Cytotoxic Activity and Structure-Activity Relationship of Triazole-Containing Bis(Aryl Ether) Macrocycles
| Autor: | Alejandra Chávez-Riveros, Rocio Morales-Barcenas, Luis D. Miranda, Alfonso Dueñas-González, Alma Chavez-Blanco, Eduardo Hernández-Vázquez, María Teresa Ramírez-Apan, Adriana Romo-Pérez |
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| Rok vydání: | 2018 |
| Předmět: |
Macrocyclic Compounds
Stereochemistry Substituent Triazole Antineoplastic Agents Apoptosis Ether 010402 general chemistry 01 natural sciences Biochemistry Structure-Activity Relationship chemistry.chemical_compound Cell Line Tumor Drug Discovery Humans Moiety Structure–activity relationship General Pharmacology Toxicology and Pharmaceutics Pharmacology Trifluoromethyl Dose-Response Relationship Drug Molecular Structure 010405 organic chemistry Aryl Organic Chemistry Triazoles 0104 chemical sciences Solvent chemistry Molecular Medicine Drug Screening Assays Antitumor Ethers |
| Zdroj: | ChemMedChem. 13:1193-1209 |
| ISSN: | 1860-7179 |
| DOI: | 10.1002/cmdc.201800075 |
| Popis: | Cancer continues to be a worldwide health problem. Certain macrocyclic molecules have become attractive therapeutic alternatives for this disease because of their efficacy and, frequently, their novel mechanisms of action. Herein, we report the synthesis of a series of 20-, 21-, and 22-membered macrocycles containing triazole and bis(aryl ether) moieties. The compounds were prepared by a multicomponent approach from readily available commercial substrates. Notably, some of the compounds displayed interesting cytotoxicity against cancer (PC-3) and breast (MCF-7) cell lines, especially those bearing an aliphatic or a trifluoromethyl substituent on the N-phenyl moiety (IC50 |
| Databáze: | OpenAIRE |
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