期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 1, 页码 360-365出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.10.071
关键词
Lenalidomide; Pomalidomide; Thalidomide; Tumor necrosis factor-alpha (TNF-alpha); Immunomodulatory; Anti-cancer
A series of analogs of the immunomodulary drugs lenalidomide (1) and pomalidomide (2), in which the amino group is replaced with various isosteres, was prepared and assayed for immunomodulatory activity and activity against cancer cell lines. The 4-methyl and 4-chloro analogs 4 and 15, respectively, displayed potent inhibition of tumor necrosis factor-alpha (TNF-alpha) in LPS-stimulated hPBMC, potent stimulation of IL-2 in a human T cell co-stimulation assay, and anti-proliferative activity against the Namalwa lymphoma cell line. Both of these analogs displayed oral bioavailability in rat. (C) 2012 Elsevier Ltd. All rights reserved.
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