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Podophyllotoxin compounds containing 1,2,4-triazone structure and application thereof
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A technology of podophyllotoxin and epipodophyllotoxin, which is applied to the pharmaceutical composition containing the compound and the field of application in medicine, and can solve the problems of easy drug resistance and large toxic and side effects
Active Publication Date: 2019-08-09
LIAONING UNIVERSITY
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However, novel podophyllotoxin antineoplastic 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 podophyllotoxin has not stopped
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Embodiment 1
[0065] Example 1: 4β-(4-methyl-3,5-dioxo-2-phenyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carboxamide )-4-deoxyepipodophyllotoxin (compound 1)
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Abstract
The invention discloses a podophyllotoxin compound containing a 1,2,4-triazone structure, and an application thereof. The compound has a structure represented by general formula (I). Podophyllotoxin derivatives containing 1,2,4-triazone, represented by the general formula (I), and pharmaceutically acceptable salts thereof have antitumor effects. In-vitro cell activity experiments prove that the podophyllotoxin derivatives containing 1,2,4-triazone have a good inhibition effect on a human chronic myelocytic leukemiacell K562, a human cervical carcinomacellHela and a human breastcancer cellMCF-7. The compounds have a good antitumor medicine exploitation and application prospect.
Description
technical field [0001] The present invention relates to novel podophyllotoxin derivatives containing 1,2,4-triazinone structure and pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof, their preparation methods and compounds containing said compounds pharmaceutical composition. The present invention also relates to the use of the compounds and their pharmaceutically acceptable salts, hydrates, solvates or prodrugs in preparing medicines for treating and / or preventing cancer. Background technique [0002] Podophyllotoxin is a class of natural products with a 2,3-butylpropyl-4-aryltetrahydronaphthalene skeleton, which is mainly isolated from the roots and stems of plants of the genusPodophyllum in the family Berberaceae, and has significant antitumor activities . However, podophyllotoxin can cause more serious adverse reactions, such as damage to normal cells, and cause gastrointestinal discomfort, etc., so that its application as an anti-tumor drug ha...
Claims
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Application Information
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