480894

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Anticancer activity of MPT0E028, a novel potent histone deacetylase inhibitor, in human colorectal cancer HCT116 cells in vitro and in vivo.

Han-Li Huang et al.

PloS one, 7(8), e43645-e43645 (2012-08-29)

Recently, histone deacetylase (HDAC) inhibitors have emerged as a promising class of drugs for treatment of cancers, especially subcutaneous T-cell lymphoma. In this study, we demonstrated that MPT0E028, a novel N-hydroxyacrylamide-derived HDAC inhibitor, inhibited human colorectal cancer HCT116 cell growth

Accumulation of true single strand breaks and AP sites in base excision repair deficient cells.

April M Luke et al.

Mutation research, 694(1-2), 65-71 (2010-09-21)

Single strand breaks (SSBs) are one of the most frequent DNA lesions caused by endogenous and exogenous agents. The most utilized alkaline-based assays for SSB detection frequently give false positive results due to the presence of alkali-labile sites that are

Design, synthesis, and evaluation of cyclic amide/imide-bearing hydroxamic acid derivatives as class-selective histone deacetylase (HDAC) inhibitors.

Chihiro Shinji et al.

Bioorganic & medicinal chemistry, 14(22), 7625-7651 (2006-08-01)

A series of hydroxamic acid derivatives bearing a cyclic amide/imide group as a linker and/or cap structure, prepared during our structural development studies based on thalidomide, showed class-selective potent histone deacetylase (HDAC)-inhibitory activity. Structure-activity relationship studies indicated that the steric

Tetrahedron Letters, 45, 133-133 (2004)

Synthesis and biological evaluation in U87MG glioma cells of (ethynylthiophene)sulfonamido-based hydroxamates as matrix metalloproteinase inhibitors.

Elisa Nuti et al.

European journal of medicinal chemistry, 46(7), 2617-2629 (2011-04-26)

Matrix metalloproteinases (MMPs) are important factors in gliomas since these enzymes facilitate invasion into the surrounding brain and participate in neovascularization. In particular, the gelatinases (MMP-2 and MMP-9), and more recently MMP-25, have been shown to be highly expressed in

Discovery of pyrimidyl-5-hydroxamic acids as new potent histone deacetylase inhibitors.

Patrick Angibaud et al.

European journal of medicinal chemistry, 40(6), 597-606 (2005-06-01)

A series of pyrimidyl-5-hydroxamic acids was prepared for evaluation as inhibitors of histone deacetylase (HDAC). Amino-2-pyrimidinyl can be used as a linker to provide HDAC inhibitors of good enzymatic potency.

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