| 吡唑并[1，5-α]嘧啶类化合物的合成及其抗肿瘤活性 |
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| 引用本文： | 李娟,赵燕芳,陈栋,贾薇,宫平.吡唑并[1，5-α]嘧啶类化合物的合成及其抗肿瘤活性[J].中国药物化学杂志,2006,16(6):352-355. |
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| 作者姓名： | 李娟 赵燕芳 陈栋 贾薇 宫平 |
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| 作者单位： | 沈阳药科大学制药工程学院 辽宁沈阳110016 |
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| 摘 要： | 目的设计合成新的吡唑并1,5-a]嘧啶类化合物,并评价其抗肿瘤活性。方法根据吡唑并1,5-a]嘧啶类抗肿瘤药物的基本结构设计了一系列5-胺甲基-7-苯胺基吡唑并1,5-a]嘧啶类化合物,并以丙二腈和原甲酸三乙酯为起始原料,经5步反应得到目标产物。采用MTT法,以顺铂为阳性对照药,以Bel-7402和HT-1080为测试细胞株对目标化合物的抗肿瘤活性进行评价。结果与结论合成了11个未见文献报道的化合物,结构经质谱和核磁共振氢谱确证。化合物6显示出很好的抗肿瘤活性。
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| 关 键 词： | 药物化学 化合物制备 化学合成 吡唑并[1 5-a]嘧啶类化合物 抗肿瘤活性 |
| 文章编号： | 1005-0108（2006）06-0352-04 |
| 收稿时间： | 2006-04-18 |
| 修稿时间： | 2006年4月18日 |
Synthesis and antitumor activities of pyrazolo[1,5-a] pyrimidines |
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| LI Juan, ZHAO Yan-fang, CHEN Dong, JIA Wei, GONG Ping.Synthesis and antitumor activities of pyrazolo[1,5-a] pyrimidines[J].Chinese Journal of Medicinal Chemistry,2006,16(6):352-355. |
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| Authors: | LI Juan ZHAO Yan-fang CHEN Dong JIA Wei GONG Ping |
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| Institution: | School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China |
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| Abstract: | Ai mTo design andsynthesize novel pyrazolo1,5-a]pyri midine derivatives,andto assaytheir an-titumor activities.MethodsBased on the general structure of pyrazolo1,5-a]pyri midine having antitumoractivity,5-aminomethyl-7-anilinopyrazolo1,5-a] pyri midines were designed,and the target compoundswere synthesizedviaafive-step procedure startingfrom malononitrile andtriethyl orthoformate.Using cis-platin as positive control,their antitumor activities were evaluated with Bel-7402 and HT-1080in vitro.Re-sults and conclusionsEleven novel compounds were synthesized,andtheir structures were confirmed by1H-NMRand MS.Among them,compound6displayed good antitumor activity. |
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| Keywords: | medicinal chemistry compound preparation chemical synthesis pyrazolo[1 5-a]pyri midines antitumor activities |
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