Antitumor agents, 99. Synthetic ring C aromatized podophyllotoxin analogues as potential inhibitors of human DNA topoisomerase II

  • J Nat Prod. 1988 Sep-Oct;51(5):901-5. doi: 10.1021/np50059a014.
S A Beers  1 ,  Y Imakura ,  H J Dai ,  D H Li ,  Y C Cheng ,  K H Lee
Affiliations
  • 1. Division of Medicinal Chemistry and Natural Products, School of Pharmacy, University of North Carolina, Chapel Hill 27599.
PMID: 2849640 DOI: 10.1021/np50059a014
Abstract

Several ring C aromatized analogues of podophyllotoxin were synthesized for testing against human DNA Topoisomerase II. The results indicate that aromatization of ring C gave rise to no inhibition of this enzyme at 200 microM. A comparison of the cytotoxicity among these compounds also demonstrates that a free hydroxyl group at C-4 contributes to significant cytotoxicity.