Synthesis of quinazoline analogs of folic acid modified at position 10
Synthesis of quinazoline analogs of folic acid modified at position 10
复制标题
10位修饰叶酸喹唑啉类似物的合成
DOI：
--
复制
发表时间：
1977
期刊：
影响因子：
--
通讯作者：
J. Hynes
中科院分区：
文献类型：
--
作者：
J. Oatis;J. Hynes
叶酸的喹唑啉对应物（5,8-脱氮叶酸）及其 10-甲基类似物已被证明是多种不同来源的胸苷酸合成酶的有效抑制剂。本文描述了修饰的合成，其中 10 位的氮原子被硫、氧或亚甲基取代，分别得到 10-硫杂-5,8-脱氮叶酸、10-氧杂-5,8-脱氮叶酸和 5,8,10-脱氮叶酸。在初步测试中，每种目标化合物都对小鼠 L1210 白血病表现出边际活性。
The quinazoline couterpart of folic acid (5,8-deazafolic acid) as well as its 10-methyl analogue has been shown to be an effective inhibitor of thymidylate synthetase from several different sources. This paper describes the synthesis of modifications in which the nitrogen atom at position 10 is replaced by sulfur, oxygen, or methylene affording 10-thia-5,8-deazafolic acid, 10-oxa-5,8-deazafolic acid, and 5,8,10-deazafolic acid, respectively. In preliminary testing, each of the target compounds displayed marginal activity against L1210 leukemia in mice.