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首页> 外文期刊>Acta Poloniae Pharmaceutica: Durg Research >Synthesis, pro-apoptotic activity and 2D-QSAR studies of new analogues of fluphenazine.
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Synthesis, pro-apoptotic activity and 2D-QSAR studies of new analogues of fluphenazine.

机译：氟苯嗪新类似物的合成，促凋亡活性和2D-QSAR研究。

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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种氟苯嗪（FPH）的新型类似物。 FPH合成类似物对苯并致毒性（B [A] P; 7.5 microM，48H）进行酸毒性损伤的人淋巴细胞培养物中凋亡和坏死频率的影响与FPH的效果。测试化合物的活性由ED50（促凋亡活性）和TD50（pro-坏死效应，细胞毒性）表示。注意到，化合物3-9和12施加促凋亡效应明显强于FPH。另外，化合物3,9和10表现出培养物中坏死淋巴细胞频率的最弱影响。完成了2D-QSAR分析，以便在B [A] P损伤的细胞培养物中找到测试类似物结构与其促凋亡活性或亲坏死作用的定量关系。产生了几种统计上显着的QSAR模型。从2D-QSAR研究中获得的信息将进一步设计在癌症化学普通中FPH的类似物的类似物。

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