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Camptothecin derivative with antitumor activity

A technology of drugs and compounds, applied in the field of camptothecin derivatives

Inactive Publication Date: 2011-06-08
雷晓光 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This type of compound has not been reported at home and abroad, and it belongs to the new structure compound of invention

Method used

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  • Camptothecin derivative with antitumor activity
  • Camptothecin derivative with antitumor activity
  • Camptothecin derivative with antitumor activity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] The specific preparation method of compound 1:

[0046] Preparation of Intermediate Compound A:

[0047] 10-Hydroxycamptothecin (365mg, 1eq) was dissolved in 1,4-dioxane (5.0ml). To this solution was added N-iodosuccinimide (225mg, 1eq) at 0°C . Stir at room temperature for 3 hours. The final solution was spin-dried under vacuum, and the remaining solid was recrystallized in ethanol to obtain 400 mg of pure compound A (yield 82%).

[0048] Preparation of Intermediate Compound B:

[0049] Compound A (400mg, 1 equivalent) was dissolved in 1,4-dioxane (5.0ml), and chloromethyl methyl ether (0.2ml, 3 equivalents) was added to the solution at 0°C, and N, N' - Diisopropylethylamine (0.4ml, 3eq). Stir at room temperature for 10 hours. The final solution was spin-dried under vacuum, and the final product was separated by silica gel column chromatography to obtain 395 mg of pure compound B (90% yield).

[0050] Preparation of Intermediate Compound C:

[0051] Compound B ...

Embodiment 2

[0056] Preparation of Compound 2-3,

[0057] The preparation method is the same as in Example 1, except that the raw materials used are compounds corresponding to their respective substituents.

Embodiment 3

[0059] Preparation of Tablets Containing Compound 1

[0060]

[0061] Granulated and compressed into 1000 tablets (50mg / tablet).

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Abstract

The invention discloses a camptothecin derivative with antitumor activity; the compound has good water solubility and highly-active antitumor effect, can be administrated orally and intravenously, and is applicable to antitumor therapy.

Description

technical field [0001] The present invention relates to anticancer drug compounds, more specifically, to a new class of camptothecin derivatives with high anticancer activity and their preparation and application. Background technique [0002] Camptothecin (CPT), a pentacyclic alkaloid isolated from Camptotheca acuninata, is the only anti-cancer plant that selectively inhibits DNA topoisomerase I (Topo I) medicine. At present, camptothecin has become the second important anticancer drug derived from plants after paclitaxel in tumor treatment. [0003] Due to the high toxicity and poor curative effect of camptothecin, its clinical application is limited. Further search for camptothecin derivatives with low toxicity and high efficacy is the focus and focus of current research. The camptothecin derivatives developed in the early stage include Topotecan Top and Irinotecan CPT-11, which have low toxicity and good selectivity, especially irinotecan plays an important role in cl...

Claims

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Application Information

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IPC IPC(8): C07D491/22A61K31/4745A61P35/00
Inventor 雷晓光张秀国
Owner 雷晓光
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