Synthetic approaches to the guanosine and xanthosine analogues 5-amino-3-beta-D-ribofuranosylpyrazolo[3,4-e][1,3]oxazin-7-one and 3-beta-D-ribofuranosylpyrazolo[3,4-e][1,3]oxazine-5,7-dione and studies of their antitumor potential.
Synthetic approaches to the guanosine and xanthosine analogues 5-amino-3-beta-D-ribofuranosylpyrazolo[3,4-e][1,3]oxazin-7-one and 3-beta-D-ribofuranosylpyrazolo[3,4-e][1,3]oxazine-5,7-dione and studies of their antitumor potential.
复制标题
鸟苷和黄苷类似物 5-氨基-3-β-D-呋喃核糖基吡唑并[3,4-e][1,3]恶嗪-7-酮和 3-β-D-呋喃核糖基吡唑并[3,4-e]的合成方法
DOI：
10.1021/jm00111a005
复制
发表时间：
1991
影响因子：
7.3
通讯作者：
Townsend,LB
中科院分区：
文献类型：
--
作者：
Zou,RM;Beylin,VG;Groziak,MP;Wotring,LL;Townsend,LB
通过适当保护的吡唑呋林衍生物的环化和随后的杂环部分的转化，合成了5-氨基-3-/3-D-呋喃核基吡唑并[3, 4-e][1, 3]恶嗪-7-酮。这种鸟苷类似物在体外对 L1210 细胞具有轻微的细胞毒性。黄嘌呤核苷类似物 3-/3-n-呋喃核糖基吡唑并[3, 4-e]-[l, 3]恶嗪-5, 7-二酮也被合成，并被发现具有高度细胞毒性。它似乎充当吡唑呋林的前药。
5-Amino-3-/3-D-ribofuranoeylpyrazolo [3, 4-e][l, 3] oxazin-7-one has been synthesized via cyclization of the appropriately protected pyrazofurin derivatives and subsequent transformations of the heterocyclic moiety. This guanosine analogue was marginally cytotoxic to L1210 cells invitro. The xanthosineanalogue 3-/3-n-ribofuranosylpyrazolo [3, 4-e]-[l, 3] oxazine-5, 7-dione was also synthesized, and was found to be highly cytotoxic. It appeared to act as a prodrug of pyrazofurin.