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1992 Fiscal Year Final Research Report Summary

ATTEMPTS ON DECREASE IN TOXICITY OF THE CIS-PLATIN BY USING POLYMER MODIFICATION THROUGH DERIVATIZATION OF OLIGOAMINES

Research Project

Project/Area Number 03640448
Research Category

Grant-in-Aid for General Scientific Research (C)

Allocation TypeSingle-year Grants
Research Field 有機化学一般
Research InstitutionKYOTO INSTITUTE OF TECHNOLOGY

Principal Investigator

ARAKI Takeo  KYOTO INSTITUTE OF TECHNOLOGY, FACULTY OF TEXTILE SCIENCE, PROFESSOR, 繊維学部, 教授 (70028124)

Co-Investigator(Kenkyū-buntansha) HOSOYA Ken  KYOTO INSTITUTE OF TECHNOLOGY, FACULTY OF TEXTILE SCIENCE, RESEARCH ASSOCIATE, 繊維学部, 助手 (00209248)
NARITA Hiroshi  KYOTO INSTITUTE OF TECHNOLOGY, FACULTY OF TEXTILE SCIENCE, ASSOCIATE PROFESSOR, 繊維学部, 助教授 (30027875)
TANAKA Nobuo  KYOTO INSTITUTE OF TECHNOLOGY, FACULTY OF TEXTILE SCIENCE, PROFESSOR, 繊維学部, 教授 (60127165)
Project Period (FY) 1991 – 1992
KeywordsModification of cis-Platin / Non-toxic Pt complexes / Oligoamine segment / Water-soluble polyamides / Bi-functionalization of oligoamines / Polyether polyamines / Condensation polymerization / Anti-cancer drug
Research Abstract

Aimed on decreasing the severe toxicity of cis-Platin, chemical modifications of cis-Pt complex were attempted. The principal approach of our modification is the use of oligoethylenimine-containing polymeric or oligomeric ligands and syntheses of their cis-type water-soluble Pt(II)Cl_2 complexes. First of all, triethylentetramine (N4-amine) and pentaethylenhexamine (N6-amine) were protected by formaldehyde and acetaldehyde to terminally bi-functionalize these multi-functional amines. The protection methods were established to obtain high-purity bis- and tris-imidazolidyl derivatives. The protected terminally bi-functionalized N6-amine were reacted with adipoyl dichloride or succinoyl dichloride to give water-soluble linear (without crosslinking) polyamides. This procedures for the condensation polymerization were shown to applicable to ternary copolymerization using the second diamines as exemplified with hexamethylene diamine. Thus, hydrophilicity and hydrophobicity of the polyamides … More can be delicately adjusted. Deprotection gave highly water-soluble polyamides with proper degree of polymerization for the physiological applications. Similarly, the acetaldehyde-protected N4- amine was used to polyaddition reaction with a diepoxide, and showed that the oligoethylenimine segments can be incorporated in the linear polyether polyamine chains. Although the polymer itself was water-insoluble, it could be converted readily to water-soluble polymer when its salts were formed. Again, terpolymers can be prepared in the presence of the second diamines. Activated amino acids were reacted with the formaldehyde-protected N6-amine to produce diamides of N6-amine carrying bis-terminally amino acid substituents. From the water- soluble deprotected poly-or oligo-amides, water-soluble platinum(II) complexes with cisconfiguration were prepared in reasonable yields. The Pt complexes were found to be non-toxic, and showed even an indication of extension effect for the lifetime of gastronome-cancered mice. Hence, further systematic chemical modifications of cis-Pt(II) complexes with the ligands having oligoamine segments should be continued as a quite important method. Less

  • Research Products

    (10 results)

All Other

All Publications (10 results)

  • [Publications] 藤木 徹: "鎖状オリゴエチレンイミン単位を高分子主鎖に導入する方法とポリマー白金錯体形成" Polymer Preprints,Jpn.40. 2576 2578 (1991)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] T.FUJIKI: "Introduction of Linear Oligoethylene Units in the Polymer Backbone and cis-Ot Complexes" Polymer Preprints,Jpn.(English Edition). 40. E-854 E-854 (1991)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] T.FUJIKI: "Block Modification of Nylon-66 with Oligoethylenimine Segments and Their Platinum Complexes" IUPAC International Symposium on New Polymers. 53 54 (1991)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Takeo ARAKI: "Regiospecifically Incorporatod Oligoethylenimines in the Polymer Main Chain" International Symposium on Fine Chemistry and Functional Polymers. 178 179 (1992)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] 荒木 長男: "部位選択的に五員環保護したオリゴエチレンイミンとアジピン酸ジクロリドとの重縮合による水溶性ポリアミドの合成" 高分子論文集. 49. 893 898 (1992)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] 宮西 浩伸: "ポンタエチレンヘキサミンとコハク酸クロリドによる水溶性ポリアミドの合成と白金錯体形成" 日本化学会第63春季年会. (1993)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] T. Fujiki, Y. Sekido, H. Miyanishi, K. Hosoya, H. Narita, N. Tanaka, T. Araki: "Introduction of Linear Oligoethylenimine Units in the Polymer Backbone and cis-Pt Complexation" Polymer Prep. Jpn. Vol.40, No.2, E-854; No.8. 2576-2578 (1991)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] T. Fukiki, Y. Sekido, H. Miyanishi, K. Hosoya, H. Narita, N. Tanaka, T. Araki: "Block Modification of Nylon-66 with Oligoethylenimine Segments and Their Platinum Complexes" IUPAC Intern. Symp. New Polymers. 53-54 (1991)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] T. Araki, Y. Sekido, T. Fujiki, H. Miyanishi, H. Iniue: "Regiospecifically Incorporated Oligoethylenimines in the Polymer Main Chain" Intern. Symp. Fine Chem. Functional Polym. 178-179 (1992)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] T. Araki, T. Fujiki, H. Narita, N. Tanaka: "Synthesis of Water-soluble Polyamides via Polycondensation of Adipoyl Dichloride with Oligoethylenimines Site-specifically Protected by Five-Membered Rings" Kobunshi Ronbunshu. Vol.49, No.11. 893-898 (1992)

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      「研究成果報告書概要(欧文)」より

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Published: 1994-03-24  

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