The invention discloses an 8-aminoquinoline derivative, preparation thereof and application thereof to preparation of anti-malaria and anti-tumor drugs. In formula (I), R1 refers to phenyl, substituted phenyl, C5-C6 aromatic ring, C1-C10 alkyl, C1-C10 alkoxy or C1-C10 substituted alkyl, a substituting group of the substituted phenyl refers to methyl, chlorine, nitryl, fluorine or methoxyl, the substituted alkyl refers to leucine-5-azide quinoline, R2 refers to H or methyl, R3 refers to -N3, -NH2 or (formula), and R4 refers to phenyl, C5-C6 aromatic ring or C1-C10 alkyl. The 8-aminoquinoline derivative and preparation and application thereof have the advantages that simplicity, high efficiency and rapidity in operation process are achieved, raw materials are easily available, the anti-malaria activity (IC50<0.1 micrometer) of the 8-aminoquinoline derivative is improved by more than 6 times than that (IC50=0.64 micrometer) of 8-aminoquinoline, and the anti-tumor activity thereof is improved by more than 10 times than that of 8-aminoquinoline.