| 赵明霞,张东霞,常进,赵治巨,齐传民,姜俊兵.化学通报,2021,84(8):803-813. |
| 新型吡唑并[1,5-a]嘧啶-氮芥衍生物的设计、合成及抗肿瘤活性研究（英文） |
| Design, Synthesis and Anticancer Activity Studies of Novel Pyrazolo[1,5-a]pyrimidine-Nitrogen Mustard Derivatives |
| 投稿时间：2020-11-28 修订日期：2021-01-25 |
| DOI： |
| 中文关键词: 吡唑并[1,5-a]嘧啶 氮芥 抗肿瘤活性 |
| 英文关键词:Pyrazolo[1,5-a]pyrimidine Nitrogen mustard antitumor activity |
| 基金项目:国家自然科学基金项目(21571021)、山西省重点研发计划重点项目(201603D21109-2)、山西省自然科学基金项目(201701D221283)、山西省高等学校科技创新项目(2019L0985)、阳泉市科技研发项目(2019G30)和山西省大学生创新创业训练计划项目(2019001,2020001)资助 |
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| 中文摘要: |
| 吡唑并嘧啶是一类具有广泛生物活性的杂环结构母体，同时，氮芥类药物被广泛应用于临床治疗癌症。本文基于药物设计的拼合原理，以简单易得的原料制备取代吡唑并[1,5-a]嘧啶中间体，通过将其与苯胺氮芥组分进行拼接，合成了一系列新型吡唑并[1,5-a]嘧啶-氮芥化合物，并评估了目标化合物对五种不同肿瘤细胞（HepG2，SH-SY5Y，A549，MCF-7和DU145）的抗增殖活性。结果表明，化合物9a～9g 对A549，HepG2和SH-SY5Y肿瘤细胞表现出很好的抑制活性，其中化合物9b的抑制活性分别为7.44，3.69和0.84 μmol/L，活性高于参考药物索拉菲尼和美法仑。 |
| 英文摘要: |
| Pyrazolopyrimidines are skeletons with wide biological activities, and nitrogen mustards are widely used in clinical as anticancer drug. Based on the combination principles of drug design, a series of novel pyrazolo [1,5-a] pyrimidine-nitrogen mustard compounds were designed and synthesized by splicing the two components. The antiproliferative activities of the target compounds against five different tumor cells (HepG2, SH-SY5Y, A549, MCF-7 and DU145) were evaluated in vitro. The results revealed that compounds 9a～9g had good antitumor activities on A549, HepG2 and SH-SY5Y human cancer cell lines. Among them, compound 9b showed the best antitumor activity with the IC50 value of 7.44, 3.69 and 0.84 μmol/L, respectively, better than the reference drugs Sorafenib and Melphalan. |
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