3-异丙基、3-正戊基环戊二酮-1,2 Mannich碱衍生物的合成及抗癌活性

Synthesis and Evaluation of 3-Isopropanyl-1,2-Cyclopentanedione and 3-n-Pentanyl-1,2-cyclopentanedione Mannich Bases for Antitumor Activity

以３异丙基、３正戊基环戊二酮１，２为母体化合物，设计合成了９个未见文献报道的Ｍａｎｎｉｃｈ碱衍生物，并在体外进行了抗癌活性评价。初步药理活性筛选结果表明，３正戊基环戊二酮１，２Ｍａｎｎｉｃｈ碱衍生物的抗癌活性较强，３异丙基环戊二酮１，２Ｍａｎｎｉｃｈ碱衍生物的活性相对较弱，多数化合物的抗癌活性优于阳性对照药５Ｆｕ．

3 Isopropanyl 1,2 cyclopentanedione and 3 n pentanyl 1,2 cyclopentanedione as lead compounds designed and synthesized,and we evaluated its bis Mannich bases for cytotoxicity and inhibition of DNA synthesis on human tumor cell lines in vitro. Results indicated that bis Mannich bases of 3 isopropanyl 1,2 cyclopentanedione showed lower antitumor activity,but antitumor activities of most of those compounds were stronger than that of 5 Fu in vitro .