TITLE:
Synthesis and Bioactivity of Natural Occurring Petasin-Like Derivatives as Antitumor Agents
AUTHORS:
Xiaolong Shi, Saiyang Zhang, Jianghao Wang, Tingyu Li, Junju Liu, Yi Hou, Lei Liu, Dongjun Fu, Haiwei Xu, Hongmin Hongmin, Yanbing Zhang
KEYWORDS:
Petasin, SK-N-SH, Mechanism, Derivative, Antiproliferative Activity
JOURNAL NAME:
Open Journal of Medicinal Chemistry,
Vol.5 No.2,
June
8,
2015
ABSTRACT: Petasin is a potential antitumor against human neuroblastoma cell SK-N-SH by inhibiting the ERK1/2 phosphorylation. In view of its great activity and new antiproliferative mechanisms, a series of petasin derivatives were designed and synthesized, which showed great antiproliferative activity. Among them compounds 1h and 1f were more effective against SK-N-SH cells than petasin with the IC50 values of 0.87 and 2.63 μM, respectively.