Synthesis and in vitro antitumor evaluation of betulin acid ester derivatives as novel apoptosis inducers.
Eur J Med Chem
; 102: 249-55, 2015 Sep 18.
Article
en En
| MEDLINE
| ID: mdl-26280921
ABSTRACT
Nineteen betulin derivatives modified at the C-3 and C-28 positions were synthesized and assessed for antitumor activities against the MGC-803, PC3, Bcap-37, A375, and MCF-7 human cancer cell lines in vitro by MTT assay. Some derivatives (compounds 3a-3d and 5) displayed strong antitumor properties, with IC50 values between 4 and 18 µM. Compound 3c, containing piperidine group at C-28 position, had IC50 values of 4.3, 4.5, 5.2, 7.5, and 5.2 µM on the five cancer cell lines, respectively. Subsequent fluorescence staining and flow cytometric analysis indicated that compound 3c induced apoptosis in MGC-803 cell line, with an apoptosis ratio of 31.11% after 36 h of treatment at 10 µM 3c.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Triterpenos
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Apoptosis
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Ésteres
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Antineoplásicos
Límite:
Animals
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Humans
Idioma:
En
Revista:
Eur J Med Chem
Año:
2015
Tipo del documento:
Article