Suprafenacine

具有抗癌活性的微管蛋白聚合抑制剂(IC50=0.38μM)；抑制HeLa、Jurkat、SNU-16、MDA-MB-231、A549、SH-SY5Y、HCT15和KB-3-1细胞(IC50s=83-381.2nM)以及富含P-糖蛋白的KB-VI细胞(IC50=215.7nM)的增殖；在10μM浓度下增加JNK和Bcl-2的磷酸化并在HeLa细胞中诱导细胞凋亡和细胞周期停滞在G2/M期；在20mg/kg浓度下降低HCT15结肠腺癌小鼠异种移植模型中的肿瘤生长。An inhibitor of tubulin polymerization (IC50 = 0.38 μM) with anticancer activit; inhibits the proliferation of HeLa, Jurkat, SNU-16, MDA-MB-231, A549, SH-SY5Y, HCT15, and KB-3-1 cells (IC50s = 83-381.2 nM) and P-glycoprotein-enriched KB-VI cells (IC50 = 215.7 nM); increases phosphorylation of JNK and Bcl-2 and induces apoptosis and cell cycle arrest at the G2/M phase in HeLa cells at 10 μM; reduces tumor growth in an HCT15 colon adenocarcinoma mouse xenograft model at 20 mg/kg.分子式C16H18N4O分子量282.3O=C(N/N=C/C1=CC=C(C)C=C1)C2=NNC3=C2CCCC3