Isosteric analogs of lenalidomide and pomalidomide: Synthesis and biological activity

…, R Chen, L Capone, J Kang, A Parton, L Corral…

文献索引：Ruchelman, Alexander L.; Man, Hon-Wah; Zhang, Weihong; Chen, Roger; Capone, Lori; Kang, Jian; Parton, Anastasia; Corral, Laura; Schafer, Peter H.; Babusis, Darius; Moghaddam, Mehran F.; Tang, Yang; Shirley, Michael A.; Muller, George W. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 1 p. 360 - 365

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被引用次数: 18

摘要

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 ...