Novel tryptanthrin derivative, synthetic method and medicinal application thereof

2015 
The invention relates to a novel tryptanthrin (indole[2,1-b] quinazoline-6,12-diketone) derivative, a synthetic method and a medicinal application thereof. A general structural formula is as follows (see the description). The novel tryptanthrin derivative is synthesized through biomimetic synthesis, the general chemical structural formula of the novel derivative is shown in Figure 1, wherein in the formula, R,R1,R2,R3 are halogen, nitro, amido, hydroxy, alkyl, alkoxy and aryl, R1is morpholine, piperidine, N-methylpiperidine, N-ethylpiperidine, isonipecotic acid, piperazine, 1-(2-pyridyl) piperazine, dimethylamine, diethylamine, 1-(2-ethoxy) piperazine and 1-(2-furoyl) piperazine, and an o-aminobenzoic acid derivative reacts with an indole quinone derivative in solvents of methylbenzene, methyl alcohol, ethyl alcohol, dichloromethane, isopropanol and the like, so as to prepare the novel tryptanthrin derivative. The novel tryptanthrin derivative which has a good inhibiting effect and a good antibacterial effect on cancer cells is preliminarily screened through an MTT experiment and an antibacterial experiment, and the medicine has pharmacological effects in the aspects of tumor resistance, antibiosis and inflammation diminishing.
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