| 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 |
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| 引用本文： | 朴日阳,刘百里,计志忠,宋连生,付勤,任林广.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[J].中国药物化学杂志,1998(2). |
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| 作者姓名： | 朴日阳 刘百里 计志忠 宋连生 付勤 任林广 |
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| 作者单位： | 沈阳药科大学合成药物研究室，吉林省肿瘤研究所 |
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| 摘 要： | 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５Ｆｕ．
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| 关 键 词： | 3-异丙基环戊二酮-1.2 3-正戊基环戊二酮-1.2 Mannich碱 合成 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 |
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| Piao Riyang,Liu Baili,Ji Zhizhong.Synthesis and Evaluation of 3-Isopropanyl-1,2-Cyclopentanedione and 3-n-Pentanyl-1,2-cyclopentanedione Mannich Bases for Antitumor Activity[J].Chinese Journal of Medicinal Chemistry,1998(2). |
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| Authors: | Piao Riyang Liu Baili Ji Zhizhong |
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| Abstract: | 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 . |
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| Keywords: | 3 isopropanyl 1 2 cyclopentanedione 3 n pentanyl 1 2 cyclopentanedione Mannich bases synthesis antitumor activity |
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