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Virtual Screening of Chinese Medicine Small Molecule Compounds Targeting SARS-CoV-2 3CL Protease (3CL pro)

期刊: LETTERS IN DRUG DESIGN & DISCOVERY, 2021; 18 (4)

Background: The outbreak of coronavirus disease 2019 (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has attracted w......

Stachydrine Inhibits PC12 Cell Apoptosis Induced by A beta(25-35) in an In Vitro Cell Model of Neurocognitive Disorders

期刊: LETTERS IN DRUG DESIGN & DISCOVERY, 2021; 18 (5)

Background: Abnormal deposition of amyloid beta (A beta) is considered the primary cause of neurocognitive disorders (NCDs). Inhibiting cytotoxicity i......

Design, Synthesis, and Biological Evaluation of Novel Tetramethyl-pyrazine-nitrone Derivatives as Antioxidants

期刊: LETTERS IN DRUG DESIGN & DISCOVERY, 2021; 18 (5)

Background: Thrombolysis and endovascular thrombectomy are the two main therapeutic strategies for ischemic stroke in clinic. However, reperfusion inj......

Design, Synthesis and Insecticidal Activity of 3-(Ethylsulfonyl)-Pyridines Bearing Trifluoromethyl-Oxadiazole Fragment

期刊: LETTERS IN DRUG DESIGN & DISCOVERY, 2021; 18 (2)

Y Background: Oxadiazole fragment is one of the most prevalent structures in biochemicals, especially in the research of new pesticides. It is necessa......

1'-methylspiro[indoline-3,4'-piperidine] Derivatives: Design, Synthesis, Molecular Docking and Anti-tumor Activity Studies

期刊: LETTERS IN DRUG DESIGN & DISCOVERY, 2021; 18 (5)

Background: Spirocyclic indoline compounds widely exist in numerous natural products and synthetic molecules with significant biological activities. I......

Potential Inhibition of COVID-19 RNA-dependent RNA Polymerase by Hepatitis C Virus Non-nucleoside Inhibitors: An In-silico Perspective

期刊: LETTERS IN DRUG DESIGN & DISCOVERY, 2021; 18 (5)

Background: Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) is a novel member of the genus betacoronavirus in the Coronaviridae family. I......

QSAR Studies on the IC50 of a Class of Thiazolidinone/Thiazolide Based Hybrids as Antitrypanosomal Agents

期刊: LETTERS IN DRUG DESIGN & DISCOVERY, 2021; 18 (4)

Background: Trypanosomiasis is a widespread zoonotic disease and the existing drugs are not enough to prevent and treat it. Objective: This study aime......

A Novel Combinational Nanodrug Delivery System Induces Synergistic Inhibition of Lung Adenocarcinoma Cells In vitro

期刊: LETTERS IN DRUG DESIGN & DISCOVERY, 2021; 18 (1)

Background: The combination of two or more therapeutic drugs is an attractive approach to improve the treatment of experimental tumors. Leveraging nan......

Triazolylthioacetamides Confer Inhibitory Efficacy against Metallo-beta-Lactamase IMP-1

期刊: LETTERS IN DRUG DESIGN & DISCOVERY, 2021; 18 (1)

Background: The appearance of antibiotic resistance caused by metallo-beta-lactamases (M beta Ls) is a global public health threat. Developing M beta ......

New Hybrids Derived from the Natural Compound (-)-beta-Pinene and Amides or Acylthioureas as Antitumor Agents

期刊: LETTERS IN DRUG DESIGN & DISCOVERY, 2020; 17 (3)

Background: Plant-derived natural compounds have a unique molecular structure and rich biological activity, hence, they are treated as important raw m......

Lapatinib as a Dual Tyrosine Kinase Inhibitor Unexpectedly Activates Akt in MDA-MB-231 Triple-Negative Breast Cancer Cells

期刊: LETTERS IN DRUG DESIGN & DISCOVERY, 2020; 17 (8)

Background: MDA-MB-231 is a Triple-Negative Breast Cancer (TNBC) cell line, which is resistant to tyrosine kinase inhibitors, such as lapatinib. Lapat......

Drug Discovery of Acetophenone Derivatives as BRD4 Inhibitors

期刊: LETTERS IN DRUG DESIGN & DISCOVERY, 2020; 17 (3)

UBackground: The bromodomain and extra-terminal proteins (BET), in particular BRD4, has recently emerged as a potential therapeutic target for the tre......

Novel Strobilurin Derivatives Containing Carboxylate Unit as Potential Antifungal Agents

期刊: LETTERS IN DRUG DESIGN & DISCOVERY, 2020; 17 (3)

Background: Due to the extensive use of a single fungicide to control crop diseases, the increase of resistant individuals leads to control failures. ......

Synthesis of Limonin Derivatives with Improved Anti-inflammatory and Analgesic Properties

期刊: LETTERS IN DRUG DESIGN & DISCOVERY, 2020; 17 (3)

Background: Limonoids represent an important class of natural products which possess a broad range of biological activities. Albeit their enormous pot......

The Design and Synthesis of Novel Phenothiazine Derivatives as Potential Cytotoxic Agents

期刊: LETTERS IN DRUG DESIGN & DISCOVERY, 2020; 17 (1)

Background: Cancer incidence and mortality have been increasing and cancer is still the leading cause of death all over the world. Despite the enormou......

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