Provided are a novel derivative of β-apopicropodophyllin and a method of preparing the same, and more particularly, a compound represented by Formula 1 below, which is a novel derivative of β-apopicropodophyllin derived from podophyllotoxin, which is an anticancer agent, a method of preparing the same, and a composition for treating cancer, which includes the compound. In Formula 1, R is a C2 to C10 alkyl group, a C2 to C10 alkyl group containing an allyl- or alkyne, a —[CH2]n—C3 to C8 cycloalkyl group, a substituted or unsubstituted —[CH2]n-phenyl group, a substituted or unsubstituted —[CH2]n—C5 to C6 heteroaromatic group, a —C(═O)—C1 to C8 alkyl group, a substituted or unsubstituted —C(═O)—[CH2]n-phenyl group, or a substituted or unsubstituted —C(═O)—[CH2]n—C5 to C6 heteroaromatic group, wherein n is an integer of 0 to 6.