Therapeutics: DNA; histone deacetylase (HDAC)

Cell culture and mouse studies suggest compounds containing DNA-damaging β-carboline structures and HDAC-inhibiting hydroxamic acid groups could help treat colorectal cancer. Chemical synthesis of compounds containing both β-carboline and hydroxamic acid functional groups, followed by testing in four human colorectal cancer cell lines, yielded a compound that inhibited cell proliferation with IC50 values of 0.83-1.63 μM. In a xenograft mouse model of colorectal cancer, the compound decreased tumor growth compared with the hydroxamic acid Zolinza vorinostat. Next steps could include testing the compound in other cancer models...