Design, synthesis and biological potential of heterocyclic benzoxazole scaffolds as promising antimicrobial and anticancer agents.

Q1 Chemistry

Chemistry Central Journal Pub Date : 2018-09-19 DOI:10.1186/s13065-018-0464-8

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

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引用次数: 17

Abstract

Background: Benzoxazole is the most important class of heterocyclic compound in medicinal chemistry. It has been incorporated in many medicinal compounds making it a versatile heterocyclic compound that possess a wide spectrum of biological activities.

Results: The molecular structures of synthesized benzoxazole derivatives were confirmed by physicochemical and spectral means. The synthesized compounds were further evaluated for their in vitro biological potentials i.e. antimicrobial activity against selected microbial species using tube dilution method and antiproliferative activity against human colorectal carcinoma (HCT 116) cancer cell line by Sulforhodamine B assay.

Conclusion: In vitro antimicrobial results demonstrated that compounds 4, 5, 7 and 16 showed promising antimicrobial potential. The in vitro anticancer activity indicated that compounds 4 and 16 showed promising anticancer activity against human colorectal cancer cell line (HCT 116) when compared to standard drug and these compounds may serve as lead compound for further development of novel antimicrobial and anticancer agents.

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杂环苯并恶唑支架的设计、合成及生物潜力研究。

背景:苯并恶唑是药物化学中最重要的一类杂环化合物。它已被纳入许多药用化合物，使其成为一种多功能杂环化合物，具有广泛的生物活性。结果:合成的苯并恶唑衍生物的分子结构通过理化和光谱手段得到了确证。利用试管稀释法对合成的化合物进行体外生物活性评价，并利用硫代丹B法对人大肠癌(HCT 116)细胞株进行抗增殖活性评价。结论:化合物4、5、7和16具有良好的体外抗菌潜力。体外抗肿瘤活性表明，化合物4和16与标准药物相比，对人结直肠癌(HCT 116)具有较好的抗肿瘤活性，可作为开发新型抗菌和抗癌药物的先导化合物。

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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