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TRICYCLIC COMPOUNDS AS INHIBITORS OF THE HYPOXIC SIGNALING PATHWAY

机译:三环化合物作为低氧信号通路的抑制剂

摘要

Tricyclic compounds that selectively inhibit HIF-la activity are disclosed. Methods also are disclosed for reducing HIF-1a activity, and for inhibiting angiogenesis, tumorigenesis and/or metastasis, in a subject. In some embodiments, the tricyclic compounds surprisingly inhibit HIF-la activity at non-cytotoxic concentrations, thereby avoiding drug side effects associated with significant cytotoxicity.
机译:公开了选择性抑制HIF-1α活性的三环化合物。还公开了在受试者中降低HIF-1a活性并抑制血管生成,肿瘤发生和/或转移的方法。在一些实施方案中,三环化合物令人惊讶地在非细胞毒性浓度下抑制HIF-1α活性,从而避免了与明显的细胞毒性有关的药物副作用。

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