{"title":"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","authors":"Mahmut Gözelle, A. Kılıç Süloğlu","doi":"10.55262/fabadeczacilik.1134520","DOIUrl":null,"url":null,"abstract":"The aim of the study was the synthesis of novel platinum compounds\nhaving benzimidazole ligands and screening for their in vitro cytotoxic\nactivity on human cervical carcinoma HeLa, human lung carcinoma\nA549, and human lung epithelial Beas-2B cell lines. 2-Substituted\nbenzimidazole ligands were synthesized by using appropriate\naldehydes and o-phenylenediamine. Subsequently, 2-substituted\nbenzimidazole ligands and potassium tetrachloroplatinate(II)\n(K2PtCl4) were used to synthesize 2-isopropylbenzimidazole\ntetrachloroplatinate(II) (K1) and 2-(1-methylpropyl)benzimidazole\ntetrachloroplatinate(II) monohydrate (K2). HRMS, IR, elemental\nanalysis, 1H-NMR, and melting point were used to characterize\nthe synthesized compounds. Cytotoxic activities against HeLa,\nA549, and Beas-2B cells after 48 h and 72 h incubation of the\nplatinum compounds were investigated via MTT assay. Cisplatin\nand carboplatin were used as reference drugs. The cytotoxic activity\nresults showed that K2 platinum compound displayed 53.42%±2.21\n(at 160 μM) on HeLa, 88.16%±0.22 (at 160 μM) on A549 and\n92.09%±0.57 (at 160 μM) on Beas-2B after 48 h incubation, K2\ndisplayed 27.42%±2.03 (at 160 μM) on HeLa, 93.95%±0.53\n(at 160 μM) on A549 and 91.99±0.22 (at 160 μM) on Beas-2B\nafter 72 h incubation. Both of the platinum compounds have higher\ncell inhibitory effects than reference drug carboplatin after 48 h incubation for tested cells.","PeriodicalId":36004,"journal":{"name":"Fabad Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2022-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis of 2-Substitutedbenzimidazolium Tetrachloroplatinate(II) Compounds and Their Cytotoxic Activities on Different Cell Lines\",\"authors\":\"Mahmut Gözelle, A. Kılıç Süloğlu\",\"doi\":\"10.55262/fabadeczacilik.1134520\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"The aim of the study was the synthesis of novel platinum compounds\\nhaving benzimidazole ligands and screening for their in vitro cytotoxic\\nactivity on human cervical carcinoma HeLa, human lung carcinoma\\nA549, and human lung epithelial Beas-2B cell lines. 2-Substituted\\nbenzimidazole ligands were synthesized by using appropriate\\naldehydes and o-phenylenediamine. Subsequently, 2-substituted\\nbenzimidazole ligands and potassium tetrachloroplatinate(II)\\n(K2PtCl4) were used to synthesize 2-isopropylbenzimidazole\\ntetrachloroplatinate(II) (K1) and 2-(1-methylpropyl)benzimidazole\\ntetrachloroplatinate(II) monohydrate (K2). HRMS, IR, elemental\\nanalysis, 1H-NMR, and melting point were used to characterize\\nthe synthesized compounds. Cytotoxic activities against HeLa,\\nA549, and Beas-2B cells after 48 h and 72 h incubation of the\\nplatinum compounds were investigated via MTT assay. Cisplatin\\nand carboplatin were used as reference drugs. The cytotoxic activity\\nresults showed that K2 platinum compound displayed 53.42%±2.21\\n(at 160 μM) on HeLa, 88.16%±0.22 (at 160 μM) on A549 and\\n92.09%±0.57 (at 160 μM) on Beas-2B after 48 h incubation, K2\\ndisplayed 27.42%±2.03 (at 160 μM) on HeLa, 93.95%±0.53\\n(at 160 μM) on A549 and 91.99±0.22 (at 160 μM) on Beas-2B\\nafter 72 h incubation. Both of the platinum compounds have higher\\ncell inhibitory effects than reference drug carboplatin after 48 h incubation for tested cells.\",\"PeriodicalId\":36004,\"journal\":{\"name\":\"Fabad Journal of Pharmaceutical Sciences\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2022-07-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Fabad Journal of Pharmaceutical Sciences\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.55262/fabadeczacilik.1134520\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"Pharmacology, Toxicology and Pharmaceutics\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Fabad Journal of Pharmaceutical Sciences","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.55262/fabadeczacilik.1134520","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"Pharmacology, Toxicology and Pharmaceutics","Score":null,"Total":0}
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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