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Chemistry

机译:化学

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摘要

Aspirin is a common over-the-counter drug used to treat pain, fever, and inflammation. It is one of the most widely used medications in the world with an estimated 35,000 metric tons produced and consumed annually. Recent research has shown that the regular ingestion of aspirin reduces a person's risk of developing colon cancer and even promotes colorectal tumor regression. Moreover, aspirin has a demonstrated ability to inhibit the proliferation of colorectal cancer cells in vitro. Although the mechanism of action has not yet been unequivocally established, it is clear that the synthesis of novel aspirin analogs is of medicinal interest. In this study, a library of aspirin analogs of varying degrees of hydrophobicity and steric hindrance were synthesized using salicylic acid as the molecular scaffold and a variety of acyl chlorides. These aspirin analogs will be screened against an array of cancer cell lines and will also be evaluated as antibacterial agents to determine their medicinal activity. The medicinal testing of this library of aspirin analogs will help to establish new structure-activity relationships.
机译:阿司匹林是一种常见的非处方药,用于治疗疼痛,发烧和炎症。它是世界上使用最广泛的药物之一,估计每年生产和消费35,000公吨。最近的研究表明,定期摄入阿司匹林可以降低人患结肠癌的风险,甚至可以促进结肠直肠肿瘤的消退。此外,阿司匹林具有体外抑制大肠癌细胞增殖的能力。尽管尚未明确地确定作用机理,但很明显,新型阿司匹林类似物的合成具有药用价值。在这项研究中,使用水杨酸作为分子支架和各种酰氯合成了不同程度的疏水性和空间位阻的阿司匹林类似物文库。这些阿司匹林类似物将针对一系列癌细胞系进行筛选,还将被评估为抗菌剂以确定其药用活性。阿司匹林类似物库的药物测试将有助于建立新的结构-活性关系。

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  • 来源
    《Michigan Academician》 |2018年第3期|379-384|共6页
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