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

Mono- and dihydroxylated metabolites of thalidomide: Synthesis and TNF-α production-inhibitory activity

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

Faculty of Pharmaceutical Sciences

Research output: Contribution to journal › Article › peer-review

30 Citations (Scopus)

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.

Original language	English
Pages (from-to)	1709-1714
Number of pages	6
Journal	Chemical and Pharmaceutical Bulletin
Volume	54
Issue number	12
DOIs	https://doi.org/10.1248/cpb.54.1709
Publication status	Published - 2006

Keywords

Hydroxythalidomide
Metabolite
Thalidomide
Tumor necrosis factor (TNF)-α modulator

ASJC Scopus subject areas

Chemistry(all)
Drug Discovery

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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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AU - Noguchi, Tomomi

AU - Kobayashi, Hisayoshi

AU - Miyachi, Hiroyuki

AU - Hashimoto, Yuichi

PY - 2006

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AB - 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.

KW - Hydroxythalidomide

KW - Metabolite

KW - Thalidomide

KW - Tumor necrosis factor (TNF)-α modulator

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Mono- and dihydroxylated metabolites of thalidomide: Synthesis and TNF-α production-inhibitory activity

Abstract

Keywords

ASJC Scopus subject areas

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