Heterocyclic aromatic acid ester type podophyllotoxin derivatives with anti-tumor activity as well as preparation method and application

A technology of anti-tumor activity and podophyllotoxin, applied in the direction of anti-tumor drugs, organic chemistry, drug combination, etc., can solve the problems of high toxicity and side effects, easy to produce drug resistance, etc., and achieve a strong inhibitory effect
CN106008540AInactive Publication Date: 2016-10-12ZUNYI MEDICAL UNIVERSITY
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
ZUNYI MEDICAL UNIVERSITY
Publication Date
2016-10-12
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses an aromatic heterocyclic ester podophyllotoxin derivative represented by formula (I), its preparation method and its use in the preparation of antitumor drugs. The present invention combines podophyllotoxin with 4-thiazole formic acid, 1-methylpyrazole-4-formic acid, 1-methylimidazole-4-formic acid, isoquinoline-1-formic acid, 2-quinoxaline formic acid, 1- Esterification with cyclopropyl-1,4-dihydro-4-oxo-6-fluoro-7-chloroquinoline-3-carboxylic acid, 1-methylindazole-3-carboxylic acid or thioindene-2-carboxylic acid , to obtain the aromatic heterocyclic ester podophyllotoxin derivatives represented by the formula (I) with antitumor activity. In vitro cell activity experiments prove that the aromatic heterocyclic ester podophyllotoxin derivatives of the present invention can inhibit the proliferation of tumor cells, have significant antitumor activity, and are expected to be prepared as podophyllotoxin antitumor drugs.
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Description

technical field

[0001] The invention relates to a class of aromatic heterocyclic acid ester podophyllotoxin derivatives, a preparation method thereof, and an application thereof in the field of antitumor. Background technique

[0002] Podophyllotoxin is a lignan natural product isolated from podophyllum plants with significant antitumor activity. However, the clinical use of podophyllotoxin is largely limited due to its relatively large toxic and side effects and poor bioavailability. Therefore, in order to improve the activity and reduce the side effects, the structural modification and transformation of podophyllotoxin as the lead compound has attracted widespread attention, and people have successfully obtained clinical antitumor drugs such as etoposide and teniposide. However, novel podophyllotoxin-like antitumor drugs such as etoposide and teniposide still have relatively large toxic and side effects and are prone to drug resistance, so people's research on podophyllot...

Claims

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