Annulated pyrazole derivatives as a novel class of urokinase (uPA) inhibitors: Green synthesis, anticancer activity, DNA-damage evaluation, and molecular modelling study
| Autor: | Paula S. Farag, Asmaa M. AboulMagd, Magdy M. Hemdan, Aya I. Hassaballah |
|---|---|
| Rok vydání: | 2023 |
| Předmět: |
Molecular Structure
Dose-Response Relationship Drug Organic Chemistry Antineoplastic Agents DNA Urokinase-Type Plasminogen Activator Biochemistry Molecular Docking Simulation Structure-Activity Relationship Cell Line Tumor Drug Discovery Humans Pyrazoles Drug Screening Assays Antitumor Molecular Biology Cell Proliferation |
| Zdroj: | Bioorganic Chemistry. 130:106231 |
| ISSN: | 0045-2068 |
| DOI: | 10.1016/j.bioorg.2022.106231 |
| Popis: | Different series of annulated pyrazole derivatives were designed, synthesized via both green and traditional methods, and structurally characterized. In vitro uPA evaluation, antiproliferative activities and DNA binding damage was studied in this work. Thus, all the synthesized compounds were evaluated against three types of cancer cell lines; HepG-2, HCT-116, and MCF-7 cancer cell lines in addition to normal cell line WI38. Compounds 11, 20, 21, 23 and 24 displayed the most significant antiproliferative activity with IC |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect