Synthesis and evaluation of chromone-2-carboxamide derivatives as cytotoxic agents and 5-lipoxygenase inhibitors

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• 作者：Fatima Bousejra-ElGarah ; Barbora Lajoie…
• 关键词：Chromone carboxamides ; Cytotoxic activity ; Anti ; inflammatory effect ; Lipophilicity ; SAR
• 刊名：Medicinal Chemistry Research
• 出版年：2016
• 出版时间：November 2016
• 年：2016
• 卷：25
• 期：11
• 页码：2547-2556
• 全文大小：1,358 KB
• 刊物主题：Pharmacology/Toxicology; Biochemistry, general; Cell Biology;
• 出版者：Springer US
• ISSN：1554-8120
• 卷排序：25

文摘

In the present study, we prepared a series of 21 chromone carboxamide derivatives bearing diverse amide side chains. Their potency to inhibit the proliferation of breast (MCF-7), ovarian (OVCAR and IGROV), and colon (HCT-116) cancer cell lines, was evaluated in vitro using the MTT assay. Among these compounds, 13 showed promising cytotoxic activity against at least one cancer cell line with IC₅₀ in the range 0.9–10 μM. Our compounds were also screened for their anti-inflammatory activity as putative inhibitors of 5-lipoxygenase.