[EN] 2',5'-DIDEOXY-5-FLUOROURIDINE DERIVATIVES HAVING CYTOTOXIC ACTIVITY, A PROCESS FOR THE MANUFACTURE THEREOF AND APPLICATION THEREOF<br/>[FR] DÉRIVÉS DE 2',5'-DIDÉSOXY-5-FLUOROURIDINE PRÉSENTANT UNE ACTIVITÉ CYTOTOXIQUE, LEUR PROCÉDÉ DE FABRICATION ET LEUR APPLICATION
申请人:UNIV ADAM MICKIEWICZ
公开号:WO2015041550A1
公开(公告)日:2015-03-26
The subject matter of the invention is novel 2',5'-dideoxy-5-fluorouridine derivatives of general formula 1. (1) wherein R1 denotes cinchona alkaloid fragment with defined absolute configuration at C-8and C-9 atoms. In a second aspect, the subject matter of the invention is a process for the manufacture of 2',5'- dideoxy-5-fluorouridine derivatives of general formula 1. In a third aspect, the subject matter of the invention is an application of 2',5'-dideoxy-5- fluorouridine derivatives of general formula 1 in the anticancer treatment of breast cancer, cervical cancer, lung cancer and nasopharynx cancer.
本发明的主题是一种新型的通式1的2',5'-二去氧-5-氟尿苷衍生物。(1)其中R1表示奎宁生物碱片段,在C-8和C-9原子处具有定义的绝对构型。在第二方面,本发明的主题是一种制造通式1的2',5'-二去氧-5-氟尿苷衍生物的方法。在第三方面,本发明的主题是将通式1的2',5'-二去氧-5-氟尿苷衍生物应用于乳腺癌、宫颈癌、肺癌和鼻咽癌的抗癌治疗中。