1227626-89-2Relevant articles and documents
Synthesis and in vitro antitumor activity of 9-hydroxyellipticine derivatives with glucose conjugation via triazolylmethyl succinate linker
Sato, Naoya,Kawai, Yu,Akaba, Yosuke,Honma, Shoji,Sakai, Norio,Konakahara, Takeo
, p. 664 - 679 (2016)
Three types of novel 9-hydroxyellipticine derivatives 7a-c with glucose conjugation, linked by a triazolylmethyl succinic ester bond, were synthesized, and their cytotoxicity against HeLa S-3 and 293T cells was evaluated together with ellipticine (1) and 9-hydroxyellipticine (3). These new compounds 7a-c exhibited potent antitumor activity against HeLa S-3 and 293T, and water solubility of 7a was greatly higher than those of 1 and 3. The effects of an -OCH2CH2-spacer and the amino sugar moiety on the antitumor activity were examined using 7b,c. Furthermore, one of these glucose-conjugates 7a was applied to hydrolysis, catalyzed by carboxyesterase, leading to the formation of 3 under physiological conditions.