Camptothecin derivative, and preparation method thereof, and pharmaceutical composition and application

US9266911B2 · kind B2 · utility

Inventors

• Wenqiang Zhou · Changsha, CN
• Jing Deng · Ann Arbor, US

Key dates

• Filing date: Dec 19, 2013
• Grant date: Feb 23, 2016
• Expiry date: Dec 19, 2033

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07F9/6561
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The present invention relates to a camptothecin derivative having a structure as represented by Formula (II), in which Xn+ is selected from H+, K+, Na+, Li+, Mg2+, Ca2+, Zn2+, Fe3+, and ammonium ion, while R1, R2, R3, and R4 independently represent a hydrogen, a hydroxyl group, a nitro group, a cyano group, a halogen, a carboxyl group, an optionally substituted amino group, a silicon-containing group, a monocyclic aryloxy group, an optionally substituted C1-C6 alkoxy group, an optionally substituted C1-C6 alkylcarbonyl group, an optionally substituted C1-C6 alkyl group, or an optionally substituted C3-C6 cycloalkyl group; alternatively, R1 and R2 are connected via one to three other atoms to form a heterocyclic ring; and in another embodiment, R3 and R4 are oxygen atoms and connected via —O—(CH2)n—O—, forming a ring, in which n=I or 2. The compound has great water-solubility, chemical stability, and great efficacy in treatment on cancer.