RSC Medicinal Chemistry

Papers
(The TQCC of RSC Medicinal Chemistry is 7. The table below lists those papers that are above that threshold based on CrossRef citation counts [max. 250 papers]. The publications cover those that have been published in the past four years, i.e., from 2022-08-01 to 2026-08-01.)
ArticleCitations
Expanding the chemical space of ester of quinoxaline-7-carboxylate 1,4-di- N -oxide derivatives as potential antitubercular agents125
Exploration of hydrazine-based small molecules as metal chelators for KDM4 inhibition124
Integrating computational and experimental chemical biology revealed variable anticancer activities of phosphodiesterase isoenzyme 5 inhibitors (PDE5i) in lung cancer116
Development of sulfonyl fluoride chemical probes to advance the discovery of cereblon modulators107
N -Arylsulfonamide-based adenosine analogues to target RNA cap N 7-methyltransferase nsp14 of SARS-CoV-299
The effects of bioisostere substitution on the antimicrobial and physicochemical properties of supramolecular self-associating amphiphiles97
Cytotoxicity of phosphoramidate, bis-amidate and cycloSal prodrug metabolites against tumour and normal cells93
Integrated computational screen and validation of thalidomide-based PROTACs targeting SARS-CoV-2 main protease80
Effect of mono-guanidine-like derivatives on platelet aggregation and tumour cell induced platelet aggregation78
Inside front cover77
Oxadiargyl analogs as potent inhibitors of Toxoplasma gondii protoporphyrinogen oxidase74
Recent advances of phenotypic screening strategies in the application of anti-influenza virus drug discovery73
Back cover57
Back cover51
Emerging opportunities in the rewiring of biology through proximity inducing small molecules50
Triarylphosphonium-conjugated Sn( iv )-porphyrins for antimicrobial photodynamic therapy: impact of substituents on lipophilicity, aggregation, and p47
Biocompatible glycolipid derived from bhilawanol as an antibiofilm agent and a promising platform for drug delivery47
Emerging cellular uptake mechanisms of bRo5 PROTACs41
Design, synthesis and structure–activity relationship analysis of dibenzodiazepinone derivatives against Osimertinib resistant NSCLC41
Research progress of anticancer drugs targeting CDK1240
Discovery of novel BCAT2 inhibitors: design, synthesis, in vitro evaluation, and molecular modeling studies40
New azole derivatives linked to indole/indoline moieties combined with FLC against drug-resistant Candida albicans40
Exploring the potential of tamoxifen-based copper( ii ) dichloride in breast cancer therapy39
Synthesis and biological evaluation of novel D-ring fused steroidal N (2)-substituted-1,2,3-triazoles38
Design, synthesis, in vitro and in silico evaluation of indole-based tetrazole derivatives as putative ant37
Unusual Ni⋯Ni interaction in Ni( ii ) complexes as potential inhibitors for the development of new anti-SARS-CoV-2 Omicron drugs36
Thiazole orange-carboplatin triplex-forming oligonucleotide (TFO) combination probes enhance targeted DNA crosslinking35
Targeting DNA-PK: medicinal chemistry insights into small-molecule inhibitor discovery and optimisation33
Beta-cyclodextrin formulation of a disulfide-bond disrupting agent for improved systemic exposure32
Designing halogen-free metal–phenolic imidazolium poly(ionic liquids) with multi-functional antibacterial, anti-inflammatory and cell proliferation properties for infected wounds32
4-Trifluoromethyl bithiazoles as broad-spectrum antimicrobial agents for virus-related bacterial infections or co-infections31
ATP-competitive inhibitors for cancer treatment – kinases and the world beyond31
In vivo demonstration of enhanced mRNA delivery by cyclic disulfide-containing lipid nanoparticles for facilitating endosomal escape30
Unveiling sultam in drug discovery: spotlight on the underexplored scaffold30
Design and development of sulfenylated 5-aminopyrazoles as inhibitors of acetylcholinesterase and butyrylcholinesterase: exploring the implication for Aβ 1–42 29
Light-activatable photochemically targeting chimeras (PHOTACs) enable the optical control of targeted protein degradation of HDAC628
Structure–activity relationships of fenarimol analogues with potent in vitro and in vivo activity against 28
Sirtuin 1-activating derivatives belonging to the anilinopyridine class displaying in vivo cardioprotective activities27
Cornulacin: a new isoflavone from Cornulaca monacantha and its isolation, structure elucidation and cytotoxicity through EGFR-mediated apoptosis26
Trifluoroacetic acid-mediated synthesis of xanthene constructs and their extensive anti-tuberculosis evaluation26
Design, synthesis and exploration of cyclic imides as PDE4 inhibitors in psoriasis25
Discovery of dibenzylbutane lignan LCA derivatives as potent anti-inflammatory agents25
Design, quality and validation of the EU-OPENSCREEN fragment library poised to a high-throughput screening collection25
Natural product-inspired [3 + 2] cycloaddition-based spirooxindoles as dual anticancer agents: synthesis, characterization, and biological evaluation by in vitro 25
Water-soluble cationic porphyrins with enhanced phototoxicity to cancer cell lines for G4-targeting photodynamic therapy24
Back cover24
Bioassay-guided isolation of hepatoprotective lignans from Vernonia cinerea : DeepSAT-driven structural elucidation and predictive mechanistic insights a24
Radiosynthesis of [ 18 F]brequinar for in vivo PET imaging of hDHODH for potential studies of acute my24
Inside front cover23
Design, synthesis and pharmacological evaluation of 3 H -spiro[benzofuran-2,4′-piperidine] IRAK4 inhibitors for the treatment of diffuse large B-cell lym22
Contents list22
3-Hydroxypyrimidine-2,4-dione derivatives as monkeypox virus resolvase (Mpr) inhibitors22
Research progress regarding iminosugars for glycosidase inhibition and hypoglycemic activity21
Evolution of structure-guided drug design strategies targeting mutations in codon 12 of KRAS21
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: 21
Pretargeted imaging beyond the blood–brain barrier21
The physics-AI dialogue in drug design21
Simple accessible clemastine fumarate analogues as effective antileishmanials21
Decoding the Silent Conversations: Targeting Quorum Sensing to Disarm Bacterial Pathogens in the Age of Antimicrobial Resistance21
Beyond acrylamide: a structure-guided investigation of covalent warheads in the development of CDK7 inhibitors21
Structure-based design and evaluation of tyrosinase inhibitors targeting both human and mushroom isozymes21
Recent advances from computer-aided drug design to artificial intelligence drug design21
The relationship between cancer risk and cystic fibrosis: the role of CFTR in cell growth and cancer development20
Investigating the role of cytochrome bd oxidases in the antibacterial activity of madecassic acid and derivatives thereof20
Recent insights of PROTAC developments in inflammation-mediated and autoimmune targets: a critical review20
Design, make, test, play: a game for medicinal chemistry outreach19
Prodrugs and their activation mechanisms for brain drug delivery19
Exploration of cytotoxic potential and tubulin polymerization inhibition activity of cis -stilbene-1,2,3-triazole congeners19
Design, synthesis and biological evaluation of rhein–piperazine–furanone hybrids as potential anticancer agents19
It's ok to be outnumbered – sub-stoichiometric modulation of homomeric protein complexes19
Diversely functionalized isoquinolines and their core-embedded heterocyclic frameworks: a privileged scaffold for medicinal chemistry19
Sulfone and sulfoxide-containing pharmaceuticals: targets, pharmacological properties and SAR studies18
Stereochemical optimization of N ,2-substituted cycloalkylamines as norepinephrine reuptake inhibitors18
On-resin synthesis of Lanreotide epimers and studies of their structure–activity relationships18
Geometric deep learning-guided Suzuki reaction conditions assessment for applications in medicinal chemistry18
Enhanced inhibitory activity of compounds containing purine scaffolds compared to protein kinase CK2α considering crystalline water18
The allure of targets for novel drugs17
Druggable targets for the immunopathy of Alzheimer's disease17
Discovery of imidazo[1,2- b ]pyridazine-containing TAK1 kinase inhibitors with excellent activities against multiple myeloma17
An allosteric inhibitor targeting the STAT3 coiled-coil domain selectively suppresses proliferation of breast cancer17
NMR 1 H, 19 F-based screening of the four stem-looped structure 5_SL1–SL4 located in the 5′-untran17
Harnessing carlina oxide scaffold for the management of vector-borne diseases: synthesis and structure–activity relationship17
From fragments to follow-ups: rapid hit expansion by making use of EU-OPENSCREEN resources17
Rutaecarpine derivatives synthesized via skeletal reorganization alleviate inflammation-associated oxidative damage by inhibiting the MAPK/NF-κB signalin17
Proximity-induced membrane protein degradation for cancer therapies17
Front cover17
Correction: Design and synthesis of eugenol/isoeugenol glycoconjugates and other analogues as antifungal agents against Aspergillus fumigatus17
Synthesis and biological evaluation of thiosemicarbazone-based antibody–drug conjugates17
In vitro and in vivo studies of dehydroxylated-isoquines and -isotebuquines against trypanosomatids: a preclinical drug candid17
Inhibition of transcription and antiproliferative effects in a cancer cell line using antigene oligonucleotides containing artificial nucleoside analogues16
Stachydrine, a pyrrole alkaloid with promising therapeutic potential against metabolic syndrome and associated organ dysfunction16
Developing pyrazole–oxadiazole conjugates as potent anti-tubercular agents: an in silico and in vitro appr16
Front cover16
The importance of tyrosines in multimers of cyclic RGD nonapeptides: towards αvβ6-integrin targeted radiotherapeutics16
SETDB1 as a cancer target: challenges and perspectives in drug design16
Minimising the payload solvent exposed hydrophobic surface area optimises the antibody-drug conjugate properties16
Discovery of a nasal spray steroid, tixocortol, as an inhibitor of SARS-CoV-2 main protease and viral replication16
Contents list16
Design, synthesis and anti-proliferative activity of 3-aryl-evodiamine derivatives16
Back cover16
Design, synthesis and evaluation of 2-phenylpyrimidine derivatives as novel antifungal agents targeting CYP5116
The structural requirements of 3,5-substituted oxindoles that determine selective AMPK or GSK3β inhibition16
Recent advancements in the therapeutic approaches for Alzheimer's disease treatment: current and future perspective15
Glioblastoma antitumoral activity of tetrahydroquinoline-derived triarylmethanes15
Drug repurposing of fluvastatin as a DP2 antagonist: an ensemble learning strategy with in vitro cellular functional validation15
Recent advances towards BACE1 drug discovery and therapeutics design15
Recent advancements in the development of next-generation dual-targeting antibacterial agents15
Discovery of GBA-16-24 as a highly potent, selective ATR inhibitor for the treatment of FLT3-mutated acute myeloid leukemia15
Can large language models predict antimicrobial peptide activity and toxicity?15
Development of Hsp90 C-terminal inhibitors with noviomimetics that manifest anti-proliferative activities15
Pyridazinone-based derivatives as anticancer agents endowed with anti-microbial activity: molecular design, synthesis, and biological investigation15
Synthesis of novel rapanone derivatives via organocatalytic reductive C-alkylation: biological evaluation of antioxidant properties, 15
Outstanding Reviewers for RSC Medicinal Chemistry in 202514
Hinokitiol potentiates antimicrobial activity of bismuth drugs: a combination therapy for overcoming antimicrobial resistance14
Development of di-arylated 1,2,4-triazole-based derivatives as therapeutic agents against breast cancer: synthesis and biological evaluation14
Five years of research on 2,4-thiazolidinediones as anticancer agents: medicinal chemistry insights (2020–2024)14
Technical, preclinical, and clinical developments of Fc-glycan-specific antibody–drug conjugates14
Design, synthesis and biological evaluation of benzoyl hydrazone derivatives as anticancer agents inducing ROS-associated mitochondrial apoptosis14
Contents list14
Site-specific molecular glues for the 14-3-3/Tau pS214 protein–protein interaction via reversible covalent imine tethering14
Adjuvant strategies to tackle mcr -mediated polymyxin resistance14
Novel rhodanine–thiazole hybrids as potential antidiabetic agents: a structure-based drug design approach14
Novel glycine amides, semicarbazides and fluoroallylamines as inhibitors of the amine oxidase vascular adhesion protein-1 (VAP-1)14
Quinazolinone-1,2,3-triazole-acetamide conjugates as potent α-glucosidase inhibitors: synthesis, enzyme inhibition, kinetic analysis, and molecular docking study14
Discovery of a potent and selective PROTAC degrader for STAT314
Identification of novel phenylalanine derivatives bearing a hydroxamic acid moiety as potent quorum sensing inhibitors13
Contents list13
Mycobacterium tuberculosis CitA activity is modulated by cysteine oxidation and pyruvate binding13
Inside front cover13
Extending the architecture of bolaamphiphilic disinfectants: an investigation of octenidine and isooctenidine analogs13
Synthesis and evaluation of HFIP bearing triazolo-amides as amyloid-β aggregation inhibitors and suppressors of aggregation induced neuroinflammation13
Progress in the discovery and development of small molecule methuosis inducers13
Research progress of metal–organic framework nanozymes in bacterial sensing, detection, and treatment13
Peptides as multifunctional linchpins in targeted drug conjugates13
SLL-1A-16 suppresses proliferation and induces autophagy in non-small-cell lung cancer cells via the AKT/mTOR signaling pathway13
Anticancer potential of copper( i ) complexes based on isopropyl ester derivatives of bis(pyrazol-1-yl)acetate ligands13
Discovery of novel SIRT3 inhibitors with MLLr leukemia inhibitory potency13
Design, synthesis, and biological evaluation of novel thiazole derivatives as PI3K/mTOR dual inhibitors13
“Seasoning” antimalarial drugs' action: chloroquine bile salts as novel triple-stage antiplasmodial hits13
Inside front cover13
On the history, synthesis, and medicinal use of cantharidin, LB-100, and their analogs13
Design and synthesis of novel cathepsin C inhibitors with anti-inflammatory activity12
Evaluation of ketoclomazone and its analogues as inhibitors of 1-deoxy- d -xylulose 5-phosphate synthases and other thiamine diphosphate (ThDP)-depen12
Complexity of αvβ6-integrin targeting RGD peptide trimers: emergence of non-specific binding by synergistic interaction12
Back cover12
Synthesis and pharmacological evaluation of 1,3-diaryl substituted pyrazole based (thio)urea derivatives as potent antimicrobial agents against multi-drug resistant Staphylococc12
Lysine targeting covalent inhibitors of malarial kinase Pf CLK312
Discovery and optimization of pyrrolopyrimidines as highly potent, selective and brain-penetrant LRRK2 inhibitors12
Inhibition of DXR in the MEP pathway with lipophilic N -alkoxyaryl FR900098 analogs12
Rational design and in vitro testing of new urease inhibitors to prevent urinary catheter blockage12
Inside front cover12
Bisarylthiourea comprising cycloalkyl-thiophene-3-carboxylate derivatives as potential human toll-like receptor (TLR2) agonists: design, synthesis, and structure–activity relationship enabling the swi12
Back cover12
Identification of SARS-CoV-2 Mpro inhibitors through deep reinforcement learning for de novo drug design and computational chemistry approaches12
Contents list12
Endoperoxide delivered singlet oxygen: the future of PDT, without light or oxygen12
Outstanding Reviewers for RSC Medicinal Chemistry in 202412
Back cover12
Novel lithocholic acid-diindolylmethane hybrids as potent sialyltransferase inhibitors targeting triple-negative breast cancer: a molecular hybridization approach12
Development of a nitric oxide-releasing cephalexin-based hybrid compound for enhanced antimicrobial efficacy and biofilm disruption12
Contents list12
Diversifying the triquinazine scaffold of a Janus kinase inhibitor12
Synthesis and antiplasmodial activity of 6 H ,13 H -pyrazino[1,2- a 12
AlbiCDN: albumin-binding amphiphilic STING agonists augment the immune activity for cancer immunotherapy12
Development of trisubstituted thiophene-3-arboxamide selenide derivatives as novel EGFR kinase inhibitors with cytotoxic activity12
Preventing SARS-CoV-2 infection using Fv-antibodies targeting the proprotein convertase (PPC) cleavage site11
Guggulsterone – a potent bioactive phytosteroid: synthesis, structural modification, and its improved bioactivities11
Molecular understanding of the therapeutic potential of melanin inhibiting natural products11
Fragment-based discovery of dual ligand pharmacophores for lipid-sensing transcription factors for designed polypharmacology11
Ribosome-targeting antibiotics and resistance via ribosomal RNA methylation11
Synthesis and investigation of thieno[2,3- b ]pyridines that restore activity of topotecan11
Thiazolidine-2,4-dione hybrids as dual alpha-amylase and alpha-glucosidase inhibitors: design, synthesis, in vitro and in vivo11
EGFR AP : a predictive machine learning model for assessing small molecule activity against the epidermal growth factor receptor11
Expanding the chemical space for antiviral discovery: the potential of twistenediones11
Integrating a quinone substructure into histone deacetylase inhibitors to cope with Alzheimer's disease and cancer11
Development of thiazole-appended novel hydrazones as a new class of α-amylase inhibitors with anticancer assets: an in silico and 11
Cyclometalated complexes: promising metallodrugs in the battle against cancer11
Distinctive roles of aquaporins and novel therapeutic opportunities against cancer11
Inside front cover11
Semisynthetic blasticidin S ester derivatives show enhanced antibiotic activity11
Design of chitosan-coated CeO 2 -doped ZnCr LDO nanocomposites for optimized azithromycin delivery: a kinetic and mechanistic perspective11
Recent developments in membrane targeting antifungal agents to mitigate antifungal resistance11
The synthesis and bioactivities of ROCK2 inhibitors with 1,2-dithiolan-3-yl motif11
Design, synthesis, and anti-fibrotic evaluation of novel sulfonamide-embedded 1,2,4-triazinone derivatives in TGF-β-activated hepatic stellate cells (LX-2)11
Design and synthesis of cyclic lipidated peptides derived from the C-terminus of Cx43 for hemichannel inhibition and cardiac endothelium targeting11
Correction: Minimising the payload solvent exposed hydrophobic surface area optimises the antibody–drug conjugate properties10
Polysucrose hydrogel loaded with natural molecules/extracts for multiphase-directed sustainable wound healing10
Contents list10
Design, synthesis, and biological evaluation of sulfonamide-functionalized pyridine carbothioamides as potent tubulin-targeting anticancer agents10
Contents list10
Design, synthesis and biological evaluation of novel β-caryophyllene derivatives as potential anti-cancer agents through the ROS-mediated apoptosis pathway10
Macrocyclic RGD-peptides with high selectivity for α v β 3 integrin in cancer imaging and therapy10
Recent advances in structural modifications of natural products for anti-leishmaniasis therapy (2010–2024)10
Computer-aided discovery of triazolothiadiazoles as DYRK1A-targeted neuroprotective agents10
Front cover10
Contents list10
Introduction to the themed collection on ‘Targeting RNA with small molecules’10
Front cover10
Inhibition of bacterial RNA polymerase function and protein–protein interactions: a promising approach for next-generation antibacterial therapeutics10
Design, synthesis, and biological evaluation of new arjunolic acid derivatives as anticancer agents10
Design and synthesis of quinazoline derivatives as novel JMJD3/HDAC dual-target inhibitors10
Applications of supramolecular assemblies in drug delivery and photodynamic therapy10
Design, synthesis, molecular docking and anti-proliferative activity of novel phenothiazine containing imidazo[1,2- a ]pyridine derivatives against MARK410
Live cell screening to identify RNA-binding small molecule inhibitors of the pre-let-7–Lin28 RNA–protein interaction10
Contents list10
Novel pirfenidone derivatives: synthesis and biological evaluation10
The Mycobacterium tuberculosis mycothiol S -transferase is divalent metal-dependent for mycothiol binding 10
The rise of ultrashort cationic β-peptides as promising antimicrobial therapeutics10
QSAR, structure-based pharmacophore modelling and biological evaluation of novel platelet ADP receptor (P2Y 12 ) antagonist10
Stereoselective synthesis and antiproliferative activity of allo -gibberic acid-based 1,3-aminoalcohol regioisomers10
Introduction to the themed collection in honour of Professor Christian Leumann10
Copper selective 8-aminoquinoline based tetradentate chelators as anticancer agents10
Design, synthesis, antimicrobial activity, stability, and mechanism of action of bioresorbable ceragenins9
Discovery and computational studies of piperidine/piperazine-based compounds endowed with sigma receptor affinity9
Synthesis and evaluation of tetrahydropyrrolo[1,2- a ]quinolin-1(2 H )-ones as new tubulin polymerization 9
Tanshinones target drug-resistant tuberculosis: efficacy, selectivity, and potential mechanism of action9
In vitro evaluation of the immunogenic potential of gramicidin S and its photocontrolled analogues9
Machine learning prediction of acute toxicity with in vivo experiments on tetrazole derivatives9
Discovery of novel dehydroabietylamine–pyrimidine hybrids: design, synthesis and anti-tumor evaluation9
Novel benzimidazole hybrids: design, synthesis, mechanistic studies, antifungal potential and molecular dynamics9
Heterocyclic compounds as xanthine oxidase inhibitors for the management of hyperuricemia: synthetic strategies, structure–activity relationship and molecular docking studies (2018–2024)9
Lead optimization of 5jc21 (CG13250), a quinolin-2(1 H )-one-based inhibitor of the BRD4 member of the bro9
Expanding the structure–activity relationships of alkynyl diphenylurea scaffold as promising antibacterial agents9
Synthesis and structure–activity relationship (SAR) studies of 1,2,3-triazole, amide, and ester-based benzothiazole derivatives as potential molecular probes for tau protein9
NLRP3 inflammasome: structure, mechanism, drug-induced organ toxicity, therapeutic strategies, and future perspectives9
Front cover9
Structure-guided design of a methyltransferase-like 3 (METTL3) proteolysis targeting chimera (PROTAC) incorporating an indole–nicotinamide chemotype9
Design, synthesis, inhibitory activity, and molecular simulations study for d -glucose-conjugated thioureas containing pyrimidine ring as multitarget9
Analysis of the structural diversity of heterocycles amongst European medicines agency approved pharmaceuticals (2014–2023)9
Sorafenib Analogues Exhibit Dual Colistin-Potentiating and Anti-MRSA Activity9
Modulating polybasic character of galactose-based glycosylated antitumor ether lipids for enhanced cytotoxic response9
Development, biological evaluation, and molecular modelling of novel isocytosine and guanidine derivatives as BACE1 inhibitors using a fragment growing strategy9
Identification of spirodioxolane nsP2 helicase inhibitors with antialphaviral activity9
Enhanced skin penetration of curcumin by a nanoemulsion-embedded oligopeptide hydrogel for psoriasis topical therapy9
Contents list9
Inside front cover9
Decoding the association of polycystic ovary syndrome with metabolic-associated fatty liver: insights into CK18 and LC3II/ATG7/P62 autophagy axis and adjunct therapeutics of metformin and levothyroxin9
Mannich reaction mediated derivatization of chromones and their biological evaluations as putative multipotent ligands for the treatment of Alzheimer's disease9
Screening apelin analogues and a small molecule agonist as effective cardiovascular therapeutics against reperfusion injury9
Targeting hexokinase 2 for cancer therapy: advances, limitations, and emerging opportunities in inhibitors and degraders9
Probing pyrazolo-pyrimidines as SIRT2 inhibitors via molecular modelling and biological assays9
Design, synthesis and in vitro evaluations of new cyclotriphosphazenes as safe drug candidates9
Discovery of first-in-class PROTACs targeting maternal embryonic leucine zipper kinase (MELK) for the treatment of Burkitt lymphoma9
Front cover9
Benzenesulfonamide decorated dihydropyrimidin(thi)ones: carbonic anhydrase profiling and antiproliferative activity9
Semisynthetic polymyxins with potent antibacterial activity and reduced kidney cell toxicity9
Investigation of 2,3-diaryl-1,3-thiazolidin-4-ones as promising agents for reducing lipid accumulation in liver cells through AMPK activation: synthesis, in vitro 8
Phenylthiazoles with potent & optimum selectivity toward Clostridium difficile8
Protective effects of atractylenolide III on diquat-induced hepatic injury via PI3K/AKT/mTOR pathway inhibition and autophagy enhancement in mice8
Structural insights into the activity of carbapenemases: understanding the mechanism of action of current inhibitors and informing the design of new carbapenem adjuvants8
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