Synthesis and antitumor activity of A-ring modified hexacyclic analogues of camptothecin / 药学学报
Acta Pharmaceutica Sinica
;
(12): 241-247, 2005.
Artículo
en Inglés
| WPRIM
| ID: wpr-241320
ABSTRACT
<p><b>AIM</b>To improve the biological activity of A-ring modified analogues of camptothecin.</p><p><b>METHODS</b>A-ring modified camptothecins were synthesized from 10-hydroxycamptothecin or 7-ethyl-10-hydroxycamptothecin (SN-38) in three or four steps. Their cytotoxicity was evaluated using MTY assay, and their in vivo antitumnor activity against mouse liver cancer H22 was tested. Results Five hexacyclic camptothecins (6a, 6b, 6c, 7a and 7b) are target compounds, and ten camptothecin derivatives are new compounds.</p><p><b>CONCLUSION</b>The modification of a 1,4-oxazine-2-one ring fused with positions 9 and 10 of A-ring will reduce the antitumor activity of camptothecins.</p>
Texto completo:
Disponible
Índice:
WPRIM (Pacífico Occidental)
Asunto principal:
Patología
/
Farmacología
/
Compuestos Policíclicos
/
Camptotecina
/
Química
/
Carcinoma Hepatocelular
/
Línea Celular Tumoral
/
Quimioterapia
/
Neoplasias Hepáticas
/
Trasplante de Neoplasias
Límite:
Animales
/
Femenino
/
Humanos
Idioma:
Inglés
Revista:
Acta Pharmaceutica Sinica
Año:
2005
Tipo del documento:
Artículo
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