新型多功能香豆素的合成及抗肿瘤活性研究

IF 0.2 Q4 CHEMISTRY, MULTIDISCIPLINARY Periodico Tche Quimica Pub Date : 2020-12-20 DOI:10.52571/ptq.v17.n36.2020.886_periodico36_pgs_871_883.pdf
M. K. Bashir, Yasser Fakri Mustafa, M. Oglah
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引用次数: 20

摘要

癌症是全世界最严重的公共卫生威胁之一。合成新化合物并探索其抗肿瘤活性是解决这一健康问题的迫切需要。新支架的合成及其抗肿瘤活性评价是对抗肿瘤发展的重要途径。香豆素具有多种生物活性,其中之一就是抗肿瘤活性。本研究旨在通过席夫碱形成将香豆素前体接枝到芳香胺上合成新的香豆素,并评价其抗肿瘤活性。将一种功能化香豆素与不同的甲苯胺衍生物通过希夫碱连锁反应整合,制备了一种新的多功能香豆素(MC1-MC9)。利用FTIR, 1H-和13C- NMR进行光谱表征,确定了合成产物的化学结构。在体外对四种主要的人类癌细胞系(包括HeLa、SKG、MCF-7和AMN3)的抗肿瘤活性进行了探索。应用MTT染料进行细胞活力测定的结果表明,合成的多功能香豆素,特别是MC3,具有良好的活性。由此可见,合成的香豆素对实验细胞系的作用趋势相似,对MCF-7的作用最好,对AMN3的作用最小。该研究不仅提供了一种具有显著抗肿瘤活性的新支架,而且对其构效关系提供了一些见解。
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SYNTHESIS AND ANTITUMOR ACTIVITY OF NEW MULTIFUNCTIONAL COUMARINS
Cancer constitutes one of the most severe public health menaces worldwide. It is imperative to synthesize new compounds and explore their antitumor activity to find a potential resolution to this health problem. Synthesis of new scaffolds and evaluating their antitumor activity is a relevant approach for combating cancer development. Coumarins can exhibit diverse biological activities, and one of these is the antitumor activity. This study aimed to synthesize new coumarins by grafting their precursors to the aromatic amines via Schiff base formation and evaluating their introductory antitumor activity. New multifunctional coumarins (MC1-MC9) were prepared by integrating a functionalized coumarin with different toluidine derivatives via a Schiff-base linkage. Spectral characterization inspired by FTIR, 1H- and 13C- NMR spectroscopies has established the chemical structures of the synthesized products. The antitumor activity was explored in vitro versus four dominant human cancer lines, including HeLa, SKG, MCF-7, and AMN3. The outcomes acquired from the cell viability assay inspected by applying MTT dye have revealed that the synthesized multifunctional coumarins, particularly MC3, have a hopeful activity. It can be concluded that a similar trend of activity against the test cell lines was observed for the synthesized coumarins, with the best action being versus MCF-7 and the least one versus AMN3. This study not only affords a new scaffold of a significant antitumor activity but also provides some insights into its structureactivity relationship.
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Periodico Tche Quimica
Periodico Tche Quimica CHEMISTRY, MULTIDISCIPLINARY-
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期刊介绍: The Journal publishes original research papers, review articles, short communications (scientific publications), book reviews, forum articles, announcements or letters as well as interviews. Researchers from all countries are invited to publish on its pages.
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