifications of natural products for anti-leishmaniasis therapy (2010–2024)	7
Design, Synthesis, and Biological Evaluation of Sulfonamide-Functionalized Pyridine Carbothioamides as Potent Tubulin-Targeting Anticancer Agents	7
Computer-aided discovery of triazolothiadiazoles as DYRK1A-targeted neuroprotective agents	7
Contents list	7
Front cover	7
Development, biological evaluation, and molecular modelling of novel isocytosine and guanidine derivatives as BACE1 inhibitors using a fragment growing strategy	7
Novel benzimidazole hybrids: design, synthesis, mechanistic studies, antifungal potential and molecular dynamics	7
In vitro evaluation of the immunogenic potential of gramicidin S and its photocontrolled analogues	7
Synthesis and properties of the kojic acid dimer and its potential for the treatment of Alzheimer's disease	7
Development of pharmacophore models for AcrB protein and the identification of potential adjuvant candidates for overcoming efflux-mediated colistin resistance	7
Front cover	7
Novel benzimidazole-based pseudo-irreversible butyrylcholinesterase inhibitors with neuroprotective activity in an Alzheimer's disease mouse model	7
Discovery of first-in-class PROTACs targeting maternal embryonic leucine zipper kinase (MELK) for the treatment of Burkitt lymphoma	7
Design, synthesis and biological evaluation of light-driven on–off multitarget AChE and MAO-B inhibitors	7
Live cell screening to identify RNA-binding small molecule inhibitors of the pre-let-7–Lin28 RNA–protein interaction	7
Analysis of the structural diversity of heterocycles amongst European medicines agency approved pharmaceuticals (2014–2023)	7
Expanding the scope of novel 1,2,3-triazole derivatives as new antiparasitic drug candidates	6
Design and synthesis of coumarin-based amphoteric antimicrobials with biofilm interference and immunoregulation effects	6
From traditional medicine to nanomedicine: potential of Ginkgo biloba extracts in treating inflammatory skin diseases	6
Reactive fragments targeting carboxylate residues employing direct to biology, high-throughput chemistry	6
An overview of the development of EED inhibitors to disable the PRC2 function	6
Inhibition of monoamine oxidases by heterocyclic derived conjugated dienones: synthesis and in vitro and in silico investigations	6
Back cover	6
Back cover	6
Bicyclic temporin L peptide inhibitors targeting the SARS-CoV-2 main protease: design, synthesis, in vitro inhibition efficiency and molecular dynamics insights	6
Novel curcumin-based analogues as potential VEGFR2 inhibitors with promising metallic loading nanoparticles: synthesis, biological evaluation, and molecular modelling investigation	6
Antitubercular evaluation of dihydropyridine–triazole conjugates: design, synthesis, in vitro screening, SAR and in silico ADME predictions	6
Lactose-conjugated 2-iminothiazolidin-4-ones: synthesis, inhibitory activity and molecular simulations as potential inhibitors against enzymes responsible for type 2 diabetes	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
A review on small molecular mimics of antimicrobial peptides with an emphasis on the structure–activity relationship perspective	6
Back cover	6
Ruthenium(ii)–arene complexes as anti-metastatic agents, and related techniques	6
Structural insights into the activity of carbapenemases: understanding the mechanism of action of current inhibitors and informing the design of new carbapenem adjuvants	6
Discovery and optimisation of pyrazolo[1,5-a]pyrimidines as aryl hydrocarbon receptor antagonists	6
Repurposing of USFDA-approved drugs to identify leads for inhibition of acetylcholinesterase enzyme: a plausible utility as an anti-Alzheimer agent	6
Optimizing linker rigidity to improve intracellular behavior of PROTACs targeting hematopoietic prostaglandin D synthase	6
Prediction of synergistic gemcitabine-based combination treatment through a novel tumor stemness biomarker NANOG in pancreatic cancer	6
Chemical genetic approaches for the discovery of bacterial cell wall inhibitors	6
Front cover	6