Syntheses of prodelphinidin B3 and C2, and their antitumor activities through cell cycle arrest and caspase-3 activation

TETRAHEDRON

卷:69

Article

Fujii, Wataru²  Toda, Kazuya¹  Kawaguchi, Koichiro¹  Kawahara, Sei-ichi³  Katoh, Miyuki²  Hattori, Yasunao⁴  Fujii, Hiroshi¹  Makabe, Hidefumi² 

[1] Shinshu Univ, Dept Biosci & Biotechnol, Fac Agr, Nagano 3994598, Japan

[2] Shinshu Univ, Grad Sch Agr, Sci Funct Foods, Nagano 3994598, Japan

[3] St Cousair Co Ltd, Nagano 3891201, Japan

[4] Kyoto Pharmaceut Univ, Dept Med Chem, Yamashina Ku, Kyoto 6078412, Japan

关键词: Polyphenols;    Synthesis;    Natural product;    Anticancer agents;   

DOI  :  10.1016/j.tet.2013.02.087

来源: Elsevier

【 摘 要 】

Total synthesis of prodelphinidin B3 and C2 have been accomplished. The key step is Lewis acid-mediated equimolar condensations between a catechin and/or gallocatechin nucleophile and a gallocatechin electrophile. The antitumor effects of synthetic prodelphidin B3 and C2 against PC-3 prostate cancer cell lines have been investigated. Both compounds showed significant antitumor effects. Their activity was almost the same as that of EGCG, a known antitumor agent. (C) 2013 Elsevier Ltd. All rights reserved.

【 授权许可】

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