RSC Medicinal Chemistry

Article	Citations
Biocompatible Glycolipid derived from Bhilawanol as an Antibiofilm Agent and Promising Platform for Drug Delivery	71
Developing peptide-based fusion inhibitors as an antiviral strategy utilizing coronin 1 as a template	58
Identification of 5-amino-1,3,4-thiadiazole appended isatins as bioactive small molecules with polypharmacological activities	39
Research progress of anticancer drugs targeting CDK12	37
Fragment-based drug discovery campaigns guided by native mass spectrometry	36
Synthesis of a fluorinated pyronin that enables blue light to rapidly depolarize mitochondria	34
Back cover	27
Design, synthesis and immunological evaluation of monophosphoryl lipid A derivatives as adjuvants for a RBD-hFc based SARS-CoV-2 vaccine	26
Contents list	25
Back cover	23
Recent developments in the structural characterisation of the IR and IGF1R: implications for the design of IR–IGF1R hybrid receptor modulators	23
Contents list	20
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Contents list	20
Alkyltriphenylphosphonium turns naphthoquinoneimidazoles into potent membrane depolarizers against mycobacteria	18
Design and synthesis of atorvastatin derivatives with enhanced water solubility, hepatoselectivity and stability	18
Introduction to the antibiotic and antiviral compounds themed collection	18
Novel benzimidazole-based pseudo-irreversible butyrylcholinesterase inhibitors with neuroprotective activity in an Alzheimer's disease mouse model	16
Exploring the potential of tamoxifen-based copper(ii) dichloride in breast cancer therapy	16
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	16
Contents list	16
Synthesis and migrastatic activity of cytochalasin analogues lacking a macrocyclic moiety	16
Back cover	15
Hydantoin derivative dimers as broad-spectrum antimicrobial agents against ESKAPE pathogens with enhanced killing rate and stability	15
Synthesis of a new series of 4-pyrazolylquinolinones with apoptotic antiproliferative effects as dual EGFR/BRAFV600E inhibitors	15

Biological evaluation of novel amidino substituted coumarin-benzazole hybrids as promising therapeutic agents	14
Design, synthesis, in vitro and in silico evaluation of indole-based tetrazole derivatives as putative anti-breast cancer agents	14
Unusual Ni⋯Ni interaction in Ni(ii) complexes as potential inhibitors for the development of new anti-SARS-CoV-2 Omicron drugs	14
Design, synthesis and evaluation of the anti-breast cancer activity of 1,3-oxazolo[4,5-d]pyrimidine and 1,3-oxazolo[5,4-d]pyrimidine derivatives	13
Thiazole orange-carboplatin triplex-forming oligonucleotide (TFO) combination probes enhance targeted DNA crosslinking	13
Discovery of benzoxazole–thiazolidinone hybrids as promising antibacterial agents against Staphylococcus aureus and Enterococcus species	13
Back cover	13
Front cover	13
Contents list	13
Front cover	13
Covalent cannabinoid receptor ligands – structural insight and selectivity challenges	13
Dual FLT3/haspin kinase inhibitor based on 3H-pyrazolo[4,3-f]quinoline scaffold with activities against acute myeloid leukemia	12
Semisynthetic polymyxins with potent antibacterial activity and reduced kidney cell toxicity	12
Screening and optimization of phage display cyclic peptides against the WDR5 WBM site	12
Mitochondria-targeted biotin-conjugated BODIPYs for cancer imaging and therapy	12
Front cover	12
Development of pharmacophore models for AcrB protein and the identification of potential adjuvant candidates for overcoming efflux-mediated colistin resistance	12
Chloroacetamide fragment library screening identifies new scaffolds for covalent inhibition of the TEAD·YAP1 interaction	12
Front cover	11
Detection of intact vancomycin–arginine as the active antibacterial conjugate in E. coli by whole-cell solid-state NMR	11
Back cover	11
Development of sulfonyl fluoride chemical probes to advance the discovery of cereblon modulators	11
Front cover	11
Front cover	11
Front cover	10
Identification and analysis of small molecule inhibitors of FosB from Staphylococcus aureus	10
Inside front cover	10
Synthesis and properties of the kojic acid dimer and its potential for the treatment of Alzheimer's disease	9
Inhibition and eradication of Pseudomonas aeruginosa biofilms by secondary metabolites of Nocardiopsis lucentensis EMB25	9
Synthesis, activity and metabolic stability of propan-2-one substituted tetrazolylalkanoic acids as dual inhibitors of cytosolic phospholipase A2α and fatty acid amide hydrolase	9
Design, synthesis, and evaluation of novel ferrostatin derivatives for the prevention of HG-induced VEC ferroptosis	9
Identification of the first structurally validated covalent ligands of the small GTPase RAB27A	9
Discovery and computational studies of piperidine/piperazine-based compounds endowed with sigma receptor affinity	9
The future of chemical probes is diversity	9
Contents list	9
AiZynth impact on medicinal chemistry practice at AstraZeneca	9
Metabolic labelling of cancer cells with glycodendrimers stimulate immune-mediated cytotoxicity	9
Synthesis and biological evaluation of new naphthalimide–thiourea derivatives as potent antimicrobial agents active against multidrug-resistant Staphylococcus aureus and Mycobacterium tuberc	8
Azole-based compounds as potential anti-Acanthamoeba agents	8
Front cover	8
New azole derivatives linked to indole/indoline moieties combined with FLC against drug-resistant Candida albicans	8
Contents list	8
1,5-Disubstituted tetrazoles as PD-1/PD-L1 antagonists	8
Recent advances of phenotypic screening strategies in the application of anti-influenza virus drug discovery	8
A new class of 7-deazaguanine agents targeting autoimmune diseases: dramatic reduction of synovial fibroblast IL-6 production from human rheumatoid arthritis patients and improved performance against	8
Linker substitution influences succinimide ring hydrolysis equilibrium impacting the stability of attachment to antibody–drug conjugates	7
Recent applications of covalent chemistries in protein–protein interaction inhibitors	7
Discovery of aurones bearing two amine functionalities as SHIP2 inhibitors with insulin-sensitizing effect in rat myotubes	7
Recent advancements in the structural exploration of TGR5 agonists for diabetes treatment	7
Deuterium labeling improves the therapeutic index of 3,3′-diselenodipropionic acid as an anticancer agent: insights from redox reactions	7

N-Sulfonylphenoxazines as neuronal calcium ion channel blockers	7
Benzenesulfonamide decorated dihydropyrimidin(thi)ones: carbonic anhydrase profiling and antiproliferative activity	7
Role of heterocycles in inhibition of VEGFR-2 – a recent update (2019–2022)	7
Discovery of new tricyclic spiroindole derivatives as potent P-glycoprotein inhibitors for reversing multidrug resistance enabled by a synthetic methodology-based library	7
Synergy between the clavanins as a weapon against multidrug-resistant Enterobacter cloacae	7
Expanding the structure–activity relationships of alkynyl diphenylurea scaffold as promising antibacterial agents	7
Synthetic modification of protein surfaces to mediate induced-proximity pharmacology	7
4-Aminopyrazolopyrimidine scaffold and its deformation in the design of tyrosine and serine/threonine kinase inhibitors in medicinal chemistry	6
In vivo stability of 211At-radiopharmaceuticals: on the impact of halogen bond formation	6
N-Arylsulfonamide-based adenosine analogues to target RNA cap N7-methyltransferase nsp14 of SARS-CoV-2	6
Unveiling sultam in drug discovery: spotlight on the underexplored scaffold	6
Carbopol 940-based hydrogels loading synergistic combination of quercetin and luteolin from the herbEuphorbia humifusato promoteStaphylococcus aureusinfected wound healing	6
Chemical synthesis and immunological evaluation of cancer vaccines based on ganglioside antigens and α-galactosylceramide	6
Expanding the chemical space of ester of quinoxaline-7-carboxylate 1,4-di-N-oxide derivatives as potential antitubercular agents	6
Front cover	6
Synthesis of a celastrol derivative as a cancer stem cell inhibitor through regulation of the STAT3 pathway for treatment of ovarian cancer	6
Back cover	6
Enhanced skin penetration of curcumin by a nanoemulsion-embedded oligopeptide hydrogel for psoriasis topical therapy	6
Chemical synthetic approaches to mimic the TRAIL: promising cancer therapeutics	6
Integrating computational and experimental chemical biology revealed variable anticancer activities of phosphodiesterase isoenzyme 5 inhibitors (PDE5i) in lung cancer	6
Heterocyclic compounds as xanthine oxidase inhibitors for the management of hyperuricemia: synthetic strategies, structure–activity relationship and molecular docking studies (2018–2024)	6
Design, synthesis, and mechanistic study of 2-piperazineone-bearing peptidomimetics as novel HIV capsid modulators	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
Novel sigma 1-antagonists with cis-(+)-normetazocine scaffold: synthesis, molecular modeling, and antinociceptive effect	6
Design, synthesis, and biological evaluation of indole-modified tamoxifen relatives as potent anticancer agents	5
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism	5
Oxazolidinones as versatile scaffolds in medicinal chemistry	5
Correction: Highly potent and selective phosphatidylinositol 4-kinase IIIβ inhibitors as broad-spectrum anti-rhinoviral agents	5
FLT3 inhibitors for acute myeloid leukemia: successes, defeats, and emerging paradigms	5
Potential of covalently linked tamoxifen hybrids for cancer treatment: recent update	5
Discovery of first-in-class PROTACs targeting maternal embryonic leucine zipper kinase (MELK) for the treatment of Burkitt lymphoma	5
Design, synthesis, and structure–activity relationship studies of 6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole derivatives as necroptosis inhibitors	5
Development of benzofuran derived sulfamates as dual aromatase-steroid sulfatase inhibitors (DASIs): Design, synthesis and biological evaluation	5
The era of high-quality chemical probes	5
Pyridine based dual binding site aromatase (CYP19A1) inhibitors	5
Novel pyrazolo[3,4-d]pyrimidine derivatives: design, synthesis, anticancer evaluation, VEGFR-2 inhibition, and antiangiogenic activity	5
Structure–activity relationship study of PROTACs against hematopoietic prostaglandin D2 synthase	5
Front cover	5
4-Trifluoromethyl bithiazoles as broad-spectrum antimicrobial agents for virus-related bacterial infections or co-infections	5
Siderophore conjugates to combat antibiotic-resistant bacteria	5
Development of 2-deoxystreptamine–nucleobase conjugates for the inhibition of oncogenic miRNA production	5
Recent advances in the discovery of protein tyrosine phosphatase SHP2 inhibitors	5
Novel PROTAC probes targeting KDM3 degradation to eliminate colorectal cancer stem cells through inhibition of Wnt/β-catenin signaling	5
Pyrazole-containing pharmaceuticals: target, pharmacological activity, and their SAR studies	5
Prodrugs of pyrophosphates and bisphosphonates: disguising phosphorus oxyanions	5
Design, synthesis and anti-mycobacterial evaluation of imidazo[1,2-a]pyridine analogues	5
Mannich reaction mediated derivatization of chromones and their biological evaluations as putative multipotent ligands for the treatment of Alzheimer's disease	4
Discovery of selective LATS inhibitors via scaffold hopping: enhancing drug-likeness and kinase selectivity for potential applications in regenerative medicine	4
Contents list	4
N-Methylamide-structured SB366791 derivatives with high TRPV1 antagonistic activity: toward PET radiotracers to visualize TRPV1	4
It's ok to be outnumbered – sub-stoichiometric modulation of homomeric protein complexes	4
Identification of chalcone analogues as anti-inflammatory agents through the regulation of NF-κB and JNK activation	4
Systematic generation and analysis of counterfactuals for compound activity predictions using multi-task models	4
Back cover	4
Synthesis and anti-proliferative activity of dehydroabietinol derivatives bearing a triazole moiety	4
Design, Synthesis and Evaluation of Pyrimidinobenzylamide and Pyrimidinothiophenamide Derivatives as Inhibitors of DOT1L and Related Epigenetic Targets DNMT3a, PRMT4 and other HMTs	4
Carborane clusters increase the potency of bis-substituted cyclam derivatives againstMycobacterium tuberculosis	4
Synthesis and evaluation of tetrahydropyrrolo[1,2-a]quinolin-1(2H)-ones as new tubulin polymerization inhibitors	4
Development of PROTACs targeting estrogen receptor: an emerging technique for combating endocrine resistance	4
Anti-Schistosomal activity and ADMET properties of 1,2,5-oxadiazinane-containing compound synthesized by visible-light photoredox catalysis	4
Witches, potions, and metabolites: an overview from a medicinal perspective	4
Development of novel thiazolidine-2,4-dione derivatives as PPAR-γ agonists through design, synthesis, computational docking, MD simulation, and comprehensive in vitro and in vivo evaluat	4
Chemical tools for the Gid4 subunit of the human E3 ligase C-terminal to LisH (CTLH) degradation complex	4
Importance of photophosphatidylserine and Tim-3 in photoimmunotherapy	4
An overview of the development of EED inhibitors to disable the PRC2 function	4
Radiosynthesis of [18F]brequinar for in vivo PET imaging of hDHODH for potential studies of acute myeloid leukemia and cancers	4
Effect of mono-Guanidine-like Derivatives on Platelet Aggregation and Tumour Cell Induced Platelet Aggregation	4
A cationic amphiphilic peptide chaperone rescues Aβ42 aggregation and cytotoxicity	4
Design, synthesis, antimicrobial activity, stability, and mechanism of action of bioresorbable ceragenins	4
Dual functional therapeutics: mitigating bacterial infection and associated inflammation	4
Synthesis and anti-tumor activity of new benzofuran-based chalcone derivatives as potent VEGFR-2 inhibitors	4
Cytotoxicity of phosphoramidate, bis-amidate and cycloSal prodrug metabolites against tumour and normal cells	4
Correction: A comprehensive apoptotic assessment of niloticin in cervical cancer cells: a tirucallane-type triterpenoid from Aphanamixis polystachya (Wall.) Parker	4
Synthesis and biological evaluation of novel D-ring fused steroidal N(2)-substituted-1,2,3-triazoles	4
Front cover	4
Profiling MAP kinase cysteines for targeted covalent inhibitor design	4
Current leishmaniasis drug discovery	4
A fragment-based approach leading to the discovery of inhibitors of CK2α with a novel mechanism of action	4
Design, synthesis, and evaluation of benzhydrylpiperazine-based novel dual COX-2/5-LOX inhibitors with anti-inflammatory and anti-cancer activity	4
Structure-based virtual screening discovers novel PKMYT1 inhibitors	4

Discovery of selective, metabolically stable pyrazole-based FLT3 inhibitors for the treatment of Acute Myeloid Leukemia	4
Back cover	4
Modulating polybasic character of galactose-based glycosylated antitumor ether lipids for enhanced cytotoxic response	4
A comprehensive apoptotic assessment of niloticin in cervical cancer cells: a tirucallane-type triterpenoid from Aphanamixis polystachya (Wall.) Parker	4
Ligand-centred phenotype-driven development of potent kinase inhibitors against oesophageal cancer	3
Exploration of degrons and their ability to mediate targeted protein degradation	3
Sirtuin 1-activating derivatives belonging to the anilinopyridine class displaying in vivo cardioprotective activities	3
Evolution of 3-(4-hydroxyphenyl)indoline-2-one as a scaffold for potent and selective anticancer activity	3
Contents list	3
Novel benzenesulfonamides containing a dual triazole moiety with selective carbonic anhydrase inhibition and anticancer activity	3
Impact of multiple H/D replacements on the physicochemical properties of flurbiprofen	3
Introduction to the themed collection on antimicrobial resistance	3
Contents list	3
Small-molecule inhibitors of bacterial-producing metallo-β-lactamases: insights into their resistance mechanisms and biochemical analyses of their activities	3
Enhancing allosteric inhibition of dihydrodipicolinate synthase through the design and synthesis of novel dimeric compounds	3
Dual EGFR and telomerase inhibitory potential of new triazole tethered Schiff bases endowed with apoptosis: design, synthesis, and biological assessments	3
Design, synthesis and biological evaluation of rhein–piperazine–furanone hybrids as potential anticancer agents	3
Discovery of new dibenzodiazepine derivatives as antibacterials against intracellular bacteria	3
From traditional medicine to nanomedicine: potential of Ginkgo biloba extracts in treating inflammatory skin diseases	3
Synthesis of diversely substituted pyridin-2(1H)-ones and in vivo evaluation of their anti-allodynic effect on cutaneous inflammatory mechanical allodynia	3
Design and synthesis of coumarin-based amphoteric antimicrobials with biofilm interference and immunoregulation effects	3
Metal-free synthesis of N-fused quinazolino-quinazoline-diones as a MALAT1 RNA triple helix intercalator	3
Discovery of a novel pyrimidine derivative for treatment of acute lung injury through reducing oxidative stress and inflammatory response	3
Recent developments in antimicrobial small molecule quaternary phosphonium compounds (QPCs) – synthesis and biological insights	3
Contents list	3
Synthesis and anticancer evaluation of acetylated-lysine conjugated gemcitabine prodrugs	3
The evolution of small molecule enzyme activators	3
A silicon-containing aryl/penta-1,4-dien-3-one/amine hybrid exhibits antiproliferative effects on breast cancer cells by targeting the HSP90 C-terminus without inducing heat-shock response	3
Novel quinolinepiperazinyl-aryltetrazoles targeting the blood stage of Plasmodium falciparum	3
Front cover	3
Microtubule stabilising peptides: new paradigm towards management of neuronal disorders	3
News from RSC Medicinal Chemistry	3
Exploration of tricyclic heterocycles as core structures for RIOK2 inhibitors	3
Aptamer AS411 interacts with the KRAS promoter/hnRNP A1 complex and shows increased potency against drug-resistant lung cancer	3
Contents list	3
Second-generation piperazine derivatives as promising radiation countermeasures	3
Responsive ZIF-90 nanocomposite material: targeted delivery of 10-hydroxycamptothecine to enhance the therapeutic effect of colon cancer (HCT116) cells	3
Natural product-inspired [3 + 2] cycloaddition-based spirooxindoles as dual anticancer agents: synthesis, characterization, and biological evaluation by in vitro and in silico methods	3
Development, biological evaluation, and molecular modelling of some benzene-sulfonamide derivatives as protein tyrosine phosphatase-1B inhibitors for managing diabetes mellitus and associated metaboli	3
The Physics-AI Dialogue in Drug Design	3
Prodrugs and their activation mechanisms for brain drug delivery	3
Formulation of a fast-disintegrating drug delivery system from cyclodextrin/naproxen inclusion complex nanofibrous films	3
Pretargeted imaging beyond the blood–brain barrier	3
Overview of CFTR activators and their recent studies for dry eye disease: a review	3
Contents list	3
Back cover	3
Design, synthesis and biological evaluation of phenanthridine amide and 1,2,3-triazole analogues against Mycobacterium tuberculosis	3
Discovery of benzoheterocyclic-substituted amide derivatives as apoptosis signal-regulating kinase 1 (ASK1) inhibitors	3
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Inside front cover	3
Discovery of dibenzylbutane lignan LCA derivatives as potent anti-inflammatory agents	3
Antitubercular evaluation of dihydropyridine–triazole conjugates: design, synthesis, in vitro screening, SAR and in silico ADME predictions	3
New pyrazole–pyridazine hybrids as selective COX-2 inhibitors: design, synthesis, molecular docking, in silico studies and investigation of their anti-inflammatory potential by evaluation of TN	3
Integrating a covalent probe with ubiquicidin fragment enables effective bacterial infection imaging	3
Copper chelating cyclic peptidomimetic inhibits Aβ fibrillogenesis	2
Design and synthesis of novel 8-(azaindolyl)-benzoazepinones as potent and selective ROCK inhibitors	2
Tackling antimicrobial stewardship through synergy and antimicrobial peptides	2
Novel irreversible peptidic inhibitors of transglutaminase 2	2
New melphalan derivatives for the treatment of retinoblastoma in combination with thermotherapy	2
Exploration of cytotoxic potential and tubulin polymerization inhibition activity of cis-stilbene-1,2,3-triazole congeners	2
Diversely functionalized isoquinolines and their core-embedded heterocyclic frameworks: a privileged scaffold for medicinal chemistry	2
Back cover	2
Structure–activity relationships of valine, tert-leucine, and phenylalanine amino acid-derived synthetic cannabinoid receptor agonists related to ADB-BUTINACA, APP-BUTINACA, and ADB-P7AICA	2
Optimization of the 2-arylquinazoline-4(3H)one scaffold for a selective and potent antitrypanosomal agent: modulation of the mechanism of action through chemical functionalization	2
Trifluoroacetic acid-mediated synthesis of xanthene constructs and their extensive anti-tuberculosis evaluation	2
Identification of fragments targeting SMYD3 using highly sensitive kinetic and multiplexed biosensor-based screening	2
Hepatocyte targeting via the asialoglycoprotein receptor	2
Antibacterial activity of the structurally novel C-2 amine-substituted analogues based on quinoxaline	2
The development of thymol–isatin hybrids as broad-spectrum antibacterial agents with potent anti-MRSA activity	2
Novel indolyl 1,2,4-triazole derivatives as potential anti-proliferative agents: in silico studies, synthesis, and biological evaluation	2
Inhibition of N-type calcium ion channels by tricyclic antidepressants – experimental and theoretical justification for their use for neuropathic pain	2
Medicinal chemistry approaches to target the MNK–eIF4E axis in cancer	2
Ruthenium(ii)–arene complexes as anti-metastatic agents, and related techniques	2
Antiproliferative activity and toxicity evaluation of 1,2,3-triazole and 4-methyl coumarin hybrids in the MCF7 breast cancer cell line	2
Reactive fragments targeting carboxylate residues employing direct to biology, high-throughput chemistry	2
Biphenyl scaffold for the design of NMDA-receptor negative modulators: molecular modeling, synthesis, and biological activity	2
A ‘click’ chemistry approach to novel entinostat (MS-275) based class I histone deacetylase proteolysis targeting chimeras	2
Newly synthesized 6-substituted piperazine/phenyl-9-cyclopentyl containing purine nucleobase analogs act as potent anticancer agents and induce apoptosis via inhibiting Src in hepatocellular ca	2
Synthesis, in silico, in vitro evaluation of furanyl- and thiophenyl-3-phenyl-1H-indole-2-carbohydrazide derivatives as tubulin inhibitors and anticancer agents	2
Development of subtype-selective covalent ligands for the adenosine A2B receptor by tuning the reactive group	2
Synthesis and antifungal evaluation of new azole derivatives containing 1,2,3-triazole	2
Design, synthesis and mechanistic insights into triclosan derived dimers as potential anti-plasmodials	2
Restoring susceptibility to aminoglycosides: identifying small molecule inhibitors of enzymatic inactivation	2
Targeting host integrated stress response: lead discovery of flavonoid compounds active against coronaviruses PEDV and PDCoV	2
Antitubercular activity of 2-mercaptobenzothiazole derivatives targeting Mycobacterium tuberculosis type II NADH dehydrogenase	2
Design, quality and validation of the EU-OPENSCREEN fragment library poised to a high-throughput screening collection	2
Discovery and optimisation of pyrazolo[1,5-a]pyrimidines as aryl hydrocarbon receptor antagonists	2
Contents list	2
Efficient selective targeting of Candida CYP51 by oxadiazole derivatives designed from plant cuminaldehyde	2
Design, synthesis, and biological evaluation of novel pyrimidin-2-amine derivatives as potent PLK4 inhibitors	2
A method for estimation of plasma protein binding using diffusion ordered NMR spectroscopy (DOSY)	2
Synthetic 18F labeled biomolecules that are selective and promising for PET imaging: major advances and applications	2
Front cover	2
meso-Substituted AB3-type phenothiazinyl porphyrins and their indium and zinc complexes photosensitising properties, cytotoxicity and phototoxicity on ovarian cancer cells	2