Angibaud P.,Ortho Biotech Oncology Research and Development |
Emelen K.V.,Johnson and Johnson Pharmaceutical Research and Development J and JPRD |
Decrane L.,Ortho Biotech Oncology Research and Development |
Brandt S.v.,Johnson and Johnson Pharmaceutical Research and Development J and JPRD |
And 23 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2010
Pursuing our efforts in designing 5-pyrimidylhydroxamic acid anti-cancer agents, we have identified a new series of potent histone deacetylase (HDAC) inhibitors. These compounds exhibit enzymatic HDAC inhibiting properties with IC50 values in the nanomolar range and inhibit tumor cell proliferation at similar levels. Good solubility, moderate bioavailability, and promising in vivo activity in xenograft model made this series of compounds interesting starting points to design new potent HDAC inhibitors. © 2009 Elsevier Ltd. All rights reserved.