Download MendeleyDihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone.
Kung, P.P., Funk, L., Meng, J., Collins, M., Zhou, J.Z., Johnson, M.C., Ekker, A., Wang, J., Mehta, P., Yin, M.J., Rodgers, C., Davies, J.F., Bayman, E., Smeal, T., Maegley, K.A., Gehring, M.R.(2008) Bioorg Med Chem Lett 18: 6273-6278
- PubMed: 18929486
- DOI: https://doi.org/10.1016/j.bmcl.2008.09.081
- Primary Citation of Related Structures:
3EKO, 3EKR - PubMed Abstract:
Information from X-ray crystal structures were used to optimize the potency of a HTS hit in a Hsp90 competitive binding assay. A class of novel and potent small molecule Hsp90 inhibitors were thereby identified. Enantio-pure compounds 31 and 33 were potent in PGA-based competitive binding assay and inhibited proliferation of various human cancer cell lines in vitro, with IC(50) values averaging 20 nM.
Organizational Affiliation:
Pfizer Global Research and Development, La Jolla Laboratories, 10770, Science Center Dr., San Diego, CA 92121, USA. [email protected]
