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Structure-based discovery of 1H-indole-2-carboxamide derivatives as potent ASK1 inhibitors for potential treatment of ulcerative colitis

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021; 211 ()

Apoptosis signal-regulating kinase 1 (ASK1), a member of the mitogen-activated protein kinase (MAPK) family, is implicated in many human diseases. Her......

Discovery and structural optimization of 3-O-beta-chacotriosyl oleanane-type triterpenoids as potent entry inhibitors of SARS-CoV-2 virus infections

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021; 215 ()

Currently, SARS-CoV-2 virus is an emerging pathogen that has posed a serious threat to public health worldwide. However, no agents have been approved ......

Design, synthesis and biological evaluation of novel FXIa inhibitors with 2-phenyl-1H-imidazole-5-carboxamide moiety as P1 fragment

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021; 220 ()

Y Factor XIa, as a blood coagulation enzyme, amplifies the generation of the last enzyme thrombin in the blood coagulation cascade. It was proved that......

Single-step fluorescent probes to detect decrotonylation activity of HDACs through intramolecular reactions

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021; 212 ()

Lysine crotonylation plays vital roles in gene transcription and cellular metabolism. Nevertheless, methods for dissecting the molecular mechanisms of......

Design, synthesis and biological evaluation of 7H-pyrrolo[2,3-d] pyrimidine derivatives containing 1,8-naphthyridine-4-one fragment

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021; 215 ()

In this study, a series of pyrrolo [2,3-d]pyrimidine derivatives containing 1,8-naphthyridine-4-one fragment were synthesized and their biological act......

Design, synthesis, biological evaluation and structure-activity relationship study of quinazolin-4(3H)-one derivatives as novel USP7 inhibitors

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021; 216 ()

Recent research has indicated that the abnormal expression of the deubiquitinase USP7 induces tumorigenesis via multiple cell pathways, and in particu......

Development of photocontrolled BRD4 PROTACs for tongue squamous cell carcinoma (TSCC)

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021; 222 ()

The catalytic properties of small-molecule proteolysis targeting chimeras (PROTACs) may lead to uncontrolled degradation. Therefore, the main disadvan......

Research progress of dual inhibitors targeting crosstalk between histone epigenetic modulators for cancer therapy

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021; 222 ()

Abnormal epigenetics is a critical hallmark of human cancers. Anticancer drug discovery directed at histone epigenetic modulators has gained impressiv......

ROS-responsive and multifunctional anti-Alzheimer prodrugs: Tacrine-ibuprofen hybrids via a phenyl boronate linker

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021; 212 ()

Current drugs available in clinic for Alzheimer's disease (AD) treatment can only alleviate disease symptoms without clearly curing or delaying the pr......

Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021; 212 ()

Inhibition of the soluble epoxide hydrolase (sEH) is a promising new therapeutic approach in the treatment of inflammation. Driven by the in-house dat......

Discovery of N-substituted sulfamoylbenzamide derivatives as novel inhibitors of STAT3 signaling pathway based on Niclosamide

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021; 218 ()

Signal transducer and activator of transcription 3 (STAT3) has been confirmed as an attractive therapeutic target for cancer therapy. Herein, we desig......

Synthesis and in vivo screening of isosteviol derivatives as new cardioprotective agents

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021; 219 ()

Isosteviol, an ent-beyerane diterpenoid, has been repeatedly reported to possess potent cardioprotective activity. With the aim of discovering new car......

First-in-class and best-in-class dendrimer nanoplatforms from concept to clinic: Lessons learned moving forward

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021; 219 ()

Research to develop active dendrimers by themselves or as nanocarriers represents a promising approach to discover new biologically active entities th......

Progress in developing MNK inhibitors

期刊: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021; 219 ()

The MNKs (mitogen-activated protein kinase-interacting protein kinases) phosphorylate eIF4E (eukaryotic initiation factor 4 E) at serine 209; eIF4E pl......

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