Design, synthesis and antiproliferative activities of artemisinin derivatives substituted by N-heterocycles / 药学学报
Acta Pharmaceutica Sinica
; (12): 868-874, 2015.
Article
en Zh
| WPRIM
| ID: wpr-257054
Biblioteca responsable:
WPRO
ABSTRACT
Increasing attention has been focused on the antitumor activity of artemisinin derivatives in recent years, for artemisinin had been reported to have cytotoxic effects against HL-60, P388 and MCF-7 tumor cells. We report here the synthesis and evaluation for antitumor activity of a series of artemisinin-ether derivatives bearing tetrahydropyrrole, morpholine, piperidine, substituted piperidines and azoles with various linkers. Sixteen 10-O-substituted dihydroartemisinin derivatives were designed and synthesized, all of which have never been reported in literatures and whose antiproliferative effects on human breast cancer MCF-7, MCF-7/Adr and HL-60 cells were determined by MTT assay or direct cell counting. Each of these artemisinin derivatives possessed better effects than dihydroartemisinin evidently against HL-60 and MCF-7 cells growth, while less potent than doxorubicin. All target compounds exhibited significantly improved potency compared to DHA and doxorubicin on the doxorubicin-resistant MCF-7/Adr cells, so did they in their sensitive counterparts MCF-7 cells. Among them, compounds GF02, GH04 and ZH04 showed strong activity against these three cell lines growth. Further research is undergoing.
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Índice:
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Asunto principal:
Patología
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Neoplasias de la Mama
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Diseño de Fármacos
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Doxorrubicina
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Química
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Células HL-60
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Artemisininas
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Proliferación Celular
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Células MCF-7
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Antineoplásicos
Límite:
Humans
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Año:
2015
Tipo del documento:
Article