Oatis J E, Hynes J B
J Med Chem. 1977 Nov;20(11):1393-6. doi: 10.1021/jm00221a008.
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.
叶酸的喹唑啉类似物（5,8-二氮杂叶酸）及其10-甲基类似物已被证明是几种不同来源的胸苷酸合成酶的有效抑制剂。本文描述了其修饰物的合成，其中10位的氮原子被硫、氧或亚甲基取代，分别得到10-硫杂-5,8-二氮杂叶酸、10-氧杂-5,8-二氮杂叶酸和5,8,10-二氮杂叶酸。在初步测试中，每种目标化合物对小鼠L1210白血病均表现出微弱活性。
