Pyrazolo N-substituted dehydronorcantharidin imide derivative as well as synthesis method, activity test method and application thereof

Abstract

The invention discloses a pyrazolo N-substituted dehydronorcantharidin imide derivative as well as a synthesis method, an activity test method and application thereof, belonging to the field of cantharidin derivatives. The pyrazolo N-substituted dehydronorcantharidin imide derivative has a structural general formula shown as a formula 1: in the formula 1, R1 is H, C1, F, CH3, OCH3, OH or NO2; and R2 is 2-phenyl-2H-1,2,3-triazole-4-substituent or quinoxaline-2-substituent. The novel N-substituted dehydronorcantharidin imide derivative introduces five-membered heterocyclic pyrazole rings into norcantharidin substituted arylamine and has favorable anti-tumor activity.

Description

Technical field: The invention belongs to the field of cantharidin derivatives, and more specifically relates to a novel pyrazolo N-substituted nordehydrocantharidin imide derivative and its synthesis method, activity testing method and application. Background technique: Cantharidin (cantharidin) is a folk medicine in my country, and it is an active ingredient of a drug for treating malignant tumors. Modern studies have proved that it has a certain curative effect on primary liver cancer, and has the advantages of increasing white blood cells and not suppressing the immune system. Therefore, it has high medicinal research value and has attracted widespread attention. But the toxicity of cantharidin is bigger, and synthesis is very complicated, recent research shows, in norcantharidin (norcantharidin), two methyl groups of 2 and 3 positions are missing, and norcantharidin not only keeps strong antitumor activity and The unique effect of increasing white blood cells, and the ...

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Problems solved by technology

There can also be a double bond between 5-C and 6-C; the 7-oxygen bridge is indispensable, which may be due to the formation of hydrogen bonds between the oxygen atom and PP1 and PP2A; 2) the reduction of the anhydride on the anhydride ring will Loss of inhibition of PP1 and PP2A

The modification of cantharidin structure 5-C or 6-C generally only introduces substituents, but the results of pharmacological tests are not ideal

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