Your browser version may not work well with NCBI's Web applications. More information here...
1: Bioorg Med Chem Lett. 2005 Jun 15;15(12):2966-9.Click here to read Links

Synthetic lanostane-type triterpenoids as inhibitors of DNA topoisomerase II.

Wada S, Tanaka R.

Laboratory of Medicinal Chemistry, Osaka University of Pharmaceutical Sciences, 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan. wada@gly.oups.ac.jp

DNA topoisomerase (Topo) II is one of the target enzymes for chemotherapeutic drug development. Lanostane-type triterpenoids with various functional groups (-Cl, -Br, -OMe, -CHO, -CN, -COOH, and -COOMe) at C-2 were synthesized from 3-oxolanost-9(11)-en-24S,25-diol (9) isolated from Pinus luchuensis and their inhibitory effects on Topo II activity and cytotoxic activities against A549 cells were examined. All the derivatives showed Topo II inhibitory effects with IC50 values ranging from 1.86 to 149.97 microM and cytotoxic activities with ED50 values ranging from 3.96 to 38.15 microM.

PMID: 15914002 [PubMed - indexed for MEDLINE]