Divergent synthesis of thapsigargin analogs.
Bioorg Med Chem Lett
; 28(16): 2705-2707, 2018 09 01.
Article
en En
| MEDLINE
| ID: mdl-29636219
Thapsigargin (3) is a potent inhibitor of the SERCA-pump protein, with potential for application in a variety of medicinal areas. The efficient and scalable syntheses of thapsigargin (3) and nortrilobolide (2) have been disclosed previously. To demonstrate the modularity of the previous routes, three natural products (compounds 6, 13, 15) and four analogs (compounds 17-20) have been divergently prepared from a common building block featuring varied acyl chains at the C2, C3, and C8 positions. Biological tests revealed that all of the compounds prepared displayed promising activity profiles.
Palabras clave
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Tapsigargina
/
Inhibidores Enzimáticos
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ATPasas Transportadoras de Calcio del Retículo Sarcoplásmico
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2018
Tipo del documento:
Article
País de afiliación:
Estados Unidos