Synthesis and antitumor activities of structure-related small molecular compounds of gambogic acid

Synthesis and antitumor activities of structure-related small molecular compounds of gambogic acid
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DOI:
10.1016/j.cclet.2007.04.010
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发表时间:
2007-06-01
影响因子:
9.1
通讯作者:
Li, Hong Yan
Li, Hong Yan
中科院分区:
化学1区
文献类型:
--
作者:
Li, Nian Guang;You, Qi Dong;Li, Hong Yan

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通过简化天然产物藤黄酸的复杂骨架,合成了色酮和呫吨酮两个系列衍生物,并通过MTT法检测了它们对多种癌细胞的体外抗肿瘤活性。结果表明,在小分子化合物中适当引入异戊二烯基团可以提高其抗肿瘤活性。合成化合物的构效关系证明藤黄酸中的桥核对于保持其抗肿瘤活性非常重要。 (C) 2007 齐东友。由Elsevier B.V.代表中国化学会出版。版权所有。
Through simplifying the complicated skeleton of the natural product gambogic acid, two series derivatives of chromone and xanthone were synthesized and examined for their antitumor activities against several cancer cells in vitro by MTT method. The results showed that appropriate introduction of prenyl group to the small molecular compounds could elevate their antitumor activities. The structure-activities relationship of synthesized compounds certified that the bridgecore in gambogic acid was very important for keeping its antitumor activities. (C) 2007 Qi Dong You. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.