Sulfur-substituted podophyllum derivative and synthetic method and application thereof

A podophyllotoxin and reaction technology, applied in the field of podophyllin derivatives, can solve problems such as toxic side effects and poor bioavailability, and achieve the effects of reducing toxic side effects, improving anti-tumor activity, and improving anti-tumor efficacy.
CN102757442AInactive Publication Date: 2012-10-31HUBEI UNIV OF TECH
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
HUBEI UNIV OF TECH
Publication Date
2012-10-31
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a sulfur-substituted podophyllum derivative, and a synthetic method and application thereof. Through sulfur substitution reaction, 2-mercapto-1,3,4-thiadiazole or 3-mercapto-1,2,4-triazole is respectively introduced into a C-4 site of podophyllotoxin or 4'-demethyl-epipodophyllotoxin so as to obtain the sulfur-substituted podophyllum derivative represented by a formula (V). Cell apoptosis test results of in-vitro BGC823, HepG2 and A549 tumor cell strains show that sulfur-substituted podophyllum derivative has good anti-tumor activity, high safety and low toxicity and can be prepared into clinical anticancer medicines.
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Description

technical field

[0001] The present invention relates to sulfur-substituted podophyllin derivatives, in particular to sulfur-substituted podophyllin derivatives obtained by substituting the 4-position of the C ring of podophyllotoxin or 4'-desmethyl epipodophyllotoxin and a preparation method thereof. The invention also relates to the use of the sulfur-substituted podophyllum derivatives in the preparation of antitumor drugs, which belongs to the field of podophyllum derivatives. Background technique

[0002] The structural formulas of Podophyllotoxin and 4'-Demethylepipodophyllotoxin are figure 1 Shown in the formulas (I) and (II), they are the natural antitumor activity extracts from podophyllum plants (for example: Berberidaceae plant Taoerqi, mountain lotus leaf, star anise lotus, etc.) active lead compound. However, their clinical use is limited due to their strong toxic side effects and poor bioavailability. Therefore, the research on drug development after structural...

Claims

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