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Podophyllotoxin (1), a naturally occurring aryltetralin lignans, is extracted as the main component from the roots and rhizomes of Podophyllum species such as P.hexandrum and P.peltatum, whose medicinal properties, such as cathartic, antirheumatic, antiviral and antitumor activity, have been well-recognized for centuries.Meanwhile, it also exhibited the interesting insecticidal and antifungal activities.More recently, as shown in Figure 1, the insecticidal activity of 4α-esters/alkyloxy of 2β-chloropodophyllotoxin (Ⅰ and Ⅱ), 4-aromatic esters (lll)/substituted benzenesulfonates (Ⅳ) of 4-deoxypodophyllotoxin, monomethyl phthalate derivatives (Ⅴ) of podophyllotoxin, 4α-a rylsulfonyloxybenzyloxy-2β-chloropodophyllotoxin derivatives (Ⅵ), 4α-alkyloxy/acyloxy-2-o/β-bromopodophyllotoxin derivatives (Ⅶ and Ⅺ), phenazine derivatives of 4β-acyloxypodophyllotoxin modified in the E-ring (Ⅷ), isoxazoline derivatives of podophyllotoxin (Ⅸ),4-α/β-acyloxypodophyllotoxins modified in the A and C rings (Ⅹ), and new deoxypodophyllotoxin-based phenazines (Ⅻ) has been studied in our research group, and some derivatives have showed the potent insecticidal activity.