Soliman F S, Salama H M
Pharmazie. 1983 Sep;38(9):585-6.
In a continuing search for new antineoplastic and antiviral agents, the preparation of some substituted indol-2(3H)-one-3-spiro-2'-3',4'-dihydroxy-5'-imino-2',5'-dihydrofurans was designed. The synthesis was achieved by reacting isatin, 1-alkyl- or 1-aralkylisatin derivative with glyoxal sodium bisulfite and potassium cyanide. However, when 1-substituted aminomethyl derivatives of isatin or of 5-bromoisatin were used in this reaction, the indolone-spiro-hydroxytetronimide unsubstituted at position 1 was, unexpectedly, the only product isolated. Two compounds were tested against P-388 lymphocytic leukemia in mice and were inactive.
为了持续寻找新的抗肿瘤和抗病毒药物，设计了一些取代吲哚 - 2(3H)-酮 - 3 - 螺 - 2'-3',4'-二羟基 - 5'-亚氨基 - 2',5'-二氢呋喃的制备方法。通过使异吲哚酮、1 - 烷基 - 或1 - 芳烷基异吲哚酮衍生物与乙二醛亚硫酸氢钠和氰化钾反应来实现合成。然而，当在此反应中使用异吲哚酮或5 - 溴异吲哚酮的1 - 取代氨甲基衍生物时，令人意外的是，在1位未取代的吲哚酮 - 螺 - 羟基四氢异酰亚胺是唯一分离得到的产物。对两种化合物进行了针对小鼠P - 388淋巴细胞白血病的测试，结果显示它们没有活性。
