4-羟基香豆素衍生物的合成及其抗肿瘤活性
Synthesis and antitumor activity of 4-hydroxycoumarin derivatives.
作者信息
Jung Jae-Chul, Lee Ji-Ho, Oh Seikwan, Lee Jae-Gon, Park Oee-Sook
机构信息
Department of Medicinal Chemistry, School of Pharmacy, University of Mississippi, PO Box 1848, University, MS 38677-1848, USA.
出版信息
Bioorg Med Chem Lett. 2004 Nov 15;14(22):5527-31. doi: 10.1016/j.bmcl.2004.09.009.
A series of 4-hydroxycoumarin derivatives was prepared and evaluated for antitumor activity. The key fragments were 2a-c, 5c, 12b, 13b, 17, and 18 which were prepared via dianion ring cyclization, Friedel-Crafts acylation, and Reformatsky reaction. Compound 20b showed the most potent antitumor activity among the total 12 derivatives and compounds 19a and 19b exhibited efficacy comparable to etoposide in vitro antitumor activity.
制备了一系列4-羟基香豆素衍生物并评估其抗肿瘤活性。关键片段为2a-c、5c、12b、13b、17和18，它们通过双负离子环化、傅克酰基化和瑞福尔马斯基反应制备。化合物20b在总共12种衍生物中显示出最强的抗肿瘤活性，化合物19a和19b在体外抗肿瘤活性方面表现出与依托泊苷相当的疗效。
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