lonafarnib

Lonafarnib (Sch66336) 是一种可口服的 FPTase 抑制剂，作用于 H-ras、K-ras 和 N-ras，IC50分别为 1.9 nM、5.2 nM 和 2.8 nM。它具有抗肝炎三角洲病毒的活性。

(Rac)-Lonafarnib (Sch66336外消旋体) 作为Lonafarnib的外消旋体，属于一种口服有效的法尼基蛋白转移酶 (FPTase) 抑制剂，针对H-ras、K-ras及N-ras展现出杰出的抑制效能，其IC50值分别为1.9 nM、5.2 nM和2.8 nM。此外，Lonafarnib还显示出对抗肝炎三角洲病毒 (HDV) 的潜在活性。

AZD-3409 is a potent prenyl transferase inhibitor. AZD-3409 showed higher potency than lonafarnib. The mean IC(50) for cytotoxicity of AZD3409 was 510 in MEF cells, 10,600 in A549 cells and 6,170 in MCF7 cells, respectively. In these cells, the IC(50) for FTase activity of AZD3409 ranged from 3.0 to 14.2 nM and of lonafarnib from 0.26 to 31.3 nM. AZD3409 inhibits farnesylation to a higher extent than geranylgeranylation. Both inhibition of farnesylation and geranylgeranylation could not be correlated to the antiproliferative activity of the drug. AZD3409 might be active in gefitinib-resistant breast carcinoma.