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Target Biopharmaceutical Technology Shenzhen Company Limited

Bo Luo

Yu Zhao

Li Hui

Haipeng Wang

Yongmei Xie

Xifei Yang

Xiangrong Song

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The invention relates to novel camptothecin derivatives and their applications, tumor cell growth inhibitors, ternary complexes, and a method for improving the solubility of the camptothecin derivatives. The camptothecin derivatives are prepared by modifying the substance shown as Formula I with glycosylated triazole at position R. In the structure shown as Formula I, Rrepresents H, Calkyl, Calkyl-D or Chaloalkyl; Rrepresents H, CHN(CH)or CHN(CD); and Rrepresents or H, wherein X represents N, O or S; and L represents polypeptide, Clinear alkyl or derivatives thereof, Clinear or branched acyl derivatives, Cethylene glycol or derivatives thereof. The camptothecin derivatives have high solubility, the anticancer drugs prepared from them have the advantages of wide anticancer spectrum and high safety, and have in vivo anticancer activity higher than irinotecan hydrochloride.

Camptothecin derivatives and preparation methods and applications thereof

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Shenzhen, China

Bo Luo