HIF-1[alpha] inhibition antitumor candidate drug and preparation method thereof

The invention discloses a HIF-1[alpha] inhibition antitumor candidate drug and a preparation method thereof. According to the present invention, a compound to be designed and synthesized can inhibit the glycolysis ability of tumor cells, the glycolysis inhibition adopts hypoxia-inducible factor 1[al...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: CAO XUAN, LIU JUAN, XIONG RUNDE, DENG XIANGPING, XIONG SHUJUAN, TANG GUOTAO, WANG ZHE, ZOU LIU
Format: Patent
Sprache:chi ; eng
Schlagworte:
Online-Zugang:Volltext bestellen
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:The invention discloses a HIF-1[alpha] inhibition antitumor candidate drug and a preparation method thereof. According to the present invention, a compound to be designed and synthesized can inhibit the glycolysis ability of tumor cells, the glycolysis inhibition adopts hypoxia-inducible factor 1[alpha] as the target, a flavone natural compound is designed and synthesized as a mother nucleus, the mother nucleus is modified with a benzimidazole derivative to synthesize series chrysin derivatives, and screening is performed by using the inhibition level of in vitro antitumor activity target protein to obtain the compound acting on the hypoxia-inducible factor 1[alpha]; the candidate drug inhibiting the glycolysis is selected; and the new potential candidate drug is provided for tumor treatment. 本发明公开了种抑制HIF-1α的抗肿瘤候选药物及制备方法,拟设计合成化合物能抑制肿瘤细胞的糖酵解能力,糖酵解抑制以低氧诱导因子1α为靶点,设计合成以黄酮天然化合物为母核,修饰苯并咪唑衍生物合成系列白杨素衍生物,采用体外抗肿瘤活性、靶点蛋白的抑制水平进行筛选,筛选出作用于低氧诱导因子1α的化合物。挑选出抑制糖酵解的候选药物;为治疗肿瘤提供潜在的新的候选药物。