RSC Medicinal Chemistry

Article	Citations
Donepezil-based rational design of N-substituted quinazolinthioacetamide candidates as potential acetylcholine esterase inhibitors for the treatment of Alzheimer's disease: in vitro and	98
Design, synthesis and in vitro evaluations of new cyclotriphosphazenes as safe drug candidates	62
Effect of mono-guanidine-like derivatives on platelet aggregation and tumour cell induced platelet aggregation	58
Oxazole and isoxazole-containing pharmaceuticals: targets, pharmacological activities, and their SAR studies	52
Structural insights, regulation, and recent advances of RAS inhibitors in the MAPK signaling cascade: a medicinal chemistry perspective	49
Design, synthesis and evaluation of pyrimidinobenzylamide and pyrimidinothiophenamide derivatives as inhibitors of DOT1L and related epigenetic targets DNMT3a, PRMT4 and other HMTs	46
Development of PROTACs targeting estrogen receptor: an emerging technique for combating endocrine resistance	40
Potential of covalently linked tamoxifen hybrids for cancer treatment: recent update	40
Design, synthesis, antimicrobial activity, stability, and mechanism of action of bioresorbable ceragenins	38
Biocompatible glycolipid derived from bhilawanol as an antibiofilm agent and a promising platform for drug delivery	31
Development of benzofuran-derived sulfamates as dual aromatase-steroid sulfatase inhibitors (DASIs): design, synthesis and biological evaluation	31
AiZynth impact on medicinal chemistry practice at AstraZeneca	31
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Contents list	29
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Introduction to the antibiotic and antiviral compounds themed collection	24
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Novel pyrazolo[3,4-d]pyrimidine derivatives: design, synthesis, anticancer evaluation, VEGFR-2 inhibition, and antiangiogenic activity	21
New azole derivatives linked to indole/indoline moieties combined with FLC against drug-resistant Candida albicans	21
Synthesis and migrastatic activity of cytochalasin analogues lacking a macrocyclic moiety	20
Front cover	19

Design, synthesis and anti-mycobacterial evaluation of imidazo[1,2-a]pyridine analogues	19
Identification of 5-amino-1,3,4-thiadiazole appended isatins as bioactive small molecules with polypharmacological activities	19
Design, synthesis, inhibitory activity, and molecular simulations study for d-glucose-conjugated thioureas containing pyrimidine ring as multitarget inhibitors against α-amylase, α-glucosid	19
Enhanced skin penetration of curcumin by a nanoemulsion-embedded oligopeptide hydrogel for psoriasis topical therapy	18
Contents list	18
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Front cover	17
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Design, synthesis, and mechanistic study of 2-piperazineone-bearing peptidomimetics as novel HIV capsid modulators	16
Inside front cover	16
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Exploring the potential of tamoxifen-based copper(ii) dichloride in breast cancer therapy	16
Chloroacetamide fragment library screening identifies new scaffolds for covalent inhibition of the TEAD·YAP1 interaction	15
Discovery and computational studies of piperidine/piperazine-based compounds endowed with sigma receptor affinity	15
Dual FLT3/haspin kinase inhibitor based on 3H-pyrazolo[4,3-f]quinoline scaffold with activities against acute myeloid leukemia	15
Synthesis, activity and metabolic stability of propan-2-one substituted tetrazolylalkanoic acids as dual inhibitors of cytosolic phospholipase A2α and fatty acid amide hydrolase	15
Mitochondria-targeted biotin-conjugated BODIPYs for cancer imaging and therapy	14
Screening and optimization of phage display cyclic peptides against the WDR5 WBM site	14
Discovery of benzoxazole–thiazolidinone hybrids as promising antibacterial agents against Staphylococcus aureus and Enterococcus species	14
Semisynthetic polymyxins with potent antibacterial activity and reduced kidney cell toxicity	14
Discovery of aurones bearing two amine functionalities as SHIP2 inhibitors with insulin-sensitizing effect in rat myotubes	13
Development of sulfonyl fluoride chemical probes to advance the discovery of cereblon modulators	13
Design, synthesis, and biological evaluation of indole-modified tamoxifen relatives as potent anticancer agents	13
Recent advances of phenotypic screening strategies in the application of anti-influenza virus drug discovery	13
Thiazole orange-carboplatin triplex-forming oligonucleotide (TFO) combination probes enhance targeted DNA crosslinking	13
Carbopol 940-based hydrogels loading synergistic combination of quercetin and luteolin from the herbEuphorbia humifusato promoteStaphylococcus aureusinfected wound healing	12
Design, synthesis, and evaluation of novel ferrostatin derivatives for the prevention of HG-induced VEC ferroptosis	12
Unusual Ni⋯Ni interaction in Ni(ii) complexes as potential inhibitors for the development of new anti-SARS-CoV-2 Omicron drugs	12
Development of pharmacophore models for AcrB protein and the identification of potential adjuvant candidates for overcoming efflux-mediated colistin resistance	12
Role of heterocycles in inhibition of VEGFR-2 – a recent update (2019–2022)	12
N-Arylsulfonamide-based adenosine analogues to target RNA cap N7-methyltransferase nsp14 of SARS-CoV-2	12
In vivo stability of 211At-radiopharmaceuticals: on the impact of halogen bond formation	12
1,5-Disubstituted tetrazoles as PD-1/PD-L1 antagonists	12
Heterocyclic compounds as xanthine oxidase inhibitors for the management of hyperuricemia: synthetic strategies, structure–activity relationship and molecular docking studies (2018–2024)	11
Recent applications of covalent chemistries in protein–protein interaction inhibitors	11
Prodrugs of pyrophosphates and bisphosphonates: disguising phosphorus oxyanions	11
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	11
Cytotoxicity of phosphoramidate, bis-amidate and cycloSal prodrug metabolites against tumour and normal cells	11
Novel benzimidazole-based pseudo-irreversible butyrylcholinesterase inhibitors with neuroprotective activity in an Alzheimer's disease mouse model	11
Azole-based compounds as potential anti-Acanthamoeba agents	11
Deuterium labeling improves the therapeutic index of 3,3′-diselenodipropionic acid as an anticancer agent: insights from redox reactions	11
4-Aminopyrazolopyrimidine scaffold and its deformation in the design of tyrosine and serine/threonine kinase inhibitors in medicinal chemistry	11
Alkyltriphenylphosphonium turns naphthoquinoneimidazoles into potent membrane depolarizers against mycobacteria	10
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	10
The future of chemical probes is diversity	10

Design and synthesis of atorvastatin derivatives with enhanced water solubility, hepatoselectivity and stability	10
Design, synthesis and immunological evaluation of monophosphoryl lipid A derivatives as adjuvants for a RBD-hFc based SARS-CoV-2 vaccine	10
Synthesis and properties of the kojic acid dimer and its potential for the treatment of Alzheimer's disease	10
Structure–activity relationship study of PROTACs against hematopoietic prostaglandin D2 synthase	10
Covalent cannabinoid receptor ligands – structural insight and selectivity challenges	10
Pyridine based dual binding site aromatase (CYP19A1) inhibitors	10
Biological evaluation of novel amidino substituted coumarin-benzazole hybrids as promising therapeutic agents	9
Expanding the structure–activity relationships of alkynyl diphenylurea scaffold as promising antibacterial agents	9
Synthesis and biological evaluation of new naphthalimide–thiourea derivatives as potent antimicrobial agents active against multidrug-resistant Staphylococcus aureus and Mycobacterium tuberc	9
Discovery of first-in-class PROTACs targeting maternal embryonic leucine zipper kinase (MELK) for the treatment of Burkitt lymphoma	9
Chemical synthetic approaches to mimic the TRAIL: promising cancer therapeutics	9
Synthetic modification of protein surfaces to mediate induced-proximity pharmacology	9
Identification and analysis of small molecule inhibitors of FosB from Staphylococcus aureus	9
Research progress of anticancer drugs targeting CDK12	9
Hydantoin derivative dimers as broad-spectrum antimicrobial agents against ESKAPE pathogens with enhanced killing rate and stability	9
Expanding the chemical space of ester of quinoxaline-7-carboxylate 1,4-di-N-oxide derivatives as potential antitubercular agents	9
Synthesis of a new series of 4-pyrazolylquinolinones with apoptotic antiproliferative effects as dual EGFR/BRAFV600E inhibitors	9
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	9
Detection of intact vancomycin–arginine as the active antibacterial conjugate in E. coli by whole-cell solid-state NMR	9
Correction: Highly potent and selective phosphatidylinositol 4-kinase IIIβ inhibitors as broad-spectrum anti-rhinoviral agents	9
Synergy between the clavanins as a weapon against multidrug-resistant Enterobacter cloacae	9
Chemical synthesis and immunological evaluation of cancer vaccines based on ganglioside antigens and α-galactosylceramide	9
N-Sulfonylphenoxazines as neuronal calcium ion channel blockers	9
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism	8
Synthesis of a celastrol derivative as a cancer stem cell inhibitor through regulation of the STAT3 pathway for treatment of ovarian cancer	8
Integrating computational and experimental chemical biology revealed variable anticancer activities of phosphodiesterase isoenzyme 5 inhibitors (PDE5i) in lung cancer	8
Modulating polybasic character of galactose-based glycosylated antitumor ether lipids for enhanced cytotoxic response	8
Novel PROTAC probes targeting KDM3 degradation to eliminate colorectal cancer stem cells through inhibition of Wnt/β-catenin signaling	8
Developing peptide-based fusion inhibitors as an antiviral strategy utilizing coronin 1 as a template	8
Discovery of selective LATS inhibitors via scaffold hopping: enhancing drug-likeness and kinase selectivity for potential applications in regenerative medicine	8
Mannich reaction mediated derivatization of chromones and their biological evaluations as putative multipotent ligands for the treatment of Alzheimer's disease	8
Synthesis of a fluorinated pyronin that enables blue light to rapidly depolarize mitochondria	8
Synthesis and biological evaluation of novel D-ring fused steroidal N(2)-substituted-1,2,3-triazoles	8
A comprehensive apoptotic assessment of niloticin in cervical cancer cells: a tirucallane-type triterpenoid from Aphanamixis polystachya (Wall.) Parker	8
Anti-Schistosomal activity and ADMET properties of 1,2,5-oxadiazinane-containing compound synthesized by visible-light photoredox catalysis	8
Synthesis and evaluation of tetrahydropyrrolo[1,2-a]quinolin-1(2H)-ones as new tubulin polymerization inhibitors	8
Development of 2-deoxystreptamine–nucleobase conjugates for the inhibition of oncogenic miRNA production	8
Discovery of selective, metabolically stable pyrazole-based FLT3 inhibitors for the treatment of acute myeloid leukemia	7
Development of p300-targeting degraders with enhanced selectivity and onset of degradation	7
Inside front cover	7
Contents list	7
Novel sigma 1-antagonists with cis-(+)-normetazocine scaffold: synthesis, molecular modeling, and antinociceptive effect	7
Contents list	7
Development, biological evaluation, and molecular modelling of novel isocytosine and guanidine derivatives as BACE1 inhibitors using a fragment growing strategy	7
Membrane lipid composition directs the cellular selectivity of antimicrobial metallohelices	7
Front cover	7
Recent advancements in the structural exploration of TGR5 agonists for diabetes treatment	7
Identification of the first structurally validated covalent ligands of the small GTPase RAB27A	7
Small molecule targeted protein degradation via the UPS: venturing beyond E3 substrate receptors	7
Inhibition and eradication of Pseudomonas aeruginosa biofilms by secondary metabolites of Nocardiopsis lucentensis EMB25	7
Front cover	7
Front cover	7
Silicon incorporated tacrine: design, synthesis, and evaluation of biological and pharmacokinetic parameters	6
Design, synthesis, in vitro and in silico evaluation of indole-based tetrazole derivatives as putative anti-breast cancer agents	6
Synthesis and anti-tumor activity of new benzofuran-based chalcone derivatives as potent VEGFR-2 inhibitors	6
Recent developments in the structural characterisation of the IR and IGF1R: implications for the design of IR–IGF1R hybrid receptor modulators	6
Back cover	6
Oxazolidinones as versatile scaffolds in medicinal chemistry	6
Structure-guided design of a truncated heterobivalent chemical probe degrader of IRE1α	6
Unveiling sultam in drug discovery: spotlight on the underexplored scaffold	6
Linker substitution influences succinimide ring hydrolysis equilibrium impacting the stability of attachment to antibody–drug conjugates	6
4-Trifluoromethyl bithiazoles as broad-spectrum antimicrobial agents for virus-related bacterial infections or co-infections	6
Correction: A comprehensive apoptotic assessment of niloticin in cervical cancer cells: a tirucallane-type triterpenoid from Aphanamixis polystachya (Wall.) Parker	6
Fragment-based drug discovery campaigns guided by native mass spectrometry	6
Pyrazole-containing pharmaceuticals: target, pharmacological activity, and their SAR studies	6
Design, synthesis, and structure–activity relationship studies of 6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole derivatives as necroptosis inhibitors	6
The era of high-quality chemical probes	6
Siderophore conjugates to combat antibiotic-resistant bacteria	6
Discovery of new tricyclic spiroindole derivatives as potent P-glycoprotein inhibitors for reversing multidrug resistance enabled by a synthetic methodology-based library	6
Metabolic labelling of cancer cells with glycodendrimers stimulate immune-mediated cytotoxicity	6
Recent advances in the discovery of protein tyrosine phosphatase SHP2 inhibitors	6
FLT3 inhibitors for acute myeloid leukemia: successes, defeats, and emerging paradigms	6
Design, synthesis, and evaluation of benzhydrylpiperazine-based novel dual COX-2/5-LOX inhibitors with anti-inflammatory and anti-cancer activity	6
Benzenesulfonamide decorated dihydropyrimidin(thi)ones: carbonic anhydrase profiling and antiproliferative activity	6
Design, synthesis and biological evaluation of phenanthridine amide and 1,2,3-triazole analogues against Mycobacterium tuberculosis	5
A method for estimation of plasma protein binding using diffusion ordered NMR spectroscopy (DOSY)	5
Front cover	5
Discovery of benzoheterocyclic-substituted amide derivatives as apoptosis signal-regulating kinase 1 (ASK1) inhibitors	5
Simple accessible clemastine fumarate analogues as effective antileishmanials	5
Design, synthesis and biological evaluation of novel morpholinopyrimidine-5-carbonitrile derivatives as dual PI3K/mTOR inhibitors	5

Novel quinolinepiperazinyl-aryltetrazoles targeting the blood stage of Plasmodium falciparum	5
Sirtuin 1-activating derivatives belonging to the anilinopyridine class displaying in vivo cardioprotective activities	5
Design, Synthesis, and SAR of Antiproliferative Activity of Trioxatriangulene Derivatives	5
Enhancing allosteric inhibition of dihydrodipicolinate synthase through the design and synthesis of novel dimeric compounds	5
Impact of multiple H/D replacements on the physicochemical properties of flurbiprofen	5
Synthesis of 2-aminopropyl benzopyran derivatives as potential agents against triple-negative breast cancer	5
Repurposing of USFDA-approved drugs to identify leads for inhibition of acetylcholinesterase enzyme: a plausible utility as an anti-Alzheimer agent	5
Design, synthesis, and biological evaluation of novel pyrimidin-2-amine derivatives as potent PLK4 inhibitors	5
Structure-based virtual screening discovers novel PKMYT1 inhibitors	5
Phenylthiazoles with potent & optimum selectivity toward Clostridium difficile	5
Synthesis of diversely substituted pyridin-2(1H)-ones and in vivo evaluation of their anti-allodynic effect on cutaneous inflammatory mechanical allodynia	5
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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	5
Trifluoroacetic acid-mediated synthesis of xanthene constructs and their extensive anti-tuberculosis evaluation	5
Novel indolyl 1,2,4-triazole derivatives as potential anti-proliferative agents: in silico studies, synthesis, and biological evaluation	5
Formulation of a fast-disintegrating drug delivery system from cyclodextrin/naproxen inclusion complex nanofibrous films	5
Leveraging efficiency metrics for the optimization of CELMoDs™ as cereblon-based molecular glue degraders	5
Microtubule stabilising peptides: new paradigm towards management of neuronal disorders	5
Ruthenium(ii)–arene complexes as anti-metastatic agents, and related techniques	5
Recent developments in antimicrobial small molecule quaternary phosphonium compounds (QPCs) – synthesis and biological insights	5
Diversely functionalized isoquinolines and their core-embedded heterocyclic frameworks: a privileged scaffold for medicinal chemistry	5
Cornulacin: a new isoflavone fromCornulaca monacanthaand its isolation, structure elucidation and cytotoxicity through EGFR-mediated apoptosis	5
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	5
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	5
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Second-generation piperazine derivatives as promising radiation countermeasures	5
In vitro and in vivo ADME of heterobifunctional degraders: a tailored approach to optimize DMPK properties of PROTACs©	5
Radiosynthesis of [18F]brequinar for in vivo PET imaging of hDHODH for potential studies of acute myeloid leukemia and cancers	5
Design, synthesis and biological evaluation of rhein–piperazine–furanone hybrids as potential anticancer agents	5
Discovery of new dibenzodiazepine derivatives as antibacterials against intracellular bacteria	5
PK 11195 derivatives: exploring the influence of amide and heterocyclic substitution on A147T TSPO discrimination	5
Back cover	5
Overview of CFTR activators and their recent studies for dry eye disease: a review	5
The development of thymol–isatin hybrids as broad-spectrum antibacterial agents with potent anti-MRSA activity	5
Synthesis and anticancer evaluation of acetylated-lysine conjugated gemcitabine prodrugs	5
Discovery and optimisation of pyrazolo[1,5-a]pyrimidines as aryl hydrocarbon receptor antagonists	5
Carborane clusters increase the potency of bis-substituted cyclam derivatives againstMycobacterium tuberculosis	4
New melphalan derivatives for the treatment of retinoblastoma in combination with thermotherapy	4
Chemical tools for the Gid4 subunit of the human E3 ligase C-terminal to LisH (CTLH) degradation complex	4
Integrating a covalent probe with ubiquicidin fragment enables effective bacterial infection imaging	4
Discovery of dibenzylbutane lignan LCA derivatives as potent anti-inflammatory agents	4
Witches, potions, and metabolites: an overview from a medicinal perspective	4
Medicinal chemistry approaches to target the MNK–eIF4E axis in cancer	4
Synthesis and anticancer activity of two highly water-soluble and ionic Pt(iv) complexes as prodrugs for Pt(ii) anticancer drugs	4
Small-molecule inhibitors of bacterial-producing metallo-β-lactamases: insights into their resistance mechanisms and biochemical analyses of their activities	4
Profiling MAP kinase cysteines for targeted covalent inhibitor design	4
Novel irreversible peptidic inhibitors of transglutaminase 2	4
Antibacterial activity of the structurally novel C-2 amine-substituted analogues based on quinoxaline	4
A cationic amphiphilic peptide chaperone rescues Aβ42 aggregation and cytotoxicity	4
Ligand-centred phenotype-driven development of potent kinase inhibitors against oesophageal cancer	4
Design and synthesis of novel 8-(azaindolyl)-benzoazepinones as potent and selective ROCK inhibitors	4
Development, biological evaluation, and molecular modelling of some benzene-sulfonamide derivatives as protein tyrosine phosphatase-1B inhibitors for managing diabetes mellitus and associated metaboli	4
Synthesis and structure–activity relationship studies of N-terminal analogues of the lipopeptide antibiotics brevicidine and laterocidine	4
Antitubercular activity of 2-mercaptobenzothiazole derivatives targeting Mycobacterium tuberculosis type II NADH dehydrogenase	4
Aptamer AS411 interacts with the KRAS promoter/hnRNP A1 complex and shows increased potency against drug-resistant lung cancer	4
Development of subtype-selective covalent ligands for the adenosine A2B receptor by tuning the reactive group	4
The pan-cancer analysis of LRG1 and its potential role in kidney renal clear cell carcinoma	4
DC-derived whole cell cytokine nano-regulator for remodelling extracellular matrix and synergizing tumor immunotherapy	4
Identification of chalcone analogues as anti-inflammatory agents through the regulation of NF-κB and JNK activation	4
An overview of the development of EED inhibitors to disable the PRC2 function	4
Expanding the scope of novel 1,2,3-triazole derivatives as new antiparasitic drug candidates	4
Efficient selective targeting of Candida CYP51 by oxadiazole derivatives designed from plant cuminaldehyde	4
It's ok to be outnumbered – sub-stoichiometric modulation of homomeric protein complexes	4
meso-Substituted AB3-type phenothiazinyl porphyrins and their indium and zinc complexes photosensitising properties, cytotoxicity and phototoxicity on ovarian cancer cells	4
Exploration of cytotoxic potential and tubulin polymerization inhibition activity of cis-stilbene-1,2,3-triazole congeners	4
Natural product-inspired [3 + 2] cycloaddition-based spirooxindoles as dual anticancer agents: synthesis, characterization, and biological evaluation by in vitro and in silico methods	4
Novel curcumin-based analogues as potential VEGFR2 inhibitors with promising metallic loading nanoparticles: synthesis, biological evaluation, and molecular modelling investigation	4
N-Methylamide-structured SB366791 derivatives with high TRPV1 antagonistic activity: toward PET radiotracers to visualize TRPV1	4
A fragment-based approach leading to the discovery of inhibitors of CK2α with a novel mechanism of action	4
Systematic generation and analysis of counterfactuals for compound activity predictions using multi-task models	4
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	4
Design, quality and validation of the EU-OPENSCREEN fragment library poised to a high-throughput screening collection	4
Tackling antimicrobial stewardship through synergy and antimicrobial peptides	4
Antiproliferative activity and toxicity evaluation of 1,2,3-triazole and 4-methyl coumarin hybrids in the MCF7 breast cancer cell line	4
Evolution of 3-(4-hydroxyphenyl)indoline-2-one as a scaffold for potent and selective anticancer activity	4
Recent developments of imidazo[1,2-a]pyridine analogues as antituberculosis agents	4
Designed hybrid anticancer nuclear-localized peptide inhibits aggressive cancer cell proliferation	4
Targeted protein degradation using the lysosomal pathway	4
Hepatocyte targeting via the asialoglycoprotein receptor	4
Introduction to the themed collection on fragment-based drug discovery	4
Metal-free synthesis of N-fused quinazolino-quinazoline-diones as a MALAT1 RNA triple helix intercalator	4
Synthesis and anti-proliferative activity of dehydroabietinol derivatives bearing a triazole moiety	4
Novel benzenesulfonamides containing a dual triazole moiety with selective carbonic anhydrase inhibition and anticancer activity	4
Strong in vitro anticancer activity of copper(ii) and zinc(ii) complexes containing naturally occurring lapachol: cellular effects in ovarian A2780 cells	4