新型吡唑支架的合成与生物学评价。

IF 0.7 4区 医学 Q4 PHARMACOLOGY & PHARMACY
Khaled Alseud
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引用次数: 0

摘要

通过苯基肼与(E)-2-((4-溴苯基)重氮基)-1-苯基-1,3-丁二酮反应生成 4-((4-溴苯基)重氮基)-5-甲基-1,3-二苯基吡唑,合成了一种含吡唑的化合物,并使用质谱仪、1H NMR 和 13C NMR 进行了表征。合成的化合物(KA5)对大肠杆菌 ATCC 8739、铜绿假单胞菌 ATCC 9027、金黄色葡萄球菌 ATCC 29213 和产气荚膜梭菌 ATCC 19404 的药理评估表明,该化合物不具有抗菌活性。不过,与索拉非尼(IC50:4.51μM)相比,KA5 在评估肝癌细胞系(HepG 2)时显示出竞争性抗癌活性(IC50:8.5μM)。此外,还利用人体皮肤成纤维细胞(HSF)研究了 KA5 对正常细胞系的影响(IC50:5.53μM)。所做的生物学评价使人们对 1、3、4-三取代吡唑的结构-活性关系有了更好的了解,并为更多研究新型含吡唑抗癌剂提供了良机。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis and biological evaluation of novel pyrazole scaffold.

synthesis of a pyrazole containing compound was achieved by reacting phenyl hydrazine with (E)-2-((4-bromophenyl) diazinyl)-1-phenylbutane-1,3-dione to produce 4-((4-bromophenyl) diazinyl)-5-methyl-1,3-diphenyl-pyrazole and characterization using mass spectrometer, 1H NMR and 13C NMR. The pharmacological evaluation of the synthesized compound, denoted as (KA5), against Escherichia coli ATCC 8739, Pseudomonas aeruginosa ATCC 9027, Staphylococcus aureus ATCC 29213 and Clostridiums sporogeneses ATCC 19404, indicate that there is no promising antibacterial activity. However, KA5 shows a competitive anticancer activity (IC50: 8.5μM) upon its evaluation against hepatocellular carcinoma cell line (HepG 2) compared to sorafenib (IC50: 4.51μM). Moreover, human skin fibroblast (HSF) was used to investigate the effect of KA5 on normal cell lines, (IC50: 5.53μM). The presented biological evaluations resulted in better understanding of structure-activity relationship for 1, 3, 4-trisubstituted pyrazoles and revealed a great opportunity for more investigations for novel pyrazole-containing anticancer agents.

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来源期刊
CiteScore
1.40
自引率
12.50%
发文量
211
审稿时长
4.5 months
期刊介绍: Pakistan Journal of Pharmaceutical Sciences (PJPS) is a peer reviewed multi-disciplinary pharmaceutical sciences journal. The PJPS had its origin in 1988 from the Faculty of Pharmacy, University of Karachi as a biannual journal, frequency converted as quarterly in 2005, and now PJPS is being published as bi-monthly from January 2013. PJPS covers Biological, Pharmaceutical and Medicinal Research (Drug Delivery, Pharmacy Management, Molecular Biology, Biochemical, Pharmacology, Pharmacokinetics, Phytochemical, Bio-analytical, Therapeutics, Biotechnology and research on nano particles.
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