AZD5718 is a potent and selective FLAP inhibitor (IC50 = 2.0 nM) for Treatment of Coronary Artery Disease. AZD5718 demonstrated a dose dependent and greater than 90% suppression of leukotriene production over 24 h. Preclinical toxicology studies in rat and dog did not show any serious adverse events of clinical significance. Currently, AZD5718 is evaluated in a phase 2a study for treatment of coronary artery disease.
SIJ1777作为GNF-7的衍生物,对携有BRAFI II III类突变的黑色素瘤细胞展现出显著的抗癌效果。该化合物有效抑制了MEK、ERK和AKT的活化,极大地诱导了细胞凋亡(apoptosis)。此外,SIJ1777也有效阻断了带BRAFI II III突变的黑色素瘤细胞的迁移、侵袭及锚定非依赖性生长。