5-脱氮-5,6,7,8-四氢叶酸及其N10-取代类似物的合成与抗肿瘤活性
Synthesis and antitumor activity of 5-deaza-5,6,7,8-tetrahydrofolic acid and its N10-substituted analogues.
作者信息
Taylor E C, Hamby J M, Shih C, Grindey G B, Rinzel S M, Beardsley G P, Moran R G
机构信息
Department of Chemistry, Princeton University, New Jersey 08544.
出版信息
J Med Chem. 1989 Jul;32(7):1517-22. doi: 10.1021/jm00127a019.
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.
描述了5-脱氮-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。这些化合物作为新型叶酸抗代谢物的先导化合物5,10-二脱氮-5,6,7,8-四氢叶酸（DDATHF）的类似物制备而成，在体外对白血病细胞具有强大的生长抑制作用，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。
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