Unlock instant, AI-driven research and patent intelligence for your innovation.

7-position oxygen and nitrogen contained substituted camptothecin derirative and its synthesis method

A synthesis method and drug technology, applied in the direction of organic chemistry, etc., can solve the problems of poor water solubility and limited application.

Inactive Publication Date: 2005-03-23
SHAANXI JIUZHOU BIOTECH
View PDF6 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Wani and colleagues have reported that 10,11-methylenedioxycamptothecin is more potent than unsubstituted camptothecin (see W.C.Wani et al., J.Med.Chem.29, 2358 (1986) and 30 , 2317(1987)). But its water solubility is as poor as camptothecin, which greatly limits its clinical application

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 7-position oxygen and nitrogen contained substituted camptothecin derirative and its synthesis method
  • 7-position oxygen and nitrogen contained substituted camptothecin derirative and its synthesis method
  • 7-position oxygen and nitrogen contained substituted camptothecin derirative and its synthesis method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0026] Example number Compound name

[0027] 1. 7-Acetoxy-20(R,S)-camptothecin;

[0028] 2. 7-acetoxy-20(S)-camptothecin;

[0029] 3. 7-acetoxy-10-hydroxy-20(R,S)-camptothecin;

[0030] 4. 7-acetoxy-10-hydroxy-20(S)-camptothecin;

[0031] 5. 7-Acetoxy-9-dimethylaminomethyl-10-hydroxy-20(R,S)-camptothecin;

[0032] 6. 7-acetoxy-9-dimethylaminomethyl-10-hydroxy-20(S)-camptothecin;

[0033] 7. 7-Methoxy-20(R,S)-camptothecin;

[0034] 8. 7-Methoxy-20(S)-camptothecin;

[0035] 9. 7-Methoxy-10-hydroxy-20(R,S)-camptothecin;

[0036] 10. 7-Methoxy-10-hydroxy-20(S)-camptothecin;

[0037] 11. 7-Methoxy-9-dimethylaminomethyl-10-hydroxy-20(R,S)-camptothecin;

[0038] 12. 7-Methoxy-9-dimethylaminomethyl-10-hydroxy-20(S)-camptothecin;

[0039] 13. 7-(Dimethylaminomethyl)acetoxy-20-(R,S)-camptothecin;

[0040] 14. 7-(Dimethylaminomethyl)acetoxy-20-(S)-camptothecin;

[0041] 15. 7-acetamido-20(R,S)-camptothecin;

[0042] 16. 7-acetamido-20(S)-camptothecin;

[0043] 17. 7-acetamido-10-hydroxy-20(R...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

A camptothecine derivative, its pharmacologically acceptable salt, and its preparing process are disclosed. Said compound has higher water solubility and antineoplastic activity.

Description

Technical field [0001] The present invention relates to 7-position oxygen-containing and nitrogen-containing camptothecin derivatives and synthetic methods. Background technique [0002] Camptothecin is a topoisomerase I inhibitor and antitumor agent. It was first isolated from the leaves and bark of the Chinese plant Camptotheca accuminata by Wall et al. (J. Am. Chem. Soc. 88, 3888 (1966)). [0003] As shown in the figure, camptothecin is an α-pyridone ring (D) fused to the lactone ring (E), a pyrrolidine ring (C) fused to the α-pyridone ring, and pyrrole A ring system composed of alkane ring and quinoline ring (A and B). [0004] [0005] It has an asymmetric carbon in the 20 position and may form two enantiomers. But the naturally occurring compound is of the "S" type as shown above. [0006] Cytotoxic agents, i.e. chemotherapeutics, are often used to control and eradicate tumors. The cytotoxic activity of camptothecin is believed to be directly related to its potency as a t...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): C07D491/22
Inventor 刘建利
Owner SHAANXI JIUZHOU BIOTECH