Synthesis and anticancer activity of thiourea derivatives bearing a benzodioxole moiety with EGFR inhibitory activity, apoptosis assay and molecular docking study
| Autor: | Reem A. K. Al-Harbi, Marwa A.M.Sh. El-Sharief, Samir Y. Abbas |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
Thiosemicarbazones
Antineoplastic Agents Apoptosis Inhibitory postsynaptic potential 01 natural sciences 03 medical and health sciences chemistry.chemical_compound Structure-Activity Relationship Cell Line Tumor Drug Discovery Ic50 values medicine Moiety Cytotoxic T cell Humans Doxorubicin Benzodioxoles Amines Protein Kinase Inhibitors 030304 developmental biology bcl-2-Associated X Protein Pharmacology 0303 health sciences 010405 organic chemistry Chemistry Organic Chemistry Thiourea General Medicine Combinatorial chemistry 0104 chemical sciences ErbB Receptors Molecular Docking Simulation Hydrazines Proto-Oncogene Proteins c-bcl-2 Cancer cell lines Drug Screening Assays Antitumor medicine.drug |
| Zdroj: | European journal of medicinal chemistry. 198 |
| ISSN: | 1768-3254 |
| Popis: | New thiourea derivatives bearing a benzodioxole moiety were synthesized via the reaction of 5-isothiocyanatobenzodioxole with amino compounds such as aromatic amines, sulfa drugs, heterocyclic amines, hydrazines and hydrazides. The anticancer activity of the synthesized thiourea derivatives was examined against HCT116, HepG2 and MCF-7 cancer cell lines. Most of thiourea derivatives revealed significant cytotoxic effect, in some cases greater than the doxorubicin. As example, IC50 values of N1,N3-disubstituted-thiosemicarbazone 7 were 1.11, 1.74 and 7.0 μM for HCT116, HepG2 and MCF7, respectively; IC50 values of doxorubicin were 8.29, 7.46 and 4.56 μM, respectively. The anticancer mechanisms were studied via EGFR inhibition and apoptosis assessments, as well as molecular docking. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect