Synthesis and biological evaluation of novel tricyclic matrinic derivatives as potential anti-filovirus agents
Acta Pharmaceutica Sinica B
;
(6): 629-638, 2018.
Article
Dans Anglais
| WPRIM
| ID: wpr-690877
ABSTRACT
Twenty-six novel tricyclic sophoridinic and matrinic derivatives containing a common chlorinated benzene fragment were designed, synthesized and evaluated for their anti-ebolavirus (EBOV) activities. Structure-activity relationship analysis indicated (i) 12-dichlorobenzyl motif was beneficial for the activity; (ii) the chiral configuration at C5 atom might not affect the activity much. Among the target compounds, compound exhibited the most potent potency against EBOV with an IC value of 5.29 μmol/L and an SI value of over 37.8. Further anti-EBOV assay of identified its high effectiveness, and anti-MARV assay of suggested its inspiring broad-spectrum anti-filovirus activity. The results provided powerful information on further strategic optimization and development of this kind of compounds against filoviruses.
Texte intégral:
Disponible
Indice:
WPRIM (Pacifique occidental)
langue:
Anglais
Texte intégral:
Acta Pharmaceutica Sinica B
Année:
2018
Type:
Article
Documents relatifs à ce sujet
MEDLINE
...
LILACS
LIS