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Abstract
Erysolin and its two metabolites which were found in blood, ERY-GSH and ERY-NAC, were synthesized by alkylation, amination, isothiocyanation and oxidation reactions from 1-bromo-4-chlorobutane and sodium methyl mercaptide. The reaction temperature, time, feed ratios and purification method were also optimized. The synthesis method was simple, green, safe and low-cost. Erysolin, ERY-GSH and ERY-NAC showed good antitumor activities against MCF-7, HeLa, HepG2, A549 and SW480 cells, which suggested that the antitumor mechanism of erysolin can also be clarified from its metabolites in addition to itself.
Graphical Abstract
Disclosure statement
No potential conflict of interest was reported by the authors.
Additional information
Funding
This work was financially supported by Health Commission of Shandong Province (No. 2018WS133), Shandong Administration of Traditional Chinese Medicine (No. 2019-0350) and the Science and Technology Bureau of Tai'an City, Shandong Province, China (No. 2018NS0129).