Mono- and Dihydroxylated Metabolites of Thalidomide: Synthesis and TNF-α Production-Inhibitory Activity

Takanori Nakamura; Tomomi Noguchi; Hisayoshi Kobayashi; Hiroyuki Miyachi; Yuichi Hashimoto

doi:10.1248/cpb.54.1709

Regular Articles

Mono- and Dihydroxylated Metabolites of Thalidomide: Synthesis and TNF-α Production-Inhibitory Activity

Takanori Nakamura, Tomomi Noguchi, Hisayoshi Kobayashi, Hiroyuki Miyachi, Yuichi Hashimoto

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Keywords: thalidomide, hydroxythalidomide, metabolite, tumor necrosis factor (TNF)-α modulator

JOURNAL FREE ACCESS

2006 Volume 54 Issue 12 Pages 1709-1714

DOI https://doi.org/10.1248/cpb.54.1709

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Abstract

Mono- and dihydroxylated metabolites of thalidomide were efficiently prepared and characterized, and their inhibitory activity on tumor necrosis factor (TNF)-α production in the human monocytic leukemia cell line THP-1 was evaluated. 5,N-Dihydroxythalidomide was a much more potent TNF-α production inhibitor than thalidomide.

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