新型PKM2抑制剂的合成及抗肿瘤活性研究

Cancer is a common and fetal disease that is a serious threat to human health. However, there is still no effective therapeutic method for treatment of cancer. Therefore, it is important to identify newtargets and develop new drugs for cancer therapeutics. M2 pyruvate kinase (PKM2) is a crucial enzyme in glycolysis that has been considered as a new target of cancer therapy. The target of this application is PKM2. A new type of target compounds as PKM2 inhibitors are designed and studied for searching new antitumor drugs. This study has the original innovation and will set up a new research direction of potential anti-tumor drugs.

肿瘤是一种严重威胁人类健康的常见病和多发病，但目前仍没有特效的治疗药物，因此研究开发新型治疗和预防肿瘤药物具有现实和重大的科学意义。M2型丙酮酸激酶（PKM2）作为肿瘤细胞糖酵解的关键酶，是最近新发现的抗肿瘤靶点，本申请以PKM2为靶点，设计了新型目标化合物作为其抑制剂，研究其合成方法、评价活性，探究结构与活性关系，寻找新的抗肿瘤药物并以此为探针进一步研究肿瘤发病机制。本研究所设计的化合物的抗肿瘤活性研究具有原始创新性，此研究将开辟一条抗肿瘤药物研究的新思路，其结果将对肿瘤发生的分子机制和新药研究均有创新性推动作用。