Mono- and dihydroxylated metabolites of thalidomide: synthesis and TNF-alpha production-inhibitory activity.
Mono- and dihydroxylated metabolites of thalidomide were efficiently prepared and characterized, and their inhibitory activity on tumor necrosis factor (TNF)-alpha production in the human monocytic leukemia cell line THP-1 was evaluated. 5,N-Dihydroxythalidomide was a much more potent TNF-alpha production inhibitor than thalidomide.
Nakamura
Takanori
T
Institute of Molecular and Cellular Biosciences, The University of Tokyo.
Noguchi
Tomomi
T
Kobayashi
Hisayoshi
H
Miyachi
Hiroyuki
H
Hashimoto
Yuichi
Y
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D045744:Cell Line, Tumor; D006801:Humans; D015394:Molecular Structure; D013792:Thalidomide / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors*
C516816:5,N-dihydroxythalidomide; D000970:Antineoplastic Agents; D014409:Tumor Necrosis Factor-alpha; D013792:Thalidomide