3α-Bromo-epipicropodophyllin and Its Derivatives: Novel Analogues of Podophyllotoxin with Antitumor Activities

Abstract

Abstract: 3α-bromo-epipicropodophyllin was prepared and its inhibition activities against KB cells and L1210 leukemia cells in vitro are higher than those of VP-16, a widely used drug in clinic at present. This is the first time to introduce substitution at C-3 of ring-C in the work of modifying structure of podophyllotoxin. It can be transformed easily to 4β-hydroxy-2,3-ene-apopicropodophyllin under basic condition, so that, corresponding derivatives of 2,3-ene-apopicropodophyllin with substitution on carbon-4 could be synthesized. This compound can be regarded not only as a leading compound to be modified because of its antitumor activities, but also as an intermediate for the structure transformation.

Key words: Podophyllotoxin, Podopgyllotoxin analogues, Antitumor activities

Supporting:

He Yong, Ma Weiyong, Zhang Chunnian . 3α-Bromo-epipicropodophyllin and Its Derivatives: Novel Analogues of Podophyllotoxin with Antitumor Activities[J]. .

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