【摘 要】
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Oridonin(1),a complex ent-kaurane diterpenoid isolated from traditional Chinese herb Rabdosia rubescens,has demonstrated great potential in the treatment of various human cancers due to its unique and
【机 构】
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CAS Key Laboratory of Receptor Research,and Synthetic Organic & Medicinal Chemistry Laboratory(SOMCL
【出 处】
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全国药物化学学术会议暨第四届中英药物化学学术会议
论文部分内容阅读
Oridonin(1),a complex ent-kaurane diterpenoid isolated from traditional Chinese herb Rabdosia rubescens,has demonstrated great potential in the treatment of various human cancers due to its unique and safe anticancer pharmacological profile.However,the clinical development of 1 for cancer therapy has been hampered by its relatively moderate potency,limited aqueous solubility and bioavailability.To date,little chemical effort has been directed toward structural modifications of the oridonin A-ring to generate the diversity,likely owing to the synthetic challenges arising from its structural complexity with multiple reactive functionalities.Herein,we report the rational design,expeditious synthesis and anticancer activity of novel oridonin derivatives.A series of efficient synthetic approaches based on the unique scaffold of 1 have been well established to readily access a number of structurally diverse derivatives.
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