Synthesis of water-soluble Irinotecan bearing symmetrically branched oligoglycerols

2016 Fiscal Year Final Research Report

• Project/Area Number: 26350502
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Biomedical engineering/Biomaterial science and engineering
• Research Institution: The University of Tokushima
• Principal Investigator: NEMOTO Hisao 徳島大学, 大学院医歯薬学研究部(薬学系), 准教授 (30208293)
• Project Period (FY): 2014-04-01 – 2017-03-31
• Keywords: 癌 / 有機合成 / 水溶性化 / イリノテカン / オリゴグリセロール

Outline of Final Research Achievements

SN38 is a basic skeleton of cancer-suspected agents, a number of derivatives have been developed and studied. A commercially available cancer-suspect agent invented in Japan, "Irinotecan", is one of them, which often have an ammonium cation moiety for their water-solubility. However, non-ionic water-soluble derivatives of SN38 has bot been developed. To design and synthesize such molecules, we examined the covalent bond formation reaction of SN38 and BGL. BGL is a glycerol oligomer, and we have now BGL003 (three glycerol units) and BGL007 (seven glycerol units). The three kinds of hybrid molecule, SN38-BGL, were synthesized. To prepare a practical amount, we developed a new preparation method for BGL, which will be published in patent soon.

Free Research Field

有機合成