Design, synthesis, antimicrobial and cytotoxicity study on human colorectal carcinoma cell line of new 4,4'-(1,4-phenylene)bis(pyrimidin-2-amine) derivatives.

Q1 Chemistry

Chemistry Central Journal Pub Date : 2018-06-25 DOI:10.1186/s13065-018-0440-3

Sanjiv Kumar, Siong Meng Lim, Kalavathy Ramasamy, Vasudevan Mani, Syed Adnan Ali Shah, Balasubramanian Narasimhan

{"title":"Design, synthesis, antimicrobial and cytotoxicity study on human colorectal carcinoma cell line of new 4,4'-(1,4-phenylene)bis(pyrimidin-2-amine) derivatives.","authors":"Sanjiv Kumar, Siong Meng Lim, Kalavathy Ramasamy, Vasudevan Mani, Syed Adnan Ali Shah, Balasubramanian Narasimhan","doi":"10.1186/s13065-018-0440-3","DOIUrl":null,"url":null,"abstract":"Background: Pyrimidine molecules attracted organic chemists very much due to their biological and chemotherapeutic importance. Their related fused heterocycles are of interest as potential bioactive molecules so, we have designed and prepared a new class of 4,4'-(1,4-phenylene)bis(pyrimidin-2-amine) molecules and screened for their in vitro antibacterial, antifungal and cytotoxicity studies.Results: The structures of synthesized bis-pyrimidine molecules were confirmed by physicochemical and spectral means. The synthesized compounds were further evaluated for their in vitro biological potentials i.e. antimicrobial activity using tube dilution method and anticancer activity against human colorectal carcinoma (HCT116) cancer cell line by Sulforhodamine B assay.Conclusions: The biological study demonstrated that compounds s7, s8, s11, s14, s16, s17 and s18 have shown more promising antimicrobial activity with best MIC values than the cefadroxil (antibacterial) and fluconazole (antifungal) and compound s3 found to have better anticancer activity against human colorectal carcinoma (HCT116) cancer cell line.","PeriodicalId":9842,"journal":{"name":"Chemistry Central Journal","volume":"12 1","pages":"73"},"PeriodicalIF":0.0000,"publicationDate":"2018-06-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1186/s13065-018-0440-3","citationCount":"11","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Chemistry Central Journal","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1186/s13065-018-0440-3","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"Chemistry","Score":null,"Total":0}

引用次数: 11

Abstract

Background: Pyrimidine molecules attracted organic chemists very much due to their biological and chemotherapeutic importance. Their related fused heterocycles are of interest as potential bioactive molecules so, we have designed and prepared a new class of 4,4'-(1,4-phenylene)bis(pyrimidin-2-amine) molecules and screened for their in vitro antibacterial, antifungal and cytotoxicity studies.

Results: The structures of synthesized bis-pyrimidine molecules were confirmed by physicochemical and spectral means. The synthesized compounds were further evaluated for their in vitro biological potentials i.e. antimicrobial activity using tube dilution method and anticancer activity against human colorectal carcinoma (HCT116) cancer cell line by Sulforhodamine B assay.

Conclusions: The biological study demonstrated that compounds s7, s8, s11, s14, s16, s17 and s18 have shown more promising antimicrobial activity with best MIC values than the cefadroxil (antibacterial) and fluconazole (antifungal) and compound s3 found to have better anticancer activity against human colorectal carcinoma (HCT116) cancer cell line.

Abstract Image

查看原文本刊更多论文

新型4,4′-(1,4-苯基)双(嘧啶-2-胺)衍生物的设计、合成、抑菌及对人大肠癌细胞系的细胞毒性研究

背景:嘧啶分子因其在生物学和化学治疗方面的重要性而受到有机化学家的广泛关注。因此，我们设计并制备了一类新的4,4′-(1,4-苯基)双(嘧啶-2-胺)分子，并对其进行了体外抗菌、抗真菌和细胞毒性研究。结果:合成的双嘧啶分子的结构通过理化和光谱手段得到了证实。采用试管稀释法对合成的化合物进行体外抑菌活性评价，并采用硫代丹胺B法对人大肠癌(HCT116)癌细胞进行抑癌活性评价。结论:生物学研究表明，化合物s7、s8、s11、s14、s16、s17和s18具有较好的抑菌活性，其MIC值优于头孢地诺酯(抗菌)和氟康唑(抗真菌)，化合物s3对人结直肠癌(HCT116)癌细胞具有较好的抑癌活性。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

求助全文

约1分钟内获得全文求助全文

来源期刊

Chemistry Central Journal 化学-化学综合

CiteScore

4.40

自引率

0.00%

发文量

审稿时长

3.5 months

期刊介绍： BMC Chemistry is an open access, peer reviewed journal that considers all articles in the broad field of chemistry, including research on fundamental concepts, new developments and the application of chemical sciences to broad range of research fields, industry, and other disciplines. It provides an inclusive platform for the dissemination and discussion of chemistry to aid the advancement of all areas of research. Sections: -Analytical Chemistry -Organic Chemistry -Environmental and Energy Chemistry -Agricultural and Food Chemistry -Inorganic Chemistry -Medicinal Chemistry -Physical Chemistry -Materials and Macromolecular Chemistry -Green and Sustainable Chemistry