Design, synthesis, and biological evaluation of angiogenesis inhibitors: Aromatic enone and dienone analogues of curcumin
Design, synthesis, and biological evaluation of angiogenesis inhibitors: Aromatic enone and dienone analogues of curcumin
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DOI：
10.1016/s0960-894x(02)00832-6
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发表时间：
2003-01-06
影响因子：
2.7
通讯作者：
Bowen, JP
中科院分区：
文献类型：
--
作者：
Robinson, TP;Ehlers, T;Bowen, JP
寻找新的抗肿瘤化合物是世界各地许多实验室正在进行的研究工作。小分子血管生成抑制剂的使用有望成为癌症治疗和预防的潜在有效方法。许多抗血管生成化合物正处于实验室评估和临床试验的不同阶段。姜黄素是一种天然产物，具有有效的抗血管生成特性。基于使用标准药物设计概念的简单药效团模型，制备和/或商业获得姜黄素的芳香烯酮和芳香二烯酮类似物。通过体外 SVR 测定筛选这些化合物的抗血管生成特性，并发现它们可以抑制细胞增殖。 (C) 2002 Elsevier Science Ltd. 保留所有权利。
The quest to find new antitumor compounds is an ongoing research endeavor in many laboratories around the world. The use of small-molecule angiogenesis inhibitors promises to be a potentially effective method for cancer treatment and possible prevention. Many antiangiogenic compounds are in various stages of laboratory evaluations and clinical trials. Curcumin is a natural product that has exhibited potent antiangiogenic properties. Based on a simple pharmacophore model using standard drug design concepts, aromatic enone and aromatic dienone analogues of curcumin were prepared and/or obtained commercially. These compounds were screened for antiangiogenic properties via an in vitro SVR assay and were found to inhibit cell proliferation. (C) 2002 Elsevier Science Ltd. All rights reserved.