Bioorganic and Medicinal Chemistry Letters p. 3331 - 3335 (2003)
Update date:2022-08-05
Topics:
Wada, Carol K.
Frey, Robin R.
Ji, Zhiqin
Curtin, Michael L.
Garland, Robert B.
Holms, James H.
Li, Junling
Pease, Lori J.
Guo, Jun
Glaser, Keith B.
Marcotte, Patrick A.
Richardson, Paul L.
Murphy, Shannon S.
Bouska, Jennifer J.
Tapang, Paul
Magoc, Terrance J.
Albert, Daniel H.
Davidsen, Steven K.
Michaelides, Michael R.
α-Keto ester and amides were found to be potent inhibitors of histone deacetylase. Nanomolar inhibitors against the isolated enzyme and sub-micromolar inhibitors of cellular proliferation were obtained. The α-keto amide 30 also exhibited significant anti-tumor effects in an in vivo tumor model.
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Doi:10.1016/S0968-0896(03)00236-0
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