European Journal of Medicinal Chemistry

Papers
(The median citation count of European Journal of Medicinal Chemistry is 5. 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 2021-05-01 to 2025-05-01.)
ArticleCitations
EGCG-like non-competitive inhibitor of DYRK1A rescues cognitive defect in a down syndrome model403
Editorial Board168
Graphical abstract contents continued165
A pro-death autophagy-based nanoplatform for enhancing antitumour efficacy with improved immune responses140
Discovery of novel dual tubulin and MMPs inhibitors for the treatment of lung cancer and overcoming drug resistance135
Exploring the modulatory influence on the antimalarial activity of amodiaquine using scaffold hybridisation with ferrocene integration134
Ligand-based design and synthesis of new trityl histamine and trityl cysteamine derivatives as SIRT2 inhibitors for cancer therapy128
A decade of USFDA-approved small molecules as anti-inflammatory agents: Recent trends and Commentaries on the “industrial” perspective125
Corrigendum to “Structure-based development of N-Arylindole derivatives as Pks13 inhibitors against Mycobacterium tuberculosis” [Europ. J. Med. Chem. 283 (2025) 117148]121
[18F]R91150: Improved radiosynthesis and in vivo evaluation as imaging probe for 5-HT2A receptors121
Contents continued118
Discovery and optimization of 4-pyrazolyl-2-aminopyrimidine derivatives as potent spleen tyrosine kinase (SYK) inhibitors114
Graphical abstract TOC107
1,2,4-Triazolo[1,5-a]pyrimidines: Efficient one-step synthesis and functionalization as influenza polymerase PA-PB1 interaction disruptors107
H2dpa derivatives containing pentadentate ligands: An acyclic adjuvant potentiates meropenem activity in vitro and in vivo against metallo-β-lactamase-producing Enterobacterales103
Identification of novel tetrahydroquinoxaline derived phenyl ureas as modulators of the hepatitis B virus nucleocapsid assembly96
Design, synthesis and biological evaluation of 1H-indazole derivatives as novel ASK1 inhibitors95
Synthesis and biological evaluation of novel pyrazole amides as potent mitochondrial complex I inhibitors90
Non-nucleoside structured compounds with antiviral activity—past 10 years (2010–2020)87
Discovery and biological evaluation of phthalazines as novel non-kinase TGFβ pathway inhibitors87
Platinum(IV) complexes as inhibitors of CD47-SIRPα axis for chemoimmunotherapy of cancer86
Design, synthesis, and biological evaluation of piperazine derivatives as pan-PPARs agonists for the treatment of liver fibrosis86
Insight on pyrimido[5,4-g]indolizine and pyrimido[4,5-c]pyrrolo[1,2-a]azepine systems as promising photosensitizers on malignant cells85
Novel 1,3,4-oxadiazole chalcogen analogues: Synthesis and cytotoxic activity85
Design and synthesis of forsythin derivatives as anti-inflammatory agents for acute lung injury84
Structure-based approaches for the design of 6-aryl-1-(3,4,5-trimethoxyphenyl)-1H-benzo[d][1,2,3]triazoles as tubulin polymerization inhibitors80
Exploration of P1 and P4 modifications of nirmatrelvir: Design, synthesis, biological evaluation, and X-ray structural studies of SARS-CoV-2 Mpro inhibitors80
Discovery of N-(5-amido-2-methylphenyl)-5-methylisoxazole-3-carboxamide as dual CSF-1R/c-Kit Inhibitors with improved stability and BBB permeability78
Cinnamic acid derivatives linked to arylpiperazines as novel potent inhibitors of tyrosinase activity and melanin synthesis77
Discovery and biological evaluation of 6-aryl-4-(3,4,5-trimethoxyphenyl)quinoline derivatives with promising antitumor activities as novel colchicine-binding site inhibitors76
Design, synthesis and biological evaluation of N-benzylaryl cinnamide derivatives as tubulin polymerization inhibitors capable of promoting YAP degradation with potent anti-gastric cancer activities76
Structure-based discovery of a 4,5-Dihydropyrazole-cored PET ligand for imaging of receptor-interacting serine/threonine-protein kinase 1 (RIPK1) in the brain76
6-Regioisomeric 5,8-quinolinediones as potent CDC25 inhibitors against colorectal cancers75
Rational drug design to explore the structure-activity relationship (SAR) of TRK inhibitors with 2,4-diaminopyrimidine scaffold74
Discovery of small molecules for autophagy-lysosome degradation of immune checkpoint proteins74
Synthesis of 8-aminomorphans with high KOR affinity74
Oleanolic acid derivatives against drug-resistant bacteria and fungi by multi-targets to avoid drug resistance73
Graphical abstract TOC72
Novel 6-hydroxybenzothiazol-2-carboxamides as potent and selective monoamine oxidase B inhibitors endowed with neuroprotective activity71
Synthesis and evaluation of 3,4,5-trisubstituted triazoles as G protein-biased kappa opioid receptor agonists71
Estrogen receptor β-targeted hypoxia-responsive near-infrared fluorescence probes for prostate cancer study68
Discovery of 3H-pyrrolo[2,3-c]quinolines with activity against Mycobacterium tuberculosis by allosteric inhibition of the glutamate-5-kinase enzyme68
Discovery of novel fluorine-containing parthenolide analogues as potential antitumor agents66
Nature-inspired new isoindole-based Passerini adducts as efficient tumor-selective apoptotic inducers via caspase-3/7 activation66
Synthesis of tropane-based σ1 receptor antagonists with antiallodynic activity65
Probing benzenesulfonamide–thiazolidinone hybrids as multitarget directed ligands for efficient control of type 2 diabetes mellitus through targeting the enzymes: α-glucosidase and carbonic anhydrase 65
Identification of novel diarylpyrimidine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against wild-type and K103N mutant viruses65
Identification of “dual-site”-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase65
Novel 3-hydroxypyridin-4(1H)-One derivatives as ferroptosis inhibitors with iron-chelating and reactive oxygen species scavenging activities and therapeutic effect in cisplatin-induced cytotoxicity64
The mechanism of UNC-51-like kinase 1 and the applications of small molecule modulators in cancer treatment64
Novel nitrogen mustard-artemisinin hybrids with potent anti-leukemia action through DNA damage and activation of GPx64
Antitumor activity and transcriptome sequencing (RNA-seq) analyses of hepatocellular carcinoma cells in response to exposure triterpene-nucleoside conjugates64
Discovery of novel fused-heterocycle-bearing diarypyrimidine derivatives as HIV-1 potent NNRTIs targeting tolerant region I for enhanced antiviral activity and resistance profile63
Synthesis of cinnamoyl tethered indoline derivatives with anti-inflammatory and antioxidant activities62
Exploration of 2-phenylquinoline-4-carboxamide linked benzene sulfonamide derivatives as isoform selective inhibitors of transmembrane human carbonic anhydrases62
Synthesis and evaluation of a new class of MIF-inhibitors in activated macrophage cells and in experimental septic shock in mice62
Synthesis, anti-allergic rhinitis evaluation and mechanism investigation of novel 1,2,4-triazole-enamides as CB1 R antagonist61
Design, synthesis and bioevaluation of PI3Kα-selective inhibitors as potential colorectal cancer drugs60
Novel pterostilbene derivatives ameliorate heart failure by reducing oxidative stress and inflammation through regulating Nrf2/NF-κB signaling pathway60
Synthesis and evaluation of (E)-4-hydroxy-3-methyl-but-2-enyl diphosphate analogs as competitive partial agonists of butyrophilin 3A159
Bestatin analogs-4-quinolinone hybrids as antileishmanial hits: Design, repurposing rational, synthesis, in vitro and in silico studies59
Rational molecular design converting fascaplysin derivatives to potent broad-spectrum inhibitors against bacterial pathogens via targeting FtsZ59
Histone deacetylases (HDACs) as the promising immunotherapeutic targets for hematologic cancer treatment58
Discovery of novel Thieno[2,3-d]imidazole derivatives as agonists of human STING for antitumor immunotherapy using systemic administration58
Design, synthesis, and biological evaluation of some 2-(3-oxo-5,6-diphenyl-1,2,4-triazin-2(3H)-yl)-N-phenylacetamide hybrids as MTDLs for Alzheimer's disease therapy58
Straightforward access to novel mitochondriotropics derived from 2-arylethanol as potent and selective antiproliferative agents56
Coumarin–benzimidazole hybrids: A review of developments in medicinal chemistry55
Monoamine oxidase inhibitors: A concise review with special emphasis on structure activity relationship studies55
Peptide inhibitors targeting Ras and Ras-associated protein–protein interactions54
Pyrazolopyrimidines as anticancer agents: A review on structural and target-based approaches54
Design and syntheses of a bimolecular STING agonist based on the covalent STING antagonist53
Engineering a biomimicking strategy for discovering nonivamide-based quorum-sensing inhibitors for controlling bacterial infection53
Design, synthesis and promising anti-tumor efficacy of novel imidazo[1,2-a]pyridine derivatives as potent autotaxin allosteric inhibitors53
Rational design, synthesis and biological evaluation of dual PARP-1/2 and TNKS1/2 inhibitors for cancer therapy53
Discovery of N-substituted sulfamoylbenzamide derivatives as novel inhibitors of STAT3 signaling pathway based on Niclosamide53
Applications of oxetanes in drug discovery and medicinal chemistry52
Palladium-mediated synthesis and biological evaluation of C-10b substituted Dihydropyrrolo[1,2-b]isoquinolines as antileishmanial agents52
An update on small molecule compounds targeting synthetic lethality for cancer therapy52
Antioxidant, anti-inflammatory and immunomodulatory roles of vitamins in COVID-19 therapy52
Anthraquinone derivatives as ADP-competitive inhibitors of liver pyruvate kinase51
Small-molecule MDM2 inhibitors in clinical trials for cancer therapy51
From tryptophan-based amides to tertiary amines: Optimization of a butyrylcholinesterase inhibitor series51
Arginine and tryptophan-rich dendritic antimicrobial peptides that disrupt membranes for bacterial infection in vivo51
Novel bifluorescent Zn(II)–cryptolepine–cyclen complexes trigger apoptosis induced by nuclear and mitochondrial DNA damage in cisplatin-resistant lung tumor cells51
Discovery of a potent, selective and cell active inhibitor of m6A demethylase ALKBH551
Discovery, structural optimization, and anti-tumor bioactivity evaluations of betulinic acid derivatives as a new type of RORγ antagonists51
Discovery of ML210-Based glutathione peroxidase 4 (GPX4) degrader inducing ferroptosis of human cancer cells50
Application of deuterium in research and development of drugs49
Inhibition of Histone Deacetylase 6 (HDAC6) as a therapeutic strategy for Alzheimer's disease: A review (2010–2020)49
Design, synthesis and in vitro evaluation of novel SARS-CoV-2 3CLpro covalent inhibitors49
The first ADC bearing the ferroptosis inducer RSL3 as a payload with conservation of the fragile electrophilic warhead49
Discovery of the novel Benzo[b]thiophene 1,1-dioxide derivatives as a potent STAT3 inhibitor against idiopathic pulmonary fibrosis49
A glycyrrhetinic acid-iridium(III) conjugate as a theranostic NIR probe for hepatocellular carcinoma with mitochondrial-targeting ability48
Antibacterial sulfonimidamide-based oligopeptides as type I signal peptidase inhibitors: Synthesis and biological evaluation48
Synthesis and biological evaluation of geniposide derivatives as inhibitors of hyperuricemia, inflammatory and fibrosis48
Synthesis and application of small molecules approved for the treatment of lymphoma48
Synthesis and antibacterial medicinal evaluation of carbothioamido hydrazonyl thiazolylquinolone with multitargeting antimicrobial potential to combat increasingly global resistance48
New β-arylchalcogeno amines with procognitive properties targeting Carbonic Anhydrases and Monoamine Oxidases48
Current trends in computer aided drug design and a highlight of drugs discovered via computational techniques: A review48
Graphical abstract TOC47
Graphical abstract TOC47
Rational design and appraisal of selective Cdc2-Like kinase 1 (Clk1) inhibitors as novel autophagy inducers for the treatment of acute liver injury (ALI)47
Immunosuppressive effects of new thiophene-based KV1.3 inhibitors47
Graphical abstract TOC47
Contents continued47
SAR and lead optimization of (Z)-5-(4-hydroxy-3-methoxybenzylidene)-3-(2-morpholinoacetyl)thiazolidine-2,4-dione as a potential multi-target antidiabetic agent46
Tandem construction of biological relevant aliphatic 5-membered N-heterocycles46
Contents continued46
Aurora kinase inhibitors as potential anticancer agents: Recent advances46
Design, synthesis, and antitumor evaluation of triazolopyridine derivatives as novel inhibitors for BRD446
Antimicrobial activity of natural and semi-synthetic carbazole alkaloids46
Discovery of novel triazine derivatives as potent retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists46
Discovery of a novel dual-target inhibitor of CDK12 and PARP1 that induces synthetic lethality for treatment of triple-negative breast cancer45
Design, synthesis and biological evaluation of new parbendazole derivatives for the treatment of HNSCC45
3-Hydroxy-pyridin-4(1H)-ones as siderophores mediated delivery of isobavachalcone enhances antibacterial activity against pathogenic Pseudomonas aeruginosa45
Exploring the potential of histone demethylase inhibition in multi-therapeutic approaches for cancer treatment45
Reversal of subtype-selectivity and function by the introduction of a para-benzamidyl substituent to N-cyclopropylmethyl nornepenthone45
Inhibitors of ABCG2-mediated multidrug resistance: Lead generation through computer-aided drug design44
Design, synthesis and biological evaluation of novel o-aminobenzamide derivatives as potential anti-gastric cancer agents in vitro and in vivo44
Synthesis and biological evaluation of tyrosine derivatives as peripheral 5HT2A receptor antagonists for nonalcoholic fatty liver disease44
Innovative C-symmetric testosterone and androstenedione dimers: Design, synthesis, biological evaluation on prostate cancer cell lines and binding study to recombinant CYP3A444
Scaffold repurposing of fendiline: Identification of potent KRAS plasma membrane localization inhibitors44
Mucormycosis: A hidden mystery of fungal infection, possible diagnosis, treatment and development of new therapeutic agents44
Microbial-derived peptides with anti-mycobacterial potential44
Water-soluble derivatives of evodiamine: Discovery of evodiamine-10-phosphate as an orally active antitumor lead compound44
Design, synthesis and bioactivity evaluation of novel evodiamine derivatives with excellent potency against gastric cancer43
Discovery of 4-(N-dithiobenzyl piperazine)-1,8-naphthalimide as a potent multi-target antitumor agent with good efficacy, limited toxicity, and low resistance43
Nonsteroidal anti-inflammatory drugs (NSAIDs) and nucleotide analog GS-441524 conjugates with potent in vivo efficacy against coronaviruses43
Synthesis and evaluation of small molecule inhibitors of LSD1 for use against MYCN-expressing neuroblastoma42
Amidoxime prodrugs convert to potent cell-active multimodal inhibitors of the dengue virus protease42
Structure-based development of potent Plasmodium falciparum M1 and M17 aminopeptidase selective and dual inhibitors via S1′-region optimisation42
Design, development and evaluation of a prodrug-type TrkA-selective inhibitor with antinociceptive effects in vivo42
Multicomponent syntheses enable the discovery of novel quisinostat-derived chemotypes as histone deacetylase inhibitors42
Discovery, enantioselective synthesis of myrtucommulone E analogues as tyrosyl-DNA phosphodiesterase 2 inhibitors and their biological activities42
Discovery and optimization of isoliquiritigenin as a death-associated protein kinase 1 inhibitor42
Briarane-type diterpenoids, the inhibitors of osteoclast formation by interrupting Keap1-Nrf2 interaction and activating Nrf2 pathway41
Monofunctional dimetallic Ru(η6-arene) complexes inhibit NOTCH1 signaling pathway and synergistically enhance anticancer effect in combination with cisplatin or vitamin C41
Design, synthesis and biological evaluation of pleuromutilin-Schiff base hybrids as potent anti-MRSA agents in vitro and in vivo41
Aporphines: A privileged scaffold in CNS drug discovery41
Structure-directed identification of pyridine-2-methylamine derivatives as MmpL3 inhibitors for use as antitubercular agents40
Synthesis, computational and experimental pharmacological studies for (thio)ether-triazine 5-HT6R ligands with noticeable action on AChE/BChE and chalcogen-dependent intrinsic activity in search for n40
Design, synthesis, and biological activity evaluation of novel HDAC3 selective inhibitors for combination with Venetoclax against acute myeloid leukemia40
Bioisosteric replacement of 1H-1,2,3-triazole with 1H-tetrazole ring enhances anti-leukemic activity of (5-benzylthiazol-2-yl)benzamides40
Synthesis and evaluation of chemical linchpins for highly selective CK2α targeting40
Targeting transthyretin in Alzheimer's disease: Drug discovery of small-molecule chaperones as disease-modifying drug candidates for Alzheimer's disease40
New broad-spectrum and potent antibacterial agents with dual-targeting mechanism: Promoting FtsZ polymerization and disrupting bacterial membranes40
Covalent fragment mapping of KRasG12C revealed novel chemotypes with in vivo potency40
Novel angiogenesis inhibitors with superoxide anion radical amplification effect: Surmounting the Achilles’ heels of angiogenesis inhibitors and photosensitizers40
Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models39
Mitochondrial targeted hierarchical drug delivery system based on HA-modified liposomes for cancer therapy39
Antibody-drug conjugates for targeted cancer therapy: Recent advances in potential payloads39
Macrocyclic-based strategy in drug design: From lab to the clinic39
Amphiphilic small molecule antimicrobials: From cationic antimicrobial peptides (CAMPs) to mechanism-related, structurally-diverse antimicrobials39
Development of fibroblast activation protein-α radiopharmaceuticals: Recent advances and perspectives39
Design and synthesis of harmiquins, harmine and chloroquine hybrids as potent antiplasmodial agents38
Benzimidazole analogues active against adult Schistosoma mansoni: SAR analyses, In vivo efficacy in mice, and preliminary mechanistic studies as potential inhibitors of hemozoin formation38
Design and synthesis of diosgenin derivatives as apoptosis inducers through mitochondria-related pathways38
Novel antimalarial 3-substituted quinolones isosteres with improved pharmacokinetic properties38
Discovery of 2-((2-methylbenzyl)thio)-6-oxo-4-(3,4,5-trimethoxyphenyl)-1,6-dihydropyrimidine-5-carbonitrile as a novel and effective bromodomain and extra-terminal (BET) inhibitor for the treatment of38
Discovery of novel diaryl substituted isoquinolin-1(2H)-one derivatives as hypoxia-inducible factor-1 signaling inhibitors for the treatment of rheumatoid arthritis37
Synthesis and evaluation of novel ebselen derivatives as urease inhibitors for combating Helicobacter pylori infections37
Design and synthesis of novel derivatives of bisepoxylignans as potent anti-inflammatory agents involves the modulation of the M1/M2 microglia phenotype via TLR4/NF-κB signaling pathway37
Graphical abstract TOC37
Graphical abstract TOC37
Structure-based discovery of potent USP28 inhibitors derived from Vismodegib37
Development of novel S-N3-DABO derivatives as potent non-nucleoside reverse transcriptase inhibitors with improved potency and selectivity37
2-Phenoxy-3, 4′-bipyridine derivatives inhibit AURKB-dependent mitotic processes by disrupting its localization37
Advancing Src kinase inhibition: From structural design to therapeutic innovation - A comprehensive review37
The journey of p38 MAP kinase inhibitors: From bench to bedside in treating inflammatory diseases36
Structure-activity relationship studies and design of a PTPN22 inhibitor with enhanced isozyme selectivity and cellular efficacy36
Editorial Board36
Design, synthesis and anticancer evaluation of novel Se-NSAID hybrid molecules: Identification of a Se-indomethacin analog as a potential therapeutic for breast cancer36
Design and synthesis of new 1,2,3-triazoles derived from eugenol and analogues with in vitro and in vivo activity against Trypanosoma cruzi36
From garden to lab: C-3 chemical modifications of tomatidine unveil broad-spectrum ATP synthase inhibitors to combat bacterial resistance36
Hydrazinecarboxamides: Comprehensive review of their anticancer, anticonvulsive, anti-inflammatory, enzyme inhibition, antioxidant and other activities36
Synthesis, design, and optimization of a potent and selective series of pyridylpiperazines as promising antimalarial agents36
Development of a next-generation endogenous OCT4 inducer and its anti-aging effect in vivo36
Design, synthesis, and biological evaluation of diphenyl ether substituted quinazolin-4-amine derivatives as potent EGFRL858R/T790M/C797S inhibitors36
Recent advances on the development of NO-releasing molecules (NORMs) for biomedical applications35
Advancement of chimeric hybrid drugs to cure malaria infection: An overview with special emphasis on endoperoxide pharmacophores35
Design, synthesis, in vitro – In vivo biological evaluation of novel thiazolopyrimidine compounds as antileishmanial agent with PTR1 inhibition35
Synthesis of 10,10′-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro35
Recent developments in antimalarial activities of 4-aminoquinoline derivatives35
Recent advances in triazoles as tyrosinase inhibitors35
Discovery of novel hybrids containing clioquinol−1-benzyl-1,2,3,6-tetrahydropyridine as multi-target-directed ligands (MTDLs) against Alzheimer's disease35
Novel neuroprotective 5,6-dihydropyrido[2′,1':2,3]imidazo[4,5-c]quinoline derivatives acting through cholinesterase inhibition and CB2 signaling modulation35
Novel dual-target FAAH and TRPV1 ligands as potential pharmacotherapeutics for pain management35
Progress of NIR-II fluorescence imaging technology applied to disease diagnosis and treatment34
Graphical abstract TOC34
Recent progress toward developing axial chirality bioactive compounds34
Discovery of novel β-carboline derivatives as selective AChE inhibitors with GSK-3β inhibitory property for the treatment of Alzheimer's disease34
An overview on Estrogen receptors signaling and its ligands in breast cancer34
Graphical abstract TOC34
A biphenyl inhibitor of eIF4E targeting an internal binding site enables the design of cell-permeable PROTAC-degraders34
Promises of anionic calix[n]arenes in life science: State of the art in 202334
Contents continued34
Synthesis and preliminary anticancer evaluation of photo-responsive prodrugs of hydroxymethylene bisphosphonate alendronate33
Graphical abstract TOC33
A pH-Dependent rhodamine fluorophore with antiproliferative activity of bladder cancer in Vitro/Vivo and apoptosis mechanism33
Editorial Board33
Development of high-affinity fluorinated ligands for cannabinoid subtype 2 receptor, and in vitro evaluation of a radioactive tracer for imaging33
Graphical abstract TOC33
Metabolism guided optimization of peptidomimetics as non-covalent proteasome inhibitors for cancer treatment33
Graphical abstract TOC33
Synthesis and evaluation of N-sulfonylpiperidine-3-carboxamide derivatives as capsid assembly modulators inhibiting HBV in vitro and in HBV-transgenic mice33
Corrigendum to “Design, synthesis, and biological evaluation of 1,6-naphthyridine-2-one derivatives as novel FGFR4 inhibitors for the treatment of colorectal cancer” [Eur. J. Med. Chem. 259 (2023) 11532
Discovery of juglone and its derivatives as potent SARS-CoV-2 main proteinase inhibitors32
Advances in the development of HIV integrase strand transfer inhibitors32
Discovery of novel polyheterocyclic neuraminidase inhibitors with 1,3,4-oxadiazole thioetheramide as core backbone32
Structure-based drug design of an inhibitor of the SARS-CoV-2 (COVID-19) main protease using free software: A tutorial for students and scientists32
An oleanic acid decorated gold nanorod for highly efficient inhibition of hemagglutinin and visible rapid detection of the influenza virus32
Discovery of a tricyclic farnesoid X receptor agonist HEC96719, a clinical candidate for treatment of non-alcoholic steatohepatitis32
Lanosterol 14α-demethylase (CYP51)/histone deacetylase (HDAC) dual inhibitors for treatment of Candida tropicalis and Cryptococcus neoformans infections32
Synthesis and biological evaluation of fluoroquinolones containing a pyridoxine derivatives moiety32
Diversity-oriented synthesis and bioactivity evaluation of N-substituted ferrocifen compounds as novel antiproliferative agents against TNBC cancer cells32
Plant-derived strategies to fight against severe acute respiratory syndrome coronavirus 231
Design, synthesis and biological evaluation of conformationnally-restricted analogues of E7010 as inhibitors of tubulin assembly (ITA) and vascular disrupting agents (VDA)31
Acyclic purine and pyrimidine nucleotide analogs as ecto-5’-nucleotidase (CD73) inhibitors31
Discovery of styrylaniline derivatives as novel alpha-synuclein aggregates ligands31
Discovery of chalcone analogues as novel NLRP3 inflammasome inhibitors with potent anti-inflammation activities31
Cathepsin C inhibitors as anti-inflammatory drug discovery: Challenges and opportunities31
Design, synthesis and anti-ovarian cancer activities of thieno[2,3-d]pyrimidine based chimeric BRD4 inhibitor/nitric oxide-donator31
An overview of RAF kinases and their inhibitors (2019–2023)31
2-Substituted quinazolines: Partial agonistic and antagonistic ligands of the constitutive androstane receptor (CAR)31
Data-oriented protein kinase drug discovery30
Design, synthesis, and biological evaluation of novel 7-substituted 10,11-methylenedioxy-camptothecin derivatives against drug-resistant small-cell lung cancer in vitro and in vivo30
Comprehensive and critical view on the anti-inflammatory and immunomodulatory role of natural phenolic antioxidants30
A novel antimicrobial peptide with broad-spectrum and exceptional stability derived from the natural peptide Brevicidine30
Structural basis for specific inhibition of salicylate synthase from Mycobacterium abscessus30
A novel Al18F-labelled NOTA-modified ubiquicidin 29-41 derivative as a bacterial infection PET imaging agent30
Discovery of 6-aryl-2-(3,4,5-trimethoxyphenyl)thiazole[3,2-b][1,2,4]triazoles as potent tubulin polymerization inhibitors30
Ring closure strategy leads to potent RIPK3 inhibitors30
Small-molecule LRRK2 inhibitors for PD therapy: Current achievements and future perspectives30
Design, synthesis, and biological evaluation of N-(3-cyano-1H-indol-5/6-yl)-6-oxo-1,6-dihydropyrimidine-4-carboxamides and 5-(6-oxo-1,6-dihydropyrimidin-2-yl)-1H-indole-3-carbonitriles as novel xanthi30
HDAC8 as a target in drug discovery: Function, structure and design30
Expanding the utilization of binding pockets proves to be effective for noncovalent small molecule inhibitors against SARS-CoV-2 Mpro30
An 19F NMR fragment-based approach for the discovery and development of BRCA2-RAD51 inhibitors to pursuit synthetic lethality in combination with PARP inhibition in pancreatic cancer30
Simultaneous inhibition of FLT3 and HDAC by novel 6-ethylpyrazine-2-Carboxamide derivatives provides therapeutic advantages in acute myelocytic leukemia30
Isoalantolactone/hydroxamic acid hybrids as potent dual STAT3/HDAC inhibitors and self-assembled nanoparticles for cancer therapy30
Recent advances in the development of inhibitors targeting KRAS-G12C and its related pathways30
Comprehensive coverage on anti-mycobacterial endeavour reported during 202229
Carbamoylation at C-8 position of natural 3-arylcoumarin scaffold for the discovery of novel PARP-1 inhibitors with potent anticancer activity29
Identification and immunological evaluation of novel TLR2 agonists through structural optimization of Diprovocim29
Discovery of 4-amino-1,6-dihydro-7H-pyrrolo[2,3-d]pyridazin-7-one derivatives as potential receptor-interacting serine/threonine-protein kinase 1 (RIPK1) inhibitors29
Insight into small-molecule inhibitors targeting extracellular nucleotide pyrophosphatase/phosphodiesterase1 for potential multiple human diseases29
Identification of a dual acting SARS-CoV-2 proteases inhibitor through in silico design and step-by-step biological characterization29
Editorial Board29
Design, synthesis and biological evaluation of biaryl amide derivatives against SARS-CoV-2 with dual-target mechanism29
Structure-based discovery of potent myosin inhibitors to guide antiparasite drug development29
Novel spiro[chromanone-2,4′-piperidine]-4-one derivatives as potential inhibitors of fatty acid synthesis in pathogens: Design, synthesis, and biological evaluation29
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