Synthesis of Highly-Functional DNA Binding Indole Alkaloids and Quinolones and Their Antitumor Activity

我们成功地合成了一系列对HeLa S-3细胞具有较强抗肿瘤活性的新型β-咔啉类化合物。该化合物是一种通过与微管蛋白相互作用诱导细胞凋亡的新型抗肿瘤药物。此外，我们还成功地开发了一种利用Suzuki-Miyaura偶联反应合成椭圆碱的新方法，并开发了构建吡啶、嘧啶、吡咯、吡啶酮和喹诺酮环的新方法，有望成为新型抗肿瘤药物的骨架。

We have succeeded to develop a series of new.-carboline derivatives, which shows practically-potent antitumor activity for HeLa S-3 cell line. This compound is a new type of an antitumor agent to induce apoptosis via interaction with.-tublin. In addition, we have succeeded to develop a new and effective synthetic method for the synthesis of ellipticine using Suzuki-Miyaura coupling reaction, and to develop new methods for construction of pyridine, pyrimidine, pyrrole, pyridone, and quinolone rings, which are expected as frameworks for a new type of antitumor agents.