Tronchet J M, Grivet C, Grand E, Seman M, Dilda P
Department of Pharmaceutical Chemistry, University of Geneva, Faculty of Sciences, Switzerland.
Carbohydr Lett. 2000;4(1):5-12.
A series of modified nucleosides bearing at varied positions of the sugar moiety one 3-aryl-1-triazeno N1-oxide group and a variable number of O-TBDMS groups have been prepared and their cytotoxicities and cytostaticities measured on different cell lines. Nucleosides bearing an aryltriazeno N-oxide group and O-TBDMS groups are either devoid of cytotoxicity or possess a selective cytotoxicity. On the other hand, nucleosides bearing one triazeno group and no silyl group are devoid of cytotoxicity and silylated nucleosides without triazeno group are generally either devoid of cytotoxicity or unselectively cytotoxic. This indicates that the O-TBDMS group per se is not cytotoxic.
已制备了一系列在糖部分的不同位置带有一个3-芳基-1-三氮烯N1-氧化物基团和可变数量的O-TBDMS基团的修饰核苷，并测定了它们对不同细胞系的细胞毒性和细胞生长抑制活性。带有芳基三氮烯N-氧化物基团和O-TBDMS基团的核苷要么没有细胞毒性，要么具有选择性细胞毒性。另一方面，带有一个三氮烯基团且没有硅烷基的核苷没有细胞毒性，而没有三氮烯基团的硅烷化核苷通常要么没有细胞毒性，要么具有非选择性细胞毒性。这表明O-TBDMS基团本身没有细胞毒性。
