RSC Medicinal Chemistry

Article	Citations
Covalent cannabinoid receptor ligands – structural insight and selectivity challenges	119
Recent advances of phenotypic screening strategies in the application of anti-influenza virus drug discovery	88
Expanding the chemical space of ester of quinoxaline-7-carboxylate 1,4-di-N-oxide derivatives as potential antitubercular agents	68
Synthesis and biological evaluation of novel D-ring fused steroidal N(2)-substituted-1,2,3-triazoles	60
Structure–activity relationship study of PROTACs against hematopoietic prostaglandin D2 synthase	58
Metabolic labelling of cancer cells with glycodendrimers stimulate immune-mediated cytotoxicity	57
New azole derivatives linked to indole/indoline moieties combined with FLC against drug-resistant Candida albicans	57
Back cover	55
Back cover	52
Contents list	52
Back cover	47
Inside front cover	44
Thiazole orange-carboplatin triplex-forming oligonucleotide (TFO) combination probes enhance targeted DNA crosslinking	43
4-Trifluoromethyl bithiazoles as broad-spectrum antimicrobial agents for virus-related bacterial infections or co-infections	43
Effect of mono-guanidine-like derivatives on platelet aggregation and tumour cell induced platelet aggregation	38
Biocompatible glycolipid derived from bhilawanol as an antibiofilm agent and a promising platform for drug delivery	38
In vivo demonstration of enhanced mRNA delivery by cyclic disulfide-containing lipid nanoparticles for facilitating endosomal escape	38
Development of sulfonyl fluoride chemical probes to advance the discovery of cereblon modulators	33
Exploration of hydrazine-based small molecules as metal chelators for KDM4 inhibition	32
Research progress of anticancer drugs targeting CDK12	30
ATP-competitive inhibitors for cancer treatment – kinases and the world beyond	28
Integrating computational and experimental chemical biology revealed variable anticancer activities of phosphodiesterase isoenzyme 5 inhibitors (PDE5i) in lung cancer	28
Identification of the first structurally validated covalent ligands of the small GTPase RAB27A	27
Cytotoxicity of phosphoramidate, bis-amidate and cycloSal prodrug metabolites against tumour and normal cells	27
Exploring the potential of tamoxifen-based copper(ii) dichloride in breast cancer therapy	26

Emerging opportunities in the rewiring of biology through proximity inducing small molecules.	26
Beta-cyclodextrin formulation of a disulfide-bond disrupting agent for improved systemic exposure	26
Design, synthesis, in vitro and in silico evaluation of indole-based tetrazole derivatives as putative anti-breast cancer agents	25
N-Arylsulfonamide-based adenosine analogues to target RNA cap N7-methyltransferase nsp14 of SARS-CoV-2	24
Unveiling sultam in drug discovery: spotlight on the underexplored scaffold	24
Unusual Ni⋯Ni interaction in Ni(ii) complexes as potential inhibitors for the development of new anti-SARS-CoV-2 Omicron drugs	24
Sirtuin 1-activating derivatives belonging to the anilinopyridine class displaying in vivo cardioprotective activities	22
Inside front cover	22
Contents list	22
Front cover	21
Tackling antimicrobial stewardship through synergy and antimicrobial peptides	21
Simple accessible clemastine fumarate analogues as effective antileishmanials	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
Radiosynthesis of [18F]brequinar for in vivo PET imaging of hDHODH for potential studies of acute myeloid leukemia and cancers	20
Design, quality and validation of the EU-OPENSCREEN fragment library poised to a high-throughput screening collection	20
Cornulacin: a new isoflavone fromCornulaca monacanthaand its isolation, structure elucidation and cytotoxicity through EGFR-mediated apoptosis	20
Importance of photophosphatidylserine and Tim-3 in photoimmunotherapy	20
Design, synthesis and biological evaluation of rhein–piperazine–furanone hybrids as potential anticancer agents	19
The relationship between cancer risk and cystic fibrosis: the role of CFTR in cell growth and cancer development	19
A story of peptides, lipophilicity and chromatography – back and forth in time	19
The physics-AI dialogue in drug design	19
Trifluoroacetic acid-mediated synthesis of xanthene constructs and their extensive anti-tuberculosis evaluation	19
Bioassay-guided isolation of hepatoprotective lignans from Vernonia cinerea: DeepSAT-driven structural elucidation and predictive mechanistic insights against drug-induced liver injury	19
Evolution of structure-guided drug design strategies targeting mutations in codon 12 of KRAS	19
Pretargeted imaging beyond the blood–brain barrier	19
Recent insights of PROTAC developments in inflammation-mediated and autoimmune targets: a critical review	18
Prodrugs and their activation mechanisms for brain drug delivery	18
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
Structure-based design and evaluation of tyrosinase inhibitors targeting both human and mushroom isozymes	18
Discovery of dibenzylbutane lignan LCA derivatives as potent anti-inflammatory agents	17
Exploration of cytotoxic potential and tubulin polymerization inhibition activity of cis-stilbene-1,2,3-triazole congeners	17
Back cover	17
A ‘click’ chemistry approach to novel entinostat (MS-275) based class I histone deacetylase proteolysis targeting chimeras	17
It's ok to be outnumbered – sub-stoichiometric modulation of homomeric protein complexes	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
Recent advances from computer-aided drug design to artificial intelligence drug design	16
Hinokitiol potentiates antimicrobial activity of bismuth drugs: a combination therapy for overcoming antimicrobial resistance	16
Evolution of 3-(4-hydroxyphenyl)indoline-2-one as a scaffold for potent and selective anticancer activity	16
Contents list	16
Druggable targets for the immunopathy of Alzheimer's disease	16
Diversely functionalized isoquinolines and their core-embedded heterocyclic frameworks: a privileged scaffold for medicinal chemistry	16
Light-activatable photochemically targeting chimeras (PHOTACs) enable the optical control of targeted protein degradation of HDAC6	16
The allure of targets for novel drugs	16
Contents list	15
Correction: Design and synthesis of eugenol/isoeugenol glycoconjugates and other analogues as antifungal agents against Aspergillus fumigatus	15
Front cover	15
Front cover	15
Back cover	14
Insights into the modular design of kinase inhibitors and application to Abl and Axl	13
The importance of tyrosines in multimers of cyclic RGD nonapeptides: towards αvβ6-integrin targeted radiotherapeutics	13

Design, synthesis and evaluation of 2-phenylpyrimidine derivatives as novel antifungal agents targeting CYP51	13
Rutaecarpine derivatives synthesized via skeletal reorganization alleviate inflammation-associated oxidative damage by inhibiting the MAPK/NF-κB signaling pathway	13
Discovery of imidazo[1,2-b]pyridazine-containing TAK1 kinase inhibitors with excellent activities against multiple myeloma	13
Design, synthesis and anti-proliferative activity of 3-aryl-evodiamine derivatives	13
Stereochemical optimization of N,2-substituted cycloalkylamines as norepinephrine reuptake inhibitors	13
SETDB1 as a cancer target: challenges and perspectives in drug design	13
Discovery of a nasal spray steroid, tixocortol, as an inhibitor of SARS-CoV-2 main protease and viral replication	13
Recent advancements in the therapeutic approaches for Alzheimer's disease treatment: current and future perspective	13
An allosteric inhibitor targeting the STAT3 coiled-coil domain selectively suppresses proliferation of breast cancer	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
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
Geometric deep learning-guided Suzuki reaction conditions assessment for applications in medicinal chemistry	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	12
Enhanced inhibitory activity of compounds containing purine scaffolds compared to protein kinase CK2α considering crystalline water	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
Can large language models predict antimicrobial peptide activity and toxicity?	12
Synthesis, biological evaluation and computational studies of pyrazole derivatives as Mycobacterium tuberculosis CYP121A1 inhibitors	12
Recent advancements in the development of next-generation dual-targeting antibacterial agents	12
NIR-II imaging of hepatocellular carcinoma based on a humanized anti-GPC3 antibody	12
Pyridazinone-based derivatives as anticancer agents endowed with anti-microbial activity: molecular design, synthesis, and biological investigation	12
Synthesis and biological evaluation of thiosemicarbazone-based antibody–drug conjugates	12
Proximity-induced membrane protein degradation for cancer therapies	12
Scaffold hopping from indoles to indazoles yields dual MCL-1/BCL-2 inhibitors from MCL-1 selective leads	11
Development of Hsp90 C-terminal inhibitors with noviomimetics that manifest anti-proliferative activities	11
Inside front cover	11
Research progress of metal–organic framework nanozymes in bacterial sensing, detection, and treatment	11
Site-specific molecular glues for the 14-3-3/Tau pS214 protein–protein interaction via reversible covalent imine tethering	11
Anticancer potential of copper(i) complexes based on isopropyl ester derivatives of bis(pyrazol-1-yl)acetate ligands	11
Inside front cover	11
On-resin synthesis of Lanreotide epimers and studies of their structure–activity relationships	11
Contents list	11
Discovery of a potent and selective PROTAC degrader for STAT3	11
Mycobacterium tuberculosis CitA activity is modulated by cysteine oxidation and pyruvate binding	11
Progress in the discovery and development of small molecule methuosis inducers	11
Stachydrine, a pyrrole alkaloid with promising therapeutic potential against metabolic syndrome and associated organ dysfunction	11
Novel rhodanine–thiazole hybrids as potential antidiabetic agents: a structure-based drug design approach	11
Back cover	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
SLL-1A-16 suppresses proliferation and induces autophagy in non-small-cell lung cancer cells via the AKT/mTOR signaling pathway	11
Development of di-arylated 1,2,4-triazole-based derivatives as therapeutic agents against breast cancer: synthesis and biological evaluation	10
Contents list	10
Design, synthesis, and biological evaluation of novel thiazole derivatives as PI3K/mTOR dual inhibitors	10
Adjuvant strategies to tackle mcr-mediated polymyxin resistance	10
“Seasoning” antimalarial drugs' action: chloroquine bile salts as novel triple-stage antiplasmodial hits	10
Novel tetrahydropyrimidinyl-substituted benzimidazoles and benzothiazoles: synthesis, antibacterial activity, DNA interactions and ADME profiling	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	10
Design and evaluation of poly-nitrogenous adjuvants capable of potentiating antibiotics in Gram-negative bacteria	10
Target 2035 – update on the quest for a probe for every protein	10
Five years of research on 2,4-thiazolidinediones as anticancer agents: medicinal chemistry insights (2020–2024)	10
Contents list	10
Molecular understanding of the therapeutic potential of melanin inhibiting natural products	9
Distinctive roles of aquaporins and novel therapeutic opportunities against cancer	9
Development of thiazole-appended novel hydrazones as a new class of α-amylase inhibitors with anticancer assets: anin silicoandin vitroapproach	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
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
Identification of SARS-CoV-2 Mpro inhibitors through deep reinforcement learning for de novo drug design and computational chemistry approaches	9
Complexity of αvβ6-integrin targeting RGD peptide trimers: emergence of non-specific binding by synergistic interaction	9
Lysine targeting covalent inhibitors of malarial kinase PfCLK3	9
Semisynthetic blasticidin S ester derivatives show enhanced antibiotic activity	9
Rational design and in vitro testing of new urease inhibitors to prevent urinary catheter blockage	9
Inside front cover	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
Design and synthesis of cyclic lipidated peptides derived from the C-terminus of Cx43 for hemichannel inhibition and cardiac endothelium targeting	8
Outstanding Reviewers for RSC Medicinal Chemistry in 2024	8
EGFRAP: a predictive machine learning model for assessing small molecule activity against the epidermal growth factor receptor	8
Guggulsterone – a potent bioactive phytosteroid: synthesis, structural modification, and its improved bioactivities	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
Cyclometalated Complexes: Promising Metallodrugs in the Battle Against Cancer.	8
Synthesis and investigation of thieno[2,3-b]pyridines that restore activity of topotecan	8
Insights into the recent progress in the medicinal chemistry of pyranopyrimidine analogs	8
Synthesis and antiplasmodial activity of 6H,13H-pyrazino[1,2-a;4,5-a′]diindole analogues substituted with basic side chains	8
Recent developments in membrane targeting antifungal agents to mitigate antifungal resistance	8
Integrating a quinone substructure into histone deacetylase inhibitors to cope with Alzheimer's disease and cancer	8
Inhibition of DXR in the MEP pathway with lipophilic N-alkoxyaryl FR900098 analogs	8
Ribosome-targeting antibiotics and resistance via ribosomal RNA methylation	8

AlbiCDN: albumin-binding amphiphilic STING agonists augment the immune activity for cancer immunotherapy	8
Back cover	8
The synthesis and bioactivities of ROCK2 inhibitors with 1,2-dithiolan-3-yl motif	8
Novel lithocholic acid-diindolylmethane hybrids as potent sialyltransferase inhibitors targeting triple-negative breast cancer: a molecular hybridization approach	8
Introduction to the themed collection in honour of Professor Christian Leumann	8
Copper selective 8-aminoquinoline based tetradentate chelators as anticancer agents	7
Back cover	7
QSAR, structure-based pharmacophore modelling and biological evaluation of novel platelet ADP receptor (P2Y12) antagonist	7
Stereoselective synthesis and antiproliferative activity of allo-gibberic acid-based 1,3-aminoalcohol regioisomers	7
Design, synthesis and biological evaluation of novel β-caryophyllene derivatives as potential anti-cancer agents through the ROS-mediated apoptosis pathway	7
Design of chitosan-coated CeO2-doped ZnCr LDO nanocomposites for optimized azithromycin delivery: a kinetic and mechanistic perspective	7
Introduction to the themed collection on ‘Targeting RNA with small molecules’	7
Contents list	7
Design, synthesis, and biological evaluation of new arjunolic acid derivatives as anticancer agents	7
Novel pirfenidone derivatives: synthesis and biological evaluation	7
Contents list	7
The Mycobacterium tuberculosis mycothiol S-transferase is divalent metal-dependent for mycothiol binding and transfer	7
Applications of supramolecular assemblies in drug delivery and photodynamic therapy	7
Contents list	7
Design, synthesis and biological evaluation of light-driven on–off multitarget AChE and MAO-B inhibitors	7
Computer-aided discovery of triazolothiadiazoles as DYRK1A-targeted neuroprotective agents	7
Expanding the chemical space for antiviral discovery: the potential of twistenediones	7
Live cell screening to identify RNA-binding small molecule inhibitors of the pre-let-7–Lin28 RNA–protein interaction	7
Macrocyclic RGD-peptides with high selectivity for αvβ3 integrin in cancer imaging and therapy	7
Back cover	7
Synthesis of full-length homodimer αD-VxXXB that targets human α7 nicotinic acetylcholine receptors	7
Contents list	7
Correction: Minimising the payload solvent exposed hydrophobic surface area optimises the antibody–drug conjugate properties	7
Front cover	7
Design, synthesis, molecular docking and anti-proliferative activity of novel phenothiazine containing imidazo[1,2-a]pyridine derivatives against MARK4 protein	7
Polysucrose hydrogel loaded with natural molecules/extracts for multiphase-directed sustainable wound healing	7
Preventing SARS-CoV-2 infection using Fv-antibodies targeting the proprotein convertase (PPC) cleavage site	7
Front cover	7
Heterocyclic compounds as xanthine oxidase inhibitors for the management of hyperuricemia: synthetic strategies, structure–activity relationship and molecular docking studies (2018–2024)	6
Front cover	6
Front cover	6
Semisynthetic polymyxins with potent antibacterial activity and reduced kidney cell toxicity	6
Inhibition of bacterial RNA polymerase function and protein–protein interactions: a promising approach for next-generation antibacterial therapeutics	6
The era of high-quality chemical probes	6
Development of pharmacophore models for AcrB protein and the identification of potential adjuvant candidates for overcoming efflux-mediated colistin resistance	6
News from RSC Medicinal Chemistry	6
Discovery of benzoheterocyclic-substituted amide derivatives as apoptosis signal-regulating kinase 1 (ASK1) inhibitors	6
Front cover	6
NLRP3 inflammasome: structure, mechanism, drug-induced organ toxicity, therapeutic strategies, and future perspectives	6
In vitro evaluation of the immunogenic potential of gramicidin S and its photocontrolled analogues	6
Synthesis and evaluation of tetrahydropyrrolo[1,2-a]quinolin-1(2H)-ones as new tubulin polymerization inhibitors	6
Enhanced skin penetration of curcumin by a nanoemulsion-embedded oligopeptide hydrogel for psoriasis topical therapy	6
Novel benzimidazole hybrids: design, synthesis, mechanistic studies, antifungal potential and molecular dynamics	6
Contents list	6
Front cover	6
Synthesis and properties of the kojic acid dimer and its potential for the treatment of Alzheimer's disease	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
Back cover	6
Back cover	6
Benzenesulfonamide decorated dihydropyrimidin(thi)ones: carbonic anhydrase profiling and antiproliferative activity	6
Design, synthesis and in vitro evaluations of new cyclotriphosphazenes as safe drug candidates	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
Structure-guided design of a methyltransferase-like 3 (METTL3) proteolysis targeting chimera (PROTAC) incorporating an indole–nicotinamide chemotype	6
Development, biological evaluation, and molecular modelling of novel isocytosine and guanidine derivatives as BACE1 inhibitors using a fragment growing strategy	6
Design, synthesis, antimicrobial activity, stability, and mechanism of action of bioresorbable ceragenins	6
Discovery of first-in-class PROTACs targeting maternal embryonic leucine zipper kinase (MELK) for the treatment of Burkitt lymphoma	6
Modulating polybasic character of galactose-based glycosylated antitumor ether lipids for enhanced cytotoxic response	6
Analysis of the structural diversity of heterocycles amongst European medicines agency approved pharmaceuticals (2014–2023)	6
Novel benzimidazole-based pseudo-irreversible butyrylcholinesterase inhibitors with neuroprotective activity in an Alzheimer's disease mouse model	6
Design, synthesis, and evaluation of benzhydrylpiperazine-based novel dual COX-2/5-LOX inhibitors with anti-inflammatory and anti-cancer activity	6
Contents list	6
From traditional medicine to nanomedicine: potential of Ginkgo biloba extracts in treating inflammatory skin diseases	6
Expanding the structure–activity relationships of alkynyl diphenylurea scaffold as promising antibacterial agents	6
Discovery and computational studies of piperidine/piperazine-based compounds endowed with sigma receptor affinity	6
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism	6
Design, synthesis, inhibitory activity, and molecular simulations study for d-glucose-conjugated thioureas containing pyrimidine ring as multitarget inhibitors against α-amylase, α-glucosid	6
Discovery of selective, metabolically stable pyrazole-based FLT3 inhibitors for the treatment of acute myeloid leukemia	6
Asymmetric imidazole-4,5-dicarboxamide derivatives as SARS-CoV-2 main protease inhibitors: design, synthesis and biological evaluation	5
Back cover	5
Non-steroidal anti-inflammatory drugs: recent advances in the use of synthetic COX-2 inhibitors	5
Inhibition of SARS-CoV-2 3CLpro by chemically modified tyrosinase from Agaricus bisporus	5
Armeniaspirol analogues with more potent Gram-positive antibiotic activity show enhanced inhibition of the ATP-dependent proteases ClpXP and ClpYQ	5
Morpholine substituted quinazoline derivatives as anticancer agents against MCF-7, A549 and SHSY-5Y cancer cell lines and mechanistic studies	5
Chromenochalcones: a comprehensive review on developments towards a medicinal perspective	5
Photoswitchable Stat3 inhibitors: design, synthesis and anticancer activity study on 2D and 3D breast cancer cell cultures	5
Ebselen analogues with dual human neutrophil elastase (HNE) inhibitory and antiradical activity	5
Naphthylthiazoles: a class of broad-spectrum antifungals	5
A concise review on hPXR ligand-recognizing residues and structure-based strategies to alleviate hPXR transactivation risk	5
Coumarin–furo[2,3-d]pyrimidone hybrid molecules targeting human liver cancer cells: synthesis, anticancer effect, EGFR inhibition and molecular docking studies	5
Synthesis and bioactivity of psilocybin analogues containing a stable carbon–phosphorus bond	5
Identification of a novel allosteric binding site on the catalytic domain of NF-κB inducing kinase (NIK)	5
Prediction of synergistic gemcitabine-based combination treatment through a novel tumor stemness biomarker NANOG in pancreatic cancer	5
Correction: Concise synthesis and biological activity evaluation of novel pyrazinyl–aryl urea derivatives against several cancer cell lines, which can especially induce T24 apoptotic and necroptotic c	5
Covalent drugs targeting histidine – an unexploited opportunity?	5
Identification of lysosomotropism using explainable machine learning and morphological profiling cell painting data	5
Inhibition of monoamine oxidases by heterocyclic derived conjugated dienones: synthesis and in vitro and in silico investigations	5
Bicyclic Temporin L Peptide Inhibitors Targeting SARS-CoV-2 Main Protease: Design, Synthesis, In-Vitro Inhibition Efficiency and Molecular Dynamics Insights	5
Front cover	5
Discovery of pyrazolopyrimidines that selectively inhibit CSF-1R kinase by iterative design, synthesis and screening against glioblastoma cells	5