...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Acta Poloniae Pharmaceutica: Durg Research >Synthesis, pro-apoptotic activity and 2D-QSAR studies of new analogues of fluphenazine.
【24h】

Synthesis, pro-apoptotic activity and 2D-QSAR studies of new analogues of fluphenazine.

机译：氟哌嗪新类似物的合成，促凋亡活性和2D-QSAR研究。

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

A series of 10 novel analogues of fluphenazine (FPh) were synthesized. Influence of the synthesized analogues of FPh on frequency of apoptosis and necrosis in cultures of human lymphocytes genotoxically damaged in vitro with benzo[a]pyrene (B[a]P; 7,5 microM, 48 h) was compared with the effect of FPh. Activity of the tested compounds was expressed by ED50 (pro-apoptotic activity) and TD50 (pro-necrotic effect, cytotoxicity). It was noticed that compounds 3-9 and 12 exerted a pro-apoptotic effect markedly stronger than that of FPh. Additionally, compounds 3, 9 and 10 exhibited the weakest influence on frequency of necrotic lymphocyte in cultures. 2D-QSAR analysis was done in order to find quantitative relationship between structures of the tested analogues and their pro-apoptotic activity or pro-necrotic effect in B[a]P-damaged cell cultures. Several statistically significant QSAR models were generated. Information obtained from 2D-QSAR study will be used in further design of analogues of FPh more active in cancer chemoprevention.
机译：合成了一系列10种新颖的氟奋乃静（FPh）类似物。将FPh的合成类似物对体外被苯并[a] Pyrene（B [a] P; 7,5 microM，48 h）遗传毒性破坏的人淋巴细胞培养物中细胞凋亡和坏死频率的影响与FPh的作用进行了比较。被测化合物的活性通过ED 50（促凋亡活性）和TD 50（促坏死作用，细胞毒性）表达。注意到化合物3-9和12具有明显比FPh强的促凋亡作用。另外，化合物3、9和10对培养物中坏死淋巴细胞的频率表现出最弱的影响。进行2D-QSAR分析是为了找到受测试类似物的结构与其在B [a] P损伤的细胞培养物中的促凋亡活性或促坏死作用之间的定量关系。生成了几个具有统计意义的QSAR模型。从2D-QSAR研究中获得的信息将用于进一步设计在癌症化学预防中更具活性的FPh类似物。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号