Chinese Academy of Sciences

East China Normal University

Nanjing Luyesike Pharmaceutical Co., Ltd.

Yu Luo

Jian Ding

Yi Chen

Wei Lv

Shanbao Yu

Provided are a camptothecin compound containing 7-membered lactone ring, as shown in general formula I, and pharmaceutically acceptable salt thereof, as well as the preparation method and use thereof. In general formula I, Ris H, a C1&#x2dc;C3 alkyl, acetyl or propionyl; Ris H, a C1&#x2dc;C6 alkyl, a C3&#x2dc;C6 cycloalkyl, piperidyl; or a C1&#x2dc;C6 alkyl substituted by an amino; Ris H, a C1&#x2dc;C3 alkyl, or a C1&#x2dc;C6 alkyl substituted by an amino; Ris H, a hydroxyl, or a C1&#x2dc;C6 alkoxy; Ris H, or a C1&#x2dc;C6 alkoxyl; or Rand Rare linked to each other to form &#x2014;OCHO&#x2014; or &#x2014;OCHCHO&#x2014;. The compound has good anti-tumor activity, and can be clinically used via oral administration, intravenous injection, and intramuscular injection, among others. 

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Shanghai, China

Yu Luo