BioCentury
ARTICLE | Distillery Therapeutics

Therapeutics: An undetermined target

June 4, 2015 7:00 AM UTC

In vitro and mouse studies suggest lactam-based analogs of oleanolic acid could help treat prostate and other cancers. Chemical synthesis and in vitro testing of a series of olean-28,13β-lactams identified a lead compound that inhibited growth of human prostate, pancreatic, lung and liver cell lines with potencies comparable to CDDO-Me (IC50 values of 0.33-0.46 μM vs. 0.24-0.81 μM, respectively), but inhibited the growth of a normal human fibroblast cell line less potently than CDDO-Me (IC50 values of 6.09 and 1.86 μM, respectively). In a xenograft mouse model of prostate cancer, the lead compound decreased tumor growth compared with vehicle. Next steps could include testing the lead compound in additional models of prostate and other cancers...