使用 Yb(OTf)3 等摩尔缩合介导合成原花青素 B2 和 B3 没食子酸酯衍生物及其抗肿瘤活性。
Syntheses of procyanidin B2 and B3 gallate derivatives using equimolar condensation mediated by Yb(OTf)3 and their antitumor activities.
机构信息
Graduate School of Agriculture, Sciences of Functional Foods, Shinshu University, 8304 Minami-Minowa Kami-Ina, Nagano 399-4598, Japan.
出版信息
Bioorg Med Chem Lett. 2013 Sep 1;23(17):4935-9. doi: 10.1016/j.bmcl.2013.06.061. Epub 2013 Jun 29.
PMID:23867167
Abstract
Synthesis of procyanidin B2 and B3 gallate derivatives, 3-O-gallate, 3"-O-gallate, and 3,3"-di-O-gallate, were synthesized using equimolar condensation mediated by Yb(OTf)3. Synthesized compounds showed significant antitumor effects against human prostate PC-3 cell lines. Their activities were weaker than well-known EGCG and prodelphinidin B3.
摘要
没食子酰基原花青素 B2 和 B3 衍生物（3-O-没食子酸酯、3"-O-没食子酸酯和 3,3"-二-O-没食子酸酯）通过 Yb(OTf)3 介导的等摩尔缩合合成。合成的化合物对人前列腺 PC-3 细胞系表现出显著的抗肿瘤作用。它们的活性弱于著名的 EGCG 和原花青素 B3。
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