New benzothienopyrimidine derivatives as dual EGFR/ARO inhibitors: Design, synthesis, and their cytotoxic effect on MCF-7 breast cancer cell line
| Autor: | Eman A. Sobh, Nadia A. Khalil, Samar I. Faggal, Marwa S. A. Hassan |
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| Rok vydání: | 2022 |
| Předmět: |
Molecular Structure
Aromatase Inhibitors Antineoplastic Agents Breast Neoplasms Caspase 9 ErbB Receptors Molecular Docking Simulation Erlotinib Hydrochloride Structure-Activity Relationship Aromatase Cell Line Tumor Drug Discovery Letrozole MCF-7 Cells Humans Female Drug Screening Assays Antitumor Protein Kinase Inhibitors Cell Proliferation |
| Zdroj: | Drug development researchREFERENCES. 83(5) |
| ISSN: | 1098-2299 |
| Popis: | New cytotoxic agents based on benzothienopyrimidine scaffold were designed, synthesized, and evaluated against the MCF-7 breast cancer line in comparison to erlotinib and letrozole as reference drugs. Eight compounds demonstrated up to 20-fold higher anticancer activity than erlotinib, and five of these compounds were up to 11-fold more potent than letrozole in MTT assay. The most promising compounds were evaluated for their inhibitory activity against EGFR and ARO enzymes. Compound 12, which demonstrated potent dual EGFR and ARO inhibitory activity with IC |
| Databáze: | OpenAIRE |
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