期刊文献+

Synthesis and Bioactivity of Natural Occurring Petasin-Like Derivatives as Antitumor Agents

Synthesis and Bioactivity of Natural Occurring Petasin-Like Derivatives as Antitumor Agents
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摘要 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 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.
出处 《Open Journal of Medicinal Chemistry》 2015年第2期23-31,共9页 药物化学期刊(英文)
关键词 Petasin SK-N-SH Mechanism DERIVATIVE ANTIPROLIFERATIVE Activity Petasin SK-N-SH Mechanism Derivative Antiproliferative Activity
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  • 1Roberts P J,Der C J.Targeting the Raf-MEK-ERK mitogen activated protein kinase cascade for the treatment of cancer. Oncegene . 2007
  • 2Jeremy L.Yap,Shilpa Worlikar,Alexander D.MacKerell,et al.Small-molecule inhibitors of the ERK signaling pathway:towards novel anticancer therapeutics. ChemMedChem . 2011

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