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Discovery of YK-029A, a novel mutant EGFR inhibitor targeting both T790 M and exon 20 insertion mutations, as a treatment for NSCLC

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023; 258 ()

Although traditional EGFR-TKIs have advanced the treatment landscape of NSCLC with sensitive driver mutations (del19 or L858R), some NSCLC patients wi......

Design, synthesis, and biological evaluation of a series of new anthraquinone derivatives as anti-ZIKV agents

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023; 258 ()

The major severe complications linked to Zika virus (ZIKV) cause the global public health problems, including microcephaly and other congenital abnorm......

Design, synthesis, and evaluation of novel pleuromutilin aryl acrylate derivatives as promising broad-spectrum antibiotics especially for combatting multi-drug resistant gram-negative bacteria

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023; 259 ()

The emergence of drug-resistant strains presents a grave challenge for traditional antibiotics, underscoring the exigency of exploring novel antibacte......

Vinylphosphonate-based cyclic dinucleotides enhance STING-mediated cancer immunotherapy

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023; 259 ()

Cyclic dinucleotides (CDNs) trigger the cyclic GMP-AMP synthase-stimulator of interferon genes (cGAS-STING) pathway, which plays a key role in cytosol......

Modification of osimertinib to discover new potent EGFRC797S-TK inhibitors

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023; 261 ()

The EGFRC797S mutation is a dominant mechanism of acquired resistance after the treatment of non-small cell lung cancer (NSCLC) with osimertinib in cl......

Recent progress in degradation of membrane proteins by PROTACs and alternative targeted protein degradation techniques

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023; 262 ()

Targeted protein degradation (TPD) is one of the key strategies of current targeted cancer therapy, and it can eliminate some of the root causes of ca......

p53 as a potential target for treatment of cancer: A perspective on recent advancements in small molecules with structural insights and SAR studies

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023; 247 ()

Cancer represents one of the world's biggest hazardous diseases. p53 is the uttermost researched tumour sup-pressor protein. It is commonly considered......

Design and synthesis of novel halogen rich salicylanilides as potential antileishmanial agents

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023; 246 ()

The available therapeutic treatment for leishmaniasis is inadequate and toxic due to side effects, expensive and emergence of drug resistance. Afforda......

Rationally designed donepezil-based hydroxamates modulate Sig-1R and HDAC isoforms to exert anti-glioblastoma effects

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023; 248 ()

The pursuit of activating the HDAC inhibitory template towards additional mechanisms spurred us to design dual modulators (Sig-1R agonist - HDAC inhib......

Synthesis and structure-activity relationships of N-(3-(1H-imidazol-2-yl) phenyl)-3-phenylpropionamide derivatives as a novel class of covalent inhibitors of p97/VCP ATPase

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023; 248 ()

Noncovalent inhibitors of p97 have entered clinical studies. Compared with noncovalent inhibitors, covalent inhibitors have unique advantages in maint......

Analogues of natural products yaequinolones as potential inflammatory inhibitors: Design, synthesis and biological evaluation

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023; 250 ()

Inflammation is connected with a variety of diseases and there is still a need to develop more effective and safer anti-inflammatory drugs. Herein, we......

Expanding role of CXCR2 and therapeutic potential of CXCR2 antagonists in inflammatory diseases and cancers

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023; 250 ()

C-X-C motif chemokine receptor 2 (CXCR2) is G protein-coupled receptor (GPCR) and plays important roles in various inflammatory diseases and cancers, ......

Design, synthesis, biological evaluation of urea substituted 1,2,5-oxadia-zole-3-carboximidamides as novel indoleamine 2,3-dioxygenase-1 (IDO1) inhibitors

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023; 250 ()

Indoleamine 2,3-dioxygenase-1 (IDO1) has been considered as an attractive target for oncology immunotherapy due to its immunosuppressive effects on th......

Highly potent Platinum(IV) complexes with multiple-bond ligands targeting mitochondria to overcome cisplatin resistance

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023; 250 ()

The efficacy and resistance of cisplatin-based compounds are very intractable problems at present. This study reports a series of platinum(IV) compoun......

Highly selective butyrylcholinesterase inhibitors related to Amaryllidaceae alkaloids- Design, synthesis, and biological evaluation

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023; 252 ()

Butyrylcholinesterase (BChE) is one of the most frequently implicated enzymes in the advanced stage of Alz-heimer's disease (AD). As part of our endea......

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