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天然产物马兜铃酸(1),它的β-硝基萘部分为抗肿瘤作用所必需。而它的某些类似物,包括许多β-硝基衍生物,在细胞培养中细胞毒性比它更强。抗生素环己亚胺(2)是蛋白质合成抑制剂,也是细胞毒素类药物,它象CG-603(3)[1-(吗啉基甲基)-4-邻苯二酰亚胺基哌啶-2,6-二酮]一样,是通过内分泌机理而起作用的。这两个化合物都含有一个戊二酰亚胺环,在(3)中它联结于侧链。此外,作用于DNA的抗病毒药物乙氨芴酮(4),有两个侧链,每一侧链都有一个叔胺基。作者试图将1～4中已知为活性所必需的化学结构合并在一个分子中,结果合成了四个新的3-
The natural product aristolochic acid (1), its β-nitronaphthalene moiety is necessary for antitumor effects. Some of its analogues, including many beta-nitro derivatives, are more cytotoxic than cell cultures. The antibiotic cycloheximide (2), a protein synthesis inhibitor, is also a cytotoxic drug that acts like a CG-603 (3) [1- (morpholinomethyl) -4-phthalimidylpiperidine -2,6-dione], works by the endocrine mechanism. Both of these compounds contain a glutarimide ring, which in (3) is attached to the side chain. In addition, the antiviral drug ethofluorenone (4) acting on the DNA has two side chains, each having a tertiary amine group. The authors attempted to combine the chemical structures necessary for activity known in 1 to 4 in one molecule, resulting in the synthesis of four new 3-