1227626-89-2Relevant academic research and scientific papers
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.
An expedient synthesis of ellipticine via Suzuki-Miyaura coupling
Konakahara, Takeo,Kiran,Okuno, Yuri,Ikeda, Reiko,Sakai, Norio
supporting information; experimental part, p. 2335 - 2338 (2010/06/13)
A simple and efficient total synthesis of ellipticine was developed via the Suzuki-Miyaura coupling of sterically sensitive 2-hydroxybenzeneboronic acid with a multifunctional aryl halide using Pd(OAc)2 as a catalyst and Cu(OAc)2·H2O as an additive in DMSO/H2O as a key step followed by double N-arylation and cyclization.
