Synthesis and antitumor activity evaluation of ursolic acid derivatives.

Meng, Yan-Qiu; Xu, Chuan-Dong; Yu, Ting-Ting; Li, Wei; Li, Qian-Wen; Li, Xiao-Xiao

Meng, Yan-Qiu; Xu, Chuan-Dong; Yu, Ting-Ting; Li, Wei; Li, Qian-Wen; Li, Xiao-Xiao.

Meng YQ; Department of Pharmaceutical Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China.
Xu CD; Department of Pharmaceutical Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China.
Yu TT; Department of Pharmaceutical Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China.
Li W; Department of Pharmaceutical Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China.
Li QW; Department of Pharmaceutical Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China.
Li XX; Department of Pharmaceutical Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China.

J Asian Nat Prod Res ; 22(4): 359-369, 2020 Apr.

Article en En | MEDLINE | ID: mdl-30829054

ABSTRACT

ABSTRACT

Eighteen uronic acid derivatives were designed and synthesized, and the cytotoxicities in vitro of two cancer cell lines (BEL7402 and SGC7901) were evaluated by MTT assay. The results showed that the inhibitory rate of the compounds on both cell lines was significantly higher than the parent compound. The IC50 of compounds II4, II6, III4, and III6 are comparable or stronger than the positive control drug, the interactions between compounds II4, II6, III4, III6, and NF-κB were also studied by docking simulations.

Asunto(s)

Antineoplásicos; Línea Celular Tumoral; Proliferación Celular; Ensayos de Selección de Medicamentos Antitumorales; Estructura Molecular; Relación Estructura-Actividad; Triterpenos; Ácido Ursólico

Palabras clave

NF-κB inhibitor; Ursolic acid derivatives; anticancer activity; synthetic

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