Alkylide derivatives of diphyllin: synthesis and preliminary anticancer evaluation.

Dong, Chen-Hu; Wang, Hui; Ma, Yu-Jie; Zhang, Ying; Si, Chao; Zhao, Yu

Dong, Chen-Hu; Wang, Hui; Ma, Yu-Jie; Zhang, Ying; Si, Chao; Zhao, Yu.

Afiliación

Dong CH; School of Pharmacy, Nantong University, Nantong 226001, China.
Wang H; R&D Department, Shanghai Rulink Biopharmaceutical Corporation, Shanghai 201203, China.
Ma YJ; School of Pharmacy, Nantong University, Nantong 226001, China.
Zhang Y; School of Pharmacy, Nantong University, Nantong 226001, China.
Si C; Pharmacy Department, Shandong Healthcare Group Xinwen Central Hospital, Xintai 271200, China.
Zhao Y; School of Pharmacy, Nantong University, Nantong 226001, China.

J Asian Nat Prod Res ; 26(7): 833-842, 2024 Jul.

Article en En | MEDLINE | ID: mdl-38584456

ABSTRACT

ABSTRACT

Fourteen diphyllin 4-C-substituted alkylide derivatives were designed and synthesized using a Heck coupling and subsequent hydrogenation reaction. Olefins 3g and 3i exhibited the highest cytotoxicity on breast cancer cell lines MCF-7 with IC50 values of 0.08 and 0.07 µM, and they showed weaker V-ATPase inhibitory potency compared to diphyllin.

Asunto(s)

Antineoplásicos; Ensayos de Selección de Medicamentos Antitumorales; Humanos; Estructura Molecular; Antineoplásicos/farmacología; Antineoplásicos/síntesis química; Antineoplásicos/química; Células MCF-7; Relación Estructura-Actividad; Alquenos/química; Alquenos/farmacología; Lignanos

Palabras clave

Diphyllin; alkylide derivatives; anticancer agents; synthesis

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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Ensayos de Selección de Medicamentos Antitumorales / Antineoplásicos Límite: Humans Idioma: En Revista: J Asian Nat Prod Res Asunto de la revista: BOTANICA / QUIMICA Año: 2024 Tipo del documento: Article País de afiliación: China

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