2-取代苯并咪唑四氯铂酸酯类化合物的合成及其对不同细胞系的细胞毒活性

Q3 Pharmacology, Toxicology and Pharmaceutics Fabad Journal of Pharmaceutical Sciences Pub Date : 2022-07-01 DOI:10.55262/fabadeczacilik.1134520
Mahmut Gözelle, A. Kılıç Süloğlu
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引用次数: 0

摘要

本研究旨在合成新型含苯并咪唑配体铂类化合物,并筛选其对人宫颈癌HeLa、人肺癌aa549和人肺上皮Beas-2B细胞系的体外细胞毒活性。采用适当的醛和邻苯二胺合成了2-取代苯并咪唑配体。随后,用2-取代苯并咪唑配体和四氯铂酸钾(II)(K2PtCl4)合成2-异丙基苯并咪唑烯四氯铂酸盐(II)(K1)和2-(1-甲基丙基)苯并咪唑烯四氯铂酸盐(II)一水合物(K2)。利用HRMS、IR、元素分析、1H-NMR和熔点对合成的化合物进行表征。MTT法观察铂类化合物对HeLa、A549和Beas-2B细胞的细胞毒活性。以顺铂和卡铂为对照药。结果表明,K2铂化合物对HeLa的细胞毒活性为53.42%±2.21(160 μM),对A549的细胞毒活性为88.16%±0.22 (160 μM),对Beas-2B的细胞毒活性为92.09%±0.57 (160 μM),对HeLa的细胞毒活性为27.42%±2.03 (160 μM),对A549的细胞毒活性为93.95%±0.53(160 μM),对Beas-2B的细胞毒活性为91.99±0.22 (160 μM)。这两种铂化合物在被试细胞孵育48小时后都比对照药物卡铂具有更高的细胞抑制作用。
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Synthesis of 2-Substitutedbenzimidazolium Tetrachloroplatinate(II) Compounds and Their Cytotoxic Activities on Different Cell Lines
The aim of the study was the synthesis of novel platinum compounds having benzimidazole ligands and screening for their in vitro cytotoxic activity on human cervical carcinoma HeLa, human lung carcinoma A549, and human lung epithelial Beas-2B cell lines. 2-Substituted benzimidazole ligands were synthesized by using appropriate aldehydes and o-phenylenediamine. Subsequently, 2-substituted benzimidazole ligands and potassium tetrachloroplatinate(II) (K2PtCl4) were used to synthesize 2-isopropylbenzimidazole tetrachloroplatinate(II) (K1) and 2-(1-methylpropyl)benzimidazole tetrachloroplatinate(II) monohydrate (K2). HRMS, IR, elemental analysis, 1H-NMR, and melting point were used to characterize the synthesized compounds. Cytotoxic activities against HeLa, A549, and Beas-2B cells after 48 h and 72 h incubation of the platinum compounds were investigated via MTT assay. Cisplatin and carboplatin were used as reference drugs. The cytotoxic activity results showed that K2 platinum compound displayed 53.42%±2.21 (at 160 μM) on HeLa, 88.16%±0.22 (at 160 μM) on A549 and 92.09%±0.57 (at 160 μM) on Beas-2B after 48 h incubation, K2 displayed 27.42%±2.03 (at 160 μM) on HeLa, 93.95%±0.53 (at 160 μM) on A549 and 91.99±0.22 (at 160 μM) on Beas-2B after 72 h incubation. Both of the platinum compounds have higher cell inhibitory effects than reference drug carboplatin after 48 h incubation for tested cells.
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来源期刊
Fabad Journal of Pharmaceutical Sciences
Fabad Journal of Pharmaceutical Sciences Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
0.80
自引率
0.00%
发文量
12
期刊介绍: The FABAD Journal of Pharmaceutical Sciences is published triannually by the Society of Pharmaceutical Sciences of Ankara (FABAD). All expressions of opinion and statements of supposed facts appearing in articles and/or advertisiments carried in this journal are published on the responsibility of the author and/or advertiser, anda re not to be regarded those of the Society of Pharmaceutical Sciences of Ankara. The manuscript submitted to the Journal has the requirement of not being published previously and has not been submitted elsewhere. Manuscripts should be prepared in accordance with the requirements specified as given in detail in the section of “Information for Authors”. The submission of the manuscript to the Journal is not a condition for acceptance; articles are accepted or rejected on merit alone. All rights reserved.
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