Design, Synthesis and Biological Evaluation of Sunitinib Analogs as Novel Antiangiogenic Anticancer Agents

• Main Authors: Yen-Chiu Chen, 陳宴秋
• Other Authors: Wen-Hsin Huang
• Format: Others
• Language: zh-TW
• Published: 2010
• Online Access: http://ndltd.ncl.edu.tw/handle/56287676315278814395

碩士 === 國防醫學院 === 藥學研究所 === 98 === Nowadays, cancer is the primary cause of death in this world. Current cancer therapeutics include surgery, radiotherapy, chemotherapy, hormone therapy and target therapy. However, conventional chemotherapy does not discriminate effectively between rapidly dividing normal cells and cancer cells, leading to high toxicity. Target therapy, designed to target cancer cells and to minimize damages to normal cells, is one of novel strategies for cancer therapeutics. Specific target therapy has been identified as selective treatments for cancer cells. Anti-angiogenesis is one of target therapies as a strategy for cancer therapeutics. At present, antiangiogenic agents can be categorized into five categories according their mode of action. Among them, sunitinib is a novel receptor tyrosine kinase inhibitor. Regarding sunitinib as the lead compound, we synthesized a series of sunitinib analogs for biological evaluations. Preliminary results showed that 14a, 15a, 15b, 15c, 16a, 16b, 16c, 17, 18 and 19 have good anti-angiogenesis activities.