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Abiraterone derivative with anti-cancer effect

A technology of abiraterone and its derivatives, which is applied in the field of abiraterone derivatives, can solve problems such as difficulties in the form of prodrugs, and achieve the effect of improving solubility and good stability

Inactive Publication Date: 2015-10-14
BEIJING LANG REBONE TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Finding a prodrug form that meets all criteria can be difficult

Method used

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  • Abiraterone derivative with anti-cancer effect
  • Abiraterone derivative with anti-cancer effect
  • Abiraterone derivative with anti-cancer effect

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] The compounds shown can be conveniently prepared using known organic synthesis techniques. Many specific preparation methods are published in references well known to those skilled in the art. One of the representative documents is March 1994, Advanced Organic Chemistry, Reactions, Mechanis and Structure, N.Y, McGraw Hi ll. This embodiment is specifically a synthesis step of the following structure:

[0035]

[0036] The first step: Raw material I (109 mg, 0.31 mmol) is dissolved in a mixture of acetic acid (5 mL), acetic anhydride (1.0 mL, 10.5 mmol) and DMSO (1.5 mL). The reaction was stirred at room temperature for 5 days, poured into 100 mL of water, neutralized with sodium bicarbonate, and extracted with ethyl acetate. The separated organic phase was dried with anhydrous sodium sulfate, then filtered and concentrated. It was separated by column chromatography on silica gel (hexane / ethyl acetate 2 / 1) to obtain product 1a (65 mg, yield 50%); diluted with ethyl acetate...

Embodiment 2

[0039] This example has similar synthesis steps as in Example 1. The steps for synthesizing the following structure are known to those skilled in the art to synthesize the following compounds by changing the starting materials and reaction conditions.

[0040]

[0041] (2)

Embodiment 3

[0043] This example has similar synthesis steps as in Example 1. The steps for synthesizing the following structure are known to those skilled in the art to synthesize the following compounds by changing the starting materials and reaction conditions.

[0044]

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PUM

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Abstract

The invention provides an abiraterone derivative with an anti-cancer effect. The general structural formula of the abiraterone derivative is as shown in the description. The abiraterone derivative can ensure improvement of biophysics properties such as abiraterone solubility and bioavailability; the stability of the abiraterone derivative is maintained very well during pharmaceutical manufacturing and drug administration; and after drug administration, the abiraterone derivative can be degraded and release active compounds; and the abiraterone derivative has the characteristics of low toxicity and the like.

Description

Technical field [0001] The present invention relates to pharmaceutical engineering, in particular to abiraterone derivatives with anticancer effects. Background technique [0002] Abiraterone (structure I) is a 17a-hydroxylase / C17, 201yase (CYP17Al) inhibitor, It has the characteristics of strong activity (IC50=4nM) and high selectivity; CYP17Al is an important enzyme for the biosynthesis of male hormones and estrogen in the body, and is highly expressed in cancer tissues such as testis, adrenal glands, and prostate. The role of CYP17Al is to catalyze the conversion of progresterone and prognenolone into the corresponding 17-hydroxy derivatives, and then further catalyze the conversion to andrognes dehydropiandrosterone (DEHA) and androsteredione, and DEHA is testosterone (testosterone) Biosynthetic precursors. Therefore, blocking the activity of CYP17Al will reduce the concentration of testosterone and other male hormones in prostate cancer patients and achieve the effect of i...

Claims

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Application Information

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IPC IPC(8): C07J43/00A61P35/00
CPCC07J51/00C07J43/003
Inventor 丁炬平
Owner BEIJING LANG REBONE TECH CO LTD
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