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Synthesis and biological activities of new tricyclic-bis-enones (TBEs)

机译:新三环双烯酮(TBEs)的合成和生物活性

摘要

This invention describes novel tricyclic-bis-enone derivatives (TBEs), such as TBE-31, TBE-34, TBE-45 and water-soluble TBEs. The methods of preparing these compounds are also disclosed. The inventors demonstrate the ability of these new TBEs to inhibit proliferation of human myeloma cells, inhibit the induction of iNOS in cells stimulated with interferon-γ, induce heme oxygenase-1 (HO-1), induce CD11b expression—a leukemia differentiation marker, inhibit proliferation of leukemia cells, induce apoptosis in human lung cancer, and induce apoptosis in other cancerous cells. The TBEs of this invention are expected to be useful agents for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.
机译:本发明描述了新颖的三环双烯酮衍生物(TBE),例如TBE-31,TBE-34,TBE-45和水溶性TBE。还公开了制备这些化合物的方法。发明人证明了这些新型TBE抑制人骨髓瘤细胞增殖,抑制干扰素-γ刺激的细胞中iNOS的诱导,诱导血红素加氧酶-1(HO-1),诱导CD11b表达(一种白血病分化标记)的能力,抑制白血病细胞的增殖,诱导人肺癌的凋亡,并诱导其他癌细胞的凋亡。预期本发明的TBE是用于治疗和预防许多疾病的有用试剂,包括癌症,神经系统疾病,炎症和涉及氧化应激的病理。

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