Synthesis of Daumone Derivatives and their Antiangiogenic Activities on Chorioallantoic Membrane
Jeremy Ricci ; Dongguk Min ; Mankil Jung ; Kwang-Kyun Park ; Won-Yoon Chung ; Hyenchong Lim ; Miyeon Oh
Medicinal Chemistry, Vol.11(8) : 747~752, 2015
Daumone, a dauer-inducing pheromone and a series of lipid derivatives were synthesized from daumone to investigate structure-activity trends. Lipid derivatives demonstrated potent in vivo antiangiogenic activity on the chorioallantoic membrane, which exceeded that of fumagillin and thalidomide as reference agents. Among the 11 synthetic compounds tested, new derivatives 3, 11 and 13 showed the most potent antiangiogenic activity, which was twice that of fumagillin and thalidomide, replacing these as the most potent known antiangiogenic agents.