Caperelli C A, Conigliaro J
J Med Chem. 1986 Oct;29(10):2117-9. doi: 10.1021/jm00160a056.
10-Acetyl-5,8-dideazafolic acid has been synthesized in good yield from the parent compound, 5,8-dideazafolic acid. This quinazoline folate analogue showed no activity as a substrate for the folate-requiring de novo purine biosynthetic enzyme glycinamide ribonucleotide transformylase isolated from the murine lymphoma cell line L5178Y, but proved to be a potent competitive inhibitor, Ki = 1.3 microM, of the purified enzyme.
10-乙酰基-5,8-二去氮叶酸已从母体化合物5,8-二去氮叶酸高产率合成。这种喹唑啉叶酸类似物作为从鼠淋巴瘤细胞系L5178Y中分离出的需要叶酸的从头嘌呤生物合成酶甘氨酰胺核糖核苷酸转甲酰基酶的底物没有活性，但被证明是纯化酶的一种有效竞争性抑制剂，抑制常数Ki = 1.3微摩尔。
