作为有前景的抗菌和抗癌药物的杂环苯并恶唑支架的设计、合成及生物活性
Design, synthesis and biological potential of heterocyclic benzoxazole scaffolds as promising antimicrobial and anticancer agents.
作者信息
Kakkar Saloni, Kumar Sanjiv, Narasimhan Balasubramanian, Lim Siong Meng, Ramasamy Kalavathy, Mani Vasudevan, Shah Syed Adnan Ali
机构信息
Faculty of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, 124001, India.
Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), 42300, Bandar Puncak Alam, Selangor Darul Ehsan, Malaysia.
出版信息
Chem Cent J. 2018 Sep 19;12(1):96. doi: 10.1186/s13065-018-0464-8.
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.
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中，使其成为一种具有多种生物活性的通用杂环化合物。
结果
通过物理化学和光谱手段确认了合成的苯并恶唑衍生物的分子结构。使用试管稀释法对合成的化合物针对选定微生物物种的体外生物活性即抗菌活性进行了进一步评估，并通过磺基罗丹明B测定法对其针对人结肠直肠癌（HCT 116）癌细胞系的抗增殖活性进行了评估。
结论
体外抗菌结果表明，化合物4、5、7和16显示出有前景的抗菌潜力。体外抗癌活性表明，与标准药物相比，化合物4和16对人结肠癌细胞系（HCT 116）显示出有前景的抗癌活性，并且这些化合物可作为进一步开发新型抗菌和抗癌药物的先导化合物。
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