Ricci Jeremy, Min Dongguk, Oh Miyeon, Lim Hyenchong, Chung Won-Yoon, Park Kwang-Kyun, Jung Mankil
Department of Chemistry, Yonsei University, Seoul 120-749, Korea.
Med Chem. 2015;11(8):747-52. doi: 10.2174/1573406411666150514100630.
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.
道莫酮，一种诱导滞育的信息素，以及一系列脂质衍生物由道莫酮合成，以研究构效关系趋势。脂质衍生物在尿囊绒膜上表现出强大的体内抗血管生成活性，超过了作为参考药物的烟曲霉素和沙利度胺。在所测试的11种合成化合物中，新衍生物3、11和13表现出最强大的抗血管生成活性，是烟曲霉素和沙利度胺的两倍，取代它们成为已知最强大的抗血管生成药物。
