RSC Medicinal Chemistry

Article	Citations
Put a ring on it: application of small aliphatic rings in medicinal chemistry	180
Recent advances in urea- and thiourea-containing compounds: focus on innovative approaches in medicinal chemistry and organic synthesis	84
Macrocyclization strategies for cyclic peptides and peptidomimetics	78
Repurposing the HCV NS3–4A protease drug boceprevir as COVID-19 therapeutics	58
β-Lactam antibiotic targets and resistance mechanisms: from covalent inhibitors to substrates	56
Non-steroidal anti-inflammatory drugs: recent advances in the use of synthetic COX-2 inhibitors	55
Nitrile-containing pharmaceuticals: target, mechanism of action, and their SAR studies	54
Recent developments on MOF-based platforms for antibacterial therapy	54
Target 2035 – update on the quest for a probe for every protein	44
Peptidomimetic nitrile warheads as SARS-CoV-2 3CL protease inhibitors	41
Fragment-based drug discovery: opportunities for organic synthesis	39
A review of the latest research on Mpro targeting SARS-COV inhibitors	37
β-Carboline-based molecular hybrids as anticancer agents: a brief sketch	32
Aloe-emodin derived azoles as a new structural type of potential antibacterial agents: design, synthesis, and evaluation of the action on membrane, DNA, and MRSA DNA isomerase	32
Recent advances in the development of covalent inhibitors	31
Itaconate is a covalent inhibitor of the Mycobacterium tuberculosis isocitrate lyase	29
Ruthenium(ii)–arene complexes as anti-metastatic agents, and related techniques	28
Polarity-based fluorescence probes: properties and applications	28
Pyrazole-containing pharmaceuticals: target, pharmacological activity, and their SAR studies	26
Targeting the SARS-CoV-2-spike protein: from antibodies to miniproteins and peptides	25
Discovery of novel JAK2 and EGFR inhibitors from a series of thiazole-based chalcone derivatives	23
Normal breast epithelial MCF-10A cells to evaluate the safety of carbon dots	23
Medicinal chemistry updates on quinoline- and endoperoxide-based hybrids with potent antimalarial activity	23
Human carboxylesterases and fluorescent probes to image their activity in live cells	23
Covalent PROTACs: the best of both worlds?	22

Challenges and opportunities of pharmaceutical cocrystals: a focused review on non-steroidal anti-inflammatory drugs	22
Porphyromonas gingivalis: where do we stand in our battle against this oral pathogen?	21
Nanoscale, automated, high throughput synthesis and screening for the accelerated discovery of protein modifiers	21
Comprehensive overview of biased pharmacology at the opioid receptors: biased ligands and bias factors	20
Physicochemical properties and Mycobacterium tuberculosis transporters: keys to efficacious antitubercular drugs?	19
Structure guided generation of thieno[3,2-d]pyrimidin-4-amine Mycobacterium tuberculosis bd oxidase inhibitors	19
Recent advances in the discovery of potent RNA-dependent RNA-polymerase (RdRp) inhibitors targeting viruses	19
A novel compound active against SARS-CoV-2 targeting uridylate-specific endoribonuclease (NendoU/NSP15): in silico and in vitro investigations	18
Natural product-informed exploration of chemical space to enable bioactive molecular discovery	18
Chemical modulation of Kv7 potassium channels	18
Recent advancements in chromone as a privileged scaffold towards the development of small molecules for neurodegenerative therapeutics	17
The era of high-quality chemical probes	17
Collaborative virtual screening to elaborate an imidazo[1,2-a]pyridine hit series for visceral leishmaniasis	17
Selective degradation-inducing probes for studying cereblon (CRBN) biology	17
Recent advances in synthetic and medicinal chemistry of phosphotyrosine and phosphonate-based phosphotyrosine analogues	17
Structural evolution of toll-like receptor 7/8 agonists from imidazoquinolines to imidazoles	17
Design, synthesis, and antibacterial activity ofN-(trifluoromethyl)phenyl substituted pyrazole derivatives	17
Siderophore conjugates to combat antibiotic-resistant bacteria	16
Identification of LASSBio-1945 as an inhibitor of SARS-CoV-2 main protease (MPRO) through in silico screening supported by molecular docking and a fragment-based pharmacophore model	16
The tridecaptins: non-ribosomal peptides that selectively target Gram-negative bacteria	16
Advances in research on 3C-like protease (3CLpro) inhibitors against SARS-CoV-2 since 2020	15
Tumor pyruvate kinase M2 modulators: a comprehensive account of activators and inhibitors as anticancer agents	15
Covalent drugs targeting histidine – an unexploited opportunity?	15
Current leishmaniasis drug discovery	15
Analysis of physicochemical properties of protein–protein interaction modulators suggests stronger alignment with the “rule of five”	14
Thiamine analogues as inhibitors of pyruvate dehydrogenase and discovery of a thiamine analogue with non-thiamine related antiplasmodial activity	14
In vitroandin vivosigma 1 receptor imaging studies in different disease states	14
Sulfonium-based liposome-encapsulated antibiotics deliver a synergistic antibacterial activity	13
Inhibition of MARK4 by serotonin as an attractive therapeutic approach to combat Alzheimer's disease and neuroinflammation	13
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	13
Multi-target weapons: diaryl-pyrazoline thiazolidinediones simultaneously targeting VEGFR-2 and HDAC cancer hallmarks	13
Benzimidazole-1,2,3-triazole hybrid molecules: synthesis and study of their interaction with G-quadruplex DNA	13
Recent developments of imidazo[1,2-a]pyridine analogues as antituberculosis agents	13
Medicinal chemistry of the myeloid C-type lectin receptors Mincle, Langerin, and DC-SIGN	13
Recent advances in the development of AHR antagonists in immuno-oncology	13
Recent developments in the structural characterisation of the IR and IGF1R: implications for the design of IR–IGF1R hybrid receptor modulators	13
Nitriles: an attractive approach to the development of covalent inhibitors	12
Deglycase-activity oriented screening to identify DJ-1 inhibitors	12
Morpholine substituted quinazoline derivatives as anticancer agents against MCF-7, A549 and SHSY-5Y cancer cell lines and mechanistic studies	12
Formulation and clinical translation of [177Lu]Lu-trastuzumab for radioimmunotheranostics of metastatic breast cancer	12
Design, synthesis, and biological evaluation of pyrazole-linked aloe emodin derivatives as potential anticancer agents	12
Insights into the medicinal chemistry of heterocycles integrated with a pyrazolo[1,5-a]pyrimidine scaffold	12
Antibacterial activities of plant-derived xanthones	12
Prodrugs of pyrophosphates and bisphosphonates: disguising phosphorus oxyanions	12
PAC-FragmentDEL – photoactivated covalent capture of DNA-encoded fragments for hit discovery	12
Activity-based protein profiling reveals deubiquitinase and aldehyde dehydrogenase targets of a cyanopyrrolidine probe	12
A ‘click’ chemistry approach to novel entinostat (MS-275) based class I histone deacetylase proteolysis targeting chimeras	12
Design, synthesis, crystal structure and anti-plasmodial evaluation of tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine derivatives	11
An overview of the development of EED inhibitors to disable the PRC2 function	11
Pyridazinone derivatives as potential anti-inflammatory agents: synthesis and biological evaluation as PDE4 inhibitors	11

Natural-product-based fluorescent probes: recent advances and applications	11
Monobodies as tool biologics for accelerating target validation and druggable site discovery	11
Pretargeted imaging beyond the blood–brain barrier	11
Design, synthesis and anti-mycobacterial evaluation of imidazo[1,2-a]pyridine analogues	11
Investigating 3,3-diaryloxetanes as potential bioisosteres through matched molecular pair analysis	11
Discovery of sustainable drugs for Alzheimer's disease: cardanol-derived cholinesterase inhibitors with antioxidant and anti-amyloid properties	11
Optimization of brain-penetrant picolinamide derived leucine-rich repeat kinase 2 (LRRK2) inhibitors	11
Recent advances in the discovery of protein tyrosine phosphatase SHP2 inhibitors	11
Amyloid inhibition by molecular chaperones in vitro can be translated to Alzheimer's pathology in vivo	10
Amino alcohol acrylonitriles as broad spectrum and tumour selective cytotoxic agents	10
Profiling MAP kinase cysteines for targeted covalent inhibitor design	10
Proline pre-conditioning of cell monolayers increases post-thaw recovery and viability by distinct mechanisms to other osmolytes	10
Small molecule therapeutics for neuroinflammation-mediated neurodegenerative disorders	10
Synthesis and immunological evaluation ofN-acyl modified Globo H derivatives as anticancer vaccine candidates	10
CDK9 inhibitors in cancer research	10
Mechanisms and inhibitors of nicotinamide N-methyltransferase	10
SF5- and SCF3-substituted tetrahydroquinoline compounds as potent bactericidal agents against multidrug-resistant persister Gram-positive bacteria	10
The modulatory role of sulfated and non-sulfated small molecule heparan sulfate-glycomimetics in endothelial dysfunction: absolute structural clarification, molecular docking and simulated dynamics, S	10
Comprehensive analysis of commercial fragment libraries	10
Peptide directed phthalocyanine–gold nanoparticles for selective photodynamic therapy of EGFR overexpressing cancers	10
Pharmacological inhibition of NF-κB-inducing kinase (NIK) with small molecules for the treatment of human diseases	10
Phenyl bioisosteres in medicinal chemistry: discovery of novel γ-secretase modulators as a potential treatment for Alzheimer's disease	10
Discovery of FtsZ inhibitors by virtual screening as antibacterial agents and study of the inhibition mechanism	10
Discovery, affinity maturation and multimerization of small molecule ligands against human tyrosinase and tyrosinase-related protein 1	10
Design and synthesis of eugenol/isoeugenol glycoconjugates and other analogues as antifungal agents against Aspergillus fumigatus	10
Replacement of oxygen with sulfur on the furanose ring of cyclic dinucleotides enhances the immunostimulatory effect via STING activation	9
Bifunctional chelators for radiorhenium: past, present and future outlook	9
Boron-based hybrids as novel scaffolds for the development of drugs with neuroprotective properties	9
Phthalimide analogs for antimalarial drug discovery	9
VISTA inhibitors in cancer immunotherapy: a short perspective on recent progresses	9
Insights into the recent progress in the medicinal chemistry of pyranopyrimidine analogs	9
Anticancer evaluation of new organometallic ruthenium(ii) flavone complexes	9
Structure-based design of haloperidol analogues as inhibitors of acetyltransferase Eis from Mycobacterium tuberculosis to overcome kanamycin resistance	9
The role of adjuvants in overcoming antibacterial resistance due to enzymatic drug modification	9
Peptide-based positron emission tomography probes: current strategies for synthesis and radiolabelling	9
Expanding the repertoire of methanocarba nucleosides from purinergic signaling to diverse targets	9
Synthesis of low-molecular weight fucoidan derivatives and their binding abilities to SARS-CoV-2 spike proteins	9
Illuminating the norepinephrine transporter: fluorescent probes based on nisoxetine and talopram	8
NIR-II imaging of hepatocellular carcinoma based on a humanized anti-GPC3 antibody	8
4-Amino-1,8-naphthalimide–ferrocene conjugates as potential multi-targeted anticancer and fluorescent cellular imaging agents	8
Estimating the cooperativity of PROTAC-induced ternary complexes using 19F NMR displacement assay	8
It takes two to tango: synthesis of cytotoxic quinones containing two redox active centers with potential antitumor activity	8
A second generation of 1,2,4-oxadiazole derivatives with enhanced solubility for inhibition of 3-hydroxykynurenine transaminase (HKT) from Aedes aegypti	8
Using membrane perturbing small molecules to target chronic persistent infections	8
Structure–activity relationships of hydrophobic alkyl acrylamides as tissue transglutaminase inhibitors	8
Cyclisation strategies for stabilising peptides with irregular conformations	8
Molecular dynamics: a powerful tool for studying the medicinal chemistry of ion channel modulators	8
A story of peptides, lipophilicity and chromatography – back and forth in time	8
Structural rationalization of GSPT1 and IKZF1 degradation by thalidomide molecular glue derivatives	8
Covalent sortase A inhibitor ML346 prevents Staphylococcus aureus infection of Galleria mellonella	8
Identification and validation of novel microtubule suppressors with an imidazopyridine scaffold through structure-based virtual screening and docking	8
Red light active Pt(iv)–BODIPY prodrug as a mitochondria and endoplasmic reticulum targeted chemo-PDT agent	8
N-1,2,3-Triazole–isatin derivatives: anti-proliferation effects and target identification in solid tumour cell lines	8
Oxazolidinones as versatile scaffolds in medicinal chemistry	8
Synthesis and evaluation of triazole congeners of nitro-benzothiazinones potentially active against drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy	8
Irreversible inhibition of BoNT/A protease: proximity-driven reactivity contingent upon a bifunctional approach	8
Inhibition of NaV1.7: the possibility of ideal analgesics	7
Uptake mechanisms of cell-internalizing nucleic acid aptamers for applications as pharmacological agents	7
Assessment of the rules related to gaining activity against Gram-negative bacteria	7
Overview of the structure, side effects, and activity assays of l-asparaginase as a therapy drug of acute lymphoblastic leukemia	7
Fragment screening at AstraZeneca: developing the next generation biophysics fragment set	7
Pharmacokinetics and pharmacodynamics in the treatment of cutaneous leishmaniasis – challenges and opportunities	7
N-Aryl mercaptoacetamides as potential multi-target inhibitors of metallo-β-lactamases (MBLs) and the virulence factor LasB from Pseudomonas aeruginosa	7
Will the chemical probes please stand up?	7
A niclosamide–tobramycin hybrid adjuvant potentiates cefiderocol againstP. aeruginosa	7
Targeting the protease of West Nile virus	7
Advanced approaches of developing targeted covalent drugs	7
Identification of molecular glues of the SLP76/14-3-3 protein–protein interaction	7
Exploring the chemical space of 1,2,3-triazolyl triclosan analogs for discovery of new antileishmanial chemotherapeutic agents	7
New prodrugs and analogs of the phenazine 5,10-dioxide natural products iodinin and myxin promote selective cytotoxicity towards human acute myeloid leukemia cells	7
Recent applications of covalent chemistries in protein–protein interaction inhibitors	7
FLT3 inhibitors for acute myeloid leukemia: successes, defeats, and emerging paradigms	7
Synthesis and pharmacological evaluation of [18F]PBR316: a novel PET ligand targeting the translocator protein 18 kDa (TSPO) with low binding sensitivity to human single nucleotide polymorp	7
Ribosome-targeting antibiotics and resistance via ribosomal RNA methylation	7
Piperazine tethered bergenin heterocyclic hybrids: design, synthesis, anticancer activity, and molecular docking studies	7
Computational design of a cyclic peptide that inhibits the CTLA4 immune checkpoint	7
Integrating a covalent probe with ubiquicidin fragment enables effective bacterial infection imaging	7
Identification of the first structurally validated covalent ligands of the small GTPase RAB27A	7
De novo molecular drug design benchmarking	7
Synthesis and biological evaluation of a monocyclic Fc-binding antibody-recruiting molecule for cancer immunotherapy	6

Latest developments in coumarin-based anticancer agents: mechanism of action and structure–activity relationship studies	6
Design, synthesis and biological evaluation of pyrazolo[3,4-b]pyridine derivatives as TRK inhibitors	6
Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood–brain barrier permeability	6
Assessing the mechanisms of action of natural molecules/extracts for phase-directed wound healing in hydrogel scaffolds	6
Metabolically stable apelin-analogues, incorporating cyclohexylalanine and homoarginine, as potent apelin receptor activators	6
Structure–activity relationship studies on 2,5,6-trisubstituted benzimidazoles targeting Mtb-FtsZ as antitubercular agents	6
New perspectives in cancer drug development: computational advances with an eye to design	6
Modulating β-arrestin 2 recruitment at the δ- and μ-opioid receptors using peptidomimetic ligands	6
Cucurbit[8]uril-based supramolecular hydrogels for biomedical applications	6
An overview on the synthesis of carbohydrate-based molecules with biological activity related to neurodegenerative diseases	6
Evaluation of the effect of a cell penetrating peptide (TAT) towards tailoring the targeting efficacy and tumor uptake of porphyrin	6
Antibiotic administration in targeted nanoparticles protects the faecal microbiota of mice	6
Small molecule-mediated induction of endoplasmic reticulum stress in cancer cells	6
Stereoisomeric Pam2CS based TLR2 agonists: synthesis, structural modelling and activity as vaccine adjuvants	5
Novel fluorinated ring-fused chlorins as promising PDT agents against melanoma and esophagus cancer	5
Identification of 2-arylquinazolines with alkyl-polyamine motifs as potent antileishmanial agents: synthesis and biological evaluation studies	5
Silver N-heterocyclic carbene complexes are potent uncompetitive inhibitors of the papain-like protease with antiviral activity against SARS-CoV-2	5
Shifting the paradigm in treating multi-factorial diseases: polypharmacological co-inhibitors of HDAC6	5
Current status and prospects of MIL-based MOF materials for biomedicine applications	5
Expanding the scope of novel 1,2,3-triazole derivatives as new antiparasitic drug candidates	5
Studies on the affinity of 6-[(n-(cyclo)aminoalkyl)oxy]-4H-chromen-4-ones for sigma 1/2 receptors	5
Efficient selective targeting of Candida CYP51 by oxadiazole derivatives designed from plant cuminaldehyde	5
Synthesis and bioactive evaluation of N-((1-methyl-1H-indol-3-yl)methyl)-N-(3,4,5-trimethoxyphenyl)acetamide derivatives as agents for inhibiting tubulin polymerization	5
Progress in mechanistically novel treatments for schizophrenia	5
Generation of reactive oxygen species is the primary mode of action and cause of survivin suppression by sepantronium bromide (YM155)	5
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	5
Host–guest binding of tetracationic cyclophanes to photodynamic agents inhibits posttreatment phototoxicity and maintains antitumour efficacy	5
Rational design of selective inhibitors of PARP4	5
Scaffold hopping from indoles to indazoles yields dual MCL-1/BCL-2 inhibitors from MCL-1 selective leads	5
Synthesis and evaluation of pyridine-derived bedaquiline analogues containing modifications at the A-ring subunit	5
A scaffold hopping strategy to generate new aryl-2-amino pyrimidine MRSA biofilm inhibitors	5
Metabolic labelling of cancer cells with glycodendrimers stimulate immune-mediated cytotoxicity	5
Revisiting a challenging p53 binding site: a diversity-optimized HEFLib reveals diverse binding modes in T-p53C-Y220C	5
Discovery of potent nucleotide pyrophosphatase/phosphodiesterase3 (NPP3) inhibitors with ancillary carbonic anhydrase inhibition for cancer (immuno)therapy	5
2-Difluoromethylpyridine as a bioisosteric replacement of pyridine-N-oxide: the case of quorum sensing inhibitors	5
The war on hTG2: warhead optimization in small molecule human tissue transglutaminase inhibitors	5
Introducing the metacore concept for multi-target ligand design	5
The role of small molecules in cell and gene therapy	5
Antibacterial activities of anthraquinones: structure–activity relationships and action mechanisms	5
Novel irreversible peptidic inhibitors of transglutaminase 2	5
Design, synthesis and biological evaluation of combretastatin A-4 sulfamate derivatives as potential anti-cancer agents	5
The right tools for the job: the central role for next generation chemical probes and chemistry-based target deconvolution methods in phenotypic drug discovery	5