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Camptothecin tenth-position cholic acid coupling compound and preparation method thereof

A technology of camptothecin and cholic acid, applied in the field of camptothecin 10-position cholic acid conjugate and preparation thereof, can solve the problems of low bioavailability, poor targeting, large toxic and side effects, etc. The effect of reducing toxicity and increasing bioavailability

Inactive Publication Date: 2012-07-04
NORTHEAST FORESTRY UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The object of the present invention is to provide a kind of pharmacological activity that fully maintains camptothecin antitumor, solves its poor targeting, low bioavailability, large toxic and side effects, etc., improves the targeting of camptothecin derivatives, reduces toxicity side effect

Method used

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Examples

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Embodiment 1

Embodiment 2

Embodiment 3

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PUM

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Abstract

The invention relates to camptothecin derivative of formula (I) and drugs thereof, in particular to a preparation method of a compound, and application of the compound serving as the drugs for treating tumors. In the formula (I), R1 is hydrogen and ethyl; R2 is hydrogen and nitryl; and R3 and R4 are hydrogen and hydroxyl.

Description

technical field The invention relates to a preparation method of a class of camptothecin derivatives and their application in antitumor therapy. Background technique In 1966, camptothecin was discovered by American scientist Monroe E.Wall et al. who studied natural products for its remarkable anti-tumor activity. In the past 38 years, medicinal chemists have worked on the structural modification of camptothecin. A lot of work, the United States, Japan, the United Kingdom, Canada and other countries have actively invested in the research and development of camptothecin derivatives, and have made great achievements. A large number of camptothecin derivatives have been designed and synthesized, and two camptothecin derivatives have been successively Alkaline derivatives Topotecan and Irinotecan have been approved as anti-tumor drugs and have been marketed around the world, and other dozen camptothecin derivatives are in different stages of clinical research and development. Ca...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J43/00A61K31/585A61P35/00
Inventor 李庆勇祖元刚赵腾飞高文轻张宝友张黎朱翘楚孙佰贺
Owner NORTHEAST FORESTRY UNIVERSITY