Synthesis of N-(5,7-diamino-3-phenyl-quinoxalin-2-yl)-3,4,5-substituted anilines and N-[4[(5,7-diamino-3-phenylquinoxalin-2-yl)amino]benzoyl]-l-glutamic acid diethyl ester: Evaluation of in vitro anti-cancer and anti-folate activities
| Autor: | Paola Corona, Mario Loriga, Giuseppe Paglietti, Stefania Ferrari, M. Paola Costi |
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| Rok vydání: | 2008 |
| Předmět: |
Models
Molecular Molecular model Stereochemistry Drug Evaluation Preclinical Molecular Conformation Drug discovery drug synthesis quinoxaline antifolates anticancer dhydrofolatereductase thymidylate synthase Antineoplastic Agents Chemical synthesis Thymidylate synthase chemistry.chemical_compound Quinoxaline Glutamates Cell Line Tumor Quinoxalines hemic and lymphatic diseases Drug Discovery Humans Cell Proliferation Pharmacology chemistry.chemical_classification Aniline Compounds Binding Sites biology Organic Chemistry Aromatic amine Biological activity General Medicine In vitro Kinetics chemistry Antifolate biology.protein Folic Acid Antagonists |
| Zdroj: | European Journal of Medicinal Chemistry. 43:189-203 |
| ISSN: | 0223-5234 |
| DOI: | 10.1016/j.ejmech.2007.03.035 |
| Popis: | Several diamino quinoxalines were designed, synthesized and evaluated as anti-tumor agents. Two compounds showed the most potent cytotoxic activities against the leukemia CCRF-CEM cell line (GI(50)0.01microM) and the ovarian cancer cell line OVCAR-4 (GI(50)=0.03microM), respectively, with comparable/better activities than Methotrexate (MTX). Docking calculations of the complexes of hDHFR with the most active compounds identified the binding mode of the described molecules with respect to MTX. |
| Databáze: | OpenAIRE |
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