以２羟基３甲基环戊２烯酮为母体化合物设计合成了１０个双Ｍａｎｎｉｃｈ碱衍生物，４个单Ｍａｎｎｉｃｈ碱衍生物．体外细胞毒性试验和ＤＮＡ合成抑制试验结果表明：脂肪胺、杂环胺双Ｍａｎｎｉｃｈ碱活性较强，优于阳性对照药５Ｆｕ；二甲胺单Ｍａｎｎｉｃｈ碱活性较强，而芳胺类Ｍａｎｎｉｃｈ碱活性很弱，ＩＣ５０值大于５０ｍｇ／Ｌ． Ten 2-Mannich base derivatives and 4 single Mannich base derivatives were designed and synthesized with 2-hydroxy-3-methylcyclopentane-2-enone as the parent compound. In vitro cytotoxicity test and DNA synthesis inhibition test results show that: aliphatic amines, heterocyclic amine Mannich double strong base activity, better than the positive control drug 5 Fu; dimethylamine single Mannich base activity is strong, and aromatic amines Mannich base activity is weak, IC50 value greater than 50mg / L.