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发明公开
CN102204905A 8-氧-8H-苊并[1,2-b]吡咯衍生物的新用途 无效 - 驳回

8-氧-8H-苊并[1,2-b]吡咯衍生物的新用途
摘要：
本发明涉及具有如下结构的8-氧-8H-苊并[1，2-b]吡咯衍生物在制备用于治疗肿瘤的药物中的用途，尤其涉及所述衍生物在制备用于治疗结肠癌、肝癌、胃癌、宫颈癌、卵巢癌、肺癌、乳腺癌、前列腺癌、膀胱癌及血液系统肿瘤的药物中的用途。此外，本发明也涉及所述衍生物在制备FGFR1选择性抑制剂的药物中的用途。上述衍生物对多种肿瘤细胞均具有较强的抑制作用，其中部分化合物是FGFR1的选择性抑制剂，并且测试结果表明这些化合物对FGFR1的抑制活性与其结构具有一定的构效关系。此外，研究证实这类FGFR1抑制剂对血管内皮细胞的迁移、管腔形成以及鸡胚尿囊膜新生血管生成有明显抑制作用。
摘要（英）：

The invention relates to applications of 8-oxy-8H-acenaphtho (1,2-b) pyrrole derivatives with the following structures in the preparation of medicines for cancer treatment, in particular to applications of the pyrrole derivatives in the preparation of medicines for colon cancer, liver cancer, stomach cancer, cervical cancer, ovarian cancer, lung cancer, breast cancer, prostate cancer, bladder cancer and hematological malignancies. In addition, the invention relates to applications of the pyrrole derivatives in the preparation of medicines for FGFR1 selective inhibitors. The pyrrole derivatives have strong inhibition effects against a plurality of tumor cells, wherein, some compounds are Fibroblast Growth Factor Receptor (FGFR) 1 selective inhibitors, and testing results show that there is a structure-effective relationship between the inhibitory activities against FGFR1 and the structures of the compounds. The study confirms that the FGFR1 inhibitors can obviously prevent migration of vascular endothelial cells, formation of lumen and generation of newborn blood vessels of chicken chorioallantoic membrane.

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