A3- and A2B-fluorocorroles: synthesis, X-ray characterization and antiviral activity evaluation against human cytomegalovirus infection
| Autor: | Kerstin Bystricky, Franck Gallardo, Léo Bucher, Sandrine Kappler-Gratias, Nicolas Desbois, Claude P. Gros, Yoann Rousselin |
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| Rok vydání: | 2020 |
| Předmět: |
Pharmacology
Human cytomegalovirus 0303 health sciences 010405 organic chemistry Chemistry Stereochemistry Organic Chemistry X-ray Pharmaceutical Science chemistry.chemical_element medicine.disease Ring (chemistry) 01 natural sciences Biochemistry 0104 chemical sciences Characterization (materials science) 03 medical and health sciences Drug Discovery medicine Fluorine Molecular Medicine Molecule Selectivity 030304 developmental biology |
| Zdroj: | RSC Medicinal Chemistry. 11:783-801 |
| ISSN: | 2632-8682 |
| DOI: | 10.1039/d0md00127a |
| Popis: | Twenty-nine fluorinated corroles were prepared, spectroscopically characterized, and studied for their antiviral activity against human cytomegalovirus infection. Six corroles were also fully characterized by X-ray crystallography giving insights on their geometrical features. The halogenated corroles reported herein exhibit significantly improved antiviral activity over their non-halogenated counterparts and over nitro-corrole analogs previously reported. Full activity of thirteen A3-corroles is achieved with four fluorine atoms present on the meso-phenyl ring reaching a selectivity index above 300. The maximum activity is achieved for A2B-corroles with selectivity indexes above 400. We thus demonstrate that the fluorocorrole is a highly potent platform to synthesize a new generation of anti hCMV molecules. |
| Databáze: | OpenAIRE |
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