Bioorganic & medicinal chemistry letters, 2013-01, Vol.23 (1), p.360-365
2013
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Details
- Autor(en) / Beteiligte
- Titel
- Isosteric analogs of lenalidomide and pomalidomide: Synthesis and biological activity
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2013-01, Vol.23 (1), p.360-365
- Ort / Verlag
- England: Elsevier Ltd
- Erscheinungsjahr
- 2013
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- 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.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2012.10.071Titel-ID: cdi_proquest_miscellaneous_1240899305
- Format
- –
- Schlagworte
- Administration, Oral, Animals, Anti-cancer, bioactive properties, bioavailability, Cell Line, Tumor, Cell Proliferation - drug effects, chemistry, drugs, Half-Life, Humans, immunomodulation, Immunomodulatory, interleukin-2, Interleukin-2 - metabolism, Lenalidomide, Leukocytes, Mononuclear - drug effects, Leukocytes, Mononuclear - metabolism, lymphoma, Pomalidomide, Rats, Structure-Activity Relationship, T-lymphocytes, T-Lymphocytes - drug effects, T-Lymphocytes - metabolism, Thalidomide, Thalidomide - analogs & derivatives, Thalidomide - chemistry, Thalidomide - pharmacokinetics, Thalidomide - toxicity, tumor necrosis factor-alpha, Tumor Necrosis Factor-alpha - metabolism, Tumor necrosis factor-α (TNF-α)