Synthesis, anticancer evaluation and molecular docking studies of methotrexate’s novel Schiff base derivatives against malignant glioma cell lines
| Autor: | Mohammad Amjad Kamal, Shahid Ayub, Aifa Nemat, Mudassir Iqbal, Saima Kalsoom, Ishaq N. Khan, Shoaib Ahmad Malik, Fazal Adnan |
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| Rok vydání: | 2020 |
| Předmět: |
Schiff base
Molecular Structure Glioma cell lines Antineoplastic Agents Glioma General Medicine Cell Line Molecular Docking Simulation Structure-Activity Relationship chemistry.chemical_compound Methotrexate chemistry Structural Biology medicine Cancer research Humans Cytotoxic T cell Drug Screening Assays Antitumor Molecular Biology Schiff Bases Cell Proliferation medicine.drug |
| Zdroj: | Journal of Biomolecular Structure and Dynamics. 40:2865-2877 |
| ISSN: | 1538-0254 0739-1102 |
| DOI: | 10.1080/07391102.2020.1844053 |
| Popis: | Recent years have witnessed advancement in cancer research that has led to the development of improved cytotoxic therapies with reduced side effects. Methotrexate (MTX) is a commonly used anticancer drug having robust activity, but with serious side effects. Several derivatives of MTX have been reported by modification at different sites to reduce its side effects and enhance efficacy. The current work describes the development of active MTX Schiff base derivatives by treating MTX with several aldehydes viz 2-chlorobenzaldehyde, 3-nitrobenzaldehyde, 5-chloro-2-hydroxybenz-aldehyde, 2-hydroxy-5-nitrobenzaldehyde, 2-thiocarboxyaldehyde, trans-2-pentenal and glutaraldehyde. Newly synthesized derivatives were evaluated for their anticancer potential against human malignant glioma U87 (MG-U87) cell lines at different concentrations of 200 μM, 100 μM, 50 μM, 25 μM, 12.5 μm, 6.25 μm and 0 μM. MTX derivatives with 2-Chlorobenzaldehyde (IC |
| Databáze: | OpenAIRE |
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