Author(s)

Xiaolong Shi^1,2, Saiyang Zhang^1,2, Jianghao Wang^1,2, Tingyu Li^1,2, Junju Liu^1,2, Yi Hou^1,2, Lei Liu^1,2, Dongjun Fu^1,2, Haiwei Xu^1,2, Hongmin Hongmin^1,2, Yanbing Zhang^1,2*

¹School of Pharmaceutical Science, Zhengzhou University, Zhengzhou, China.
²Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, Zhengzhou, China.

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.

Petasin, SK-N-SH, Mechanism, Derivative, Antiproliferative Activity

Shi, X. , Zhang, S. , Wang, J. , Li, T. , Liu, J. , Hou, Y. , Liu, L. , Fu, D. , Xu, H. , Hongmin, H. and Zhang, Y. (2015) Synthesis and Bioactivity of Natural Occurring Petasin-Like Derivatives as Antitumor Agents. Open Journal of Medicinal Chemistry, 5, 23-31. doi: 10.4236/ojmc.2015.52003.