Structure-Activity Relationships of the Antitumor C5-Curcuminoid GO-Y030
Abstract1,5-Bis(4-hydroxy-3-methoxyphenyl)-1,4-pentadiene-3-one (2) was isolated from Curcuma domestica as a curcumin (1)-related compound, which we named C5-curcumin. Intrigued by the potent antitumor activity of C5-curcumin (2)-related 1,5-bisaryl-1,4-pentadiene-3-ones [bis(arylmethylidene)acetones, termed C5-curcuminoids], we previously conducted a structure–activity relationship study of C5-curcuminoids and showed that highly active GO-Y030 [1,5-bis(3,5-bis(methoxymethoxy)phenyl)-1,4-pentadiene-3-one (4)] is the most promising antitumor compound. In this study, a panel of C5-curcuminoids based on GO-Y030, consisting of 30 new and 10 known compounds, was synthesized to elucidate in detail which moiety of GO-Y030 is significant for antitumor activity. The results confirmed that both the cross-conjugated dienone moiety and the 3,5-bis(methoxymethoxy) substituent are important for the antitumor activity. View Full-Text
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Kohyama, A.; Yamakoshi, H.; Hongo, S.; Kanoh, N.; Shibata, H.; Iwabuchi, Y. Structure-Activity Relationships of the Antitumor C5-Curcuminoid GO-Y030. Molecules 2015, 20, 15374-15391.
Kohyama A, Yamakoshi H, Hongo S, Kanoh N, Shibata H, Iwabuchi Y. Structure-Activity Relationships of the Antitumor C5-Curcuminoid GO-Y030. Molecules. 2015; 20(8):15374-15391.Chicago/Turabian Style
Kohyama, Aki; Yamakoshi, Hiroyuki; Hongo, Shoko; Kanoh, Naoki; Shibata, Hiroyuki; Iwabuchi, Yoshiharu. 2015. "Structure-Activity Relationships of the Antitumor C5-Curcuminoid GO-Y030." Molecules 20, no. 8: 15374-15391.