Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10596238 | Bioorganic & Medicinal Chemistry Letters | 2013 | 6 Pages |
Abstract
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-α (TNF-α) 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.
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Alexander L. Ruchelman, Hon-Wah Man, Weihong Zhang, Roger Chen, Lori Capone, Jian Kang, Anastasia Parton, Laura Corral, Peter H. Schafer, Darius Babusis, Mehran F. Moghaddam, Yang Tang, Michael A. Shirley, George W. Muller,