SYNTHESIS AND ANTITUMOR-ACTIVITY OF 5-DEAZA-5,6,7,8-TETRAHYDROFOLIC ACID AND ITS N-10-SUBSTITUTED ANALOGS
SYNTHESIS AND ANTITUMOR-ACTIVITY OF 5-DEAZA-5,6,7,8-TETRAHYDROFOLIC ACID AND ITS N-10-SUBSTITUTED ANALOGS
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DOI：
10.1021/jm00127a019
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发表时间：
1989-07-01
影响因子：
7.3
通讯作者：
MORAN, RG
中科院分区：
文献类型：
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作者：
TAYLOR, EC;HAMBY, JM;MORAN, RG
介绍了5-二氮杂-5,6,7,8-四氢叶酸（7a）及其10-甲酰基（7b）、10-乙酰基（7c）和10-甲基（7d）衍生物的合成。这些化合物是作为一类新的叶酸抗代谢产物的先导化合物- 5,10-二氧二氮-5,6,7,8-四氢叶酸（DDATHF）的类似物制备的，在培养中对白血病细胞具有有效的生长抑制作用，并且在体内对可移植的小鼠实体瘤具有显著的抗肿瘤活性。
Syntheses of 5-deaza-5,6,7,8-tetrahydrofolic acid (7a) and its 10-formyl (7b), 10-acetyl (7c), and 10-methyl (7d) derivatives are described. These compounds, prepared as analogues of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid (DDATHF), the lead compound of a new class of folate antimetabolites, exhibit potent growth inhibition against leukemic cells in culture as well as substantial antitumor activity against transplantable murine solid tumors in vivo.