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三氟胸苷衍生物对培养细胞及牛痘病毒感染的HeLa细胞的生长抑制作用

Growth inhibition of cells in cultures and of vaccinia virus infected HeLa cells by derivatives of trifluorothymidine.

作者信息

Parkhurst J R, Danenberg P V, Heidelberger C

出版信息

Chemotherapy. 1976;22(3-4):221-31. doi: 10.1159/000221929.

DOI:10.1159/000221929
PMID:178485
Abstract

The effects of 5-trifluoromethyluracil (F3Thy), 5-trifluoromethyl-2'-deoxyuridine (F3dThd), F3dThd-5'-P, and F3dThd-5'-methylphosphonate on the growth of HeLa cells, Novikoff hepatoma cells, L5178Y mouse leukemia cells, and on the replication of vaccinia virus in HeLa cells have been determined. F3Thy and F3dThd-5'-methylophosphonate were approximately 500-fold and 100-fold less effective, respectively, than F3dThd or F3dThd-5'-P in their inhibition of these cells. F3dThd and F3dThd-5'-P are potent inhibitors of vaccinia viral replication of HeLa cells. The nucleoside and nucleotide were 1,000-fold more inhibitory than the free base. F3dThd was nost inhibitory when added between 1 and 2 h post-infection; however, it was also somewhat inhibitory when added at later times.

摘要

已测定了5-三氟甲基尿嘧啶(F3Thy)、5-三氟甲基-2'-脱氧尿苷(F3dThd)、F3dThd-5'-磷酸酯和F3dThd-5'-甲基膦酸酯对HeLa细胞、诺维科夫肝癌细胞、L5178Y小鼠白血病细胞生长以及对痘苗病毒在HeLa细胞中复制的影响。F3Thy和F3dThd-5'-甲基膦酸酯在抑制这些细胞方面的效果分别比F3dThd或F3dThd-5'-磷酸酯低约500倍和100倍。F3dThd和F3dThd-5'-磷酸酯是HeLa细胞中痘苗病毒复制的有效抑制剂。核苷和核苷酸的抑制作用比游离碱强1000倍。感染后1至2小时之间添加F3dThd时抑制作用最强;然而,在较晚时间添加时也有一定程度的抑制作用。

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