Chemical Pharmaceutics Oriented Research on Medicinal Chemistry

2007 Fiscal Year Final Research Report Summary

• Project/Area Number: 17590099
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Single-year Grants
• Section: 一般
• Research Field: Drug development chemistry
• Research Institution: Tokyo University of Pharmacy and Life Science (2007); Kyoto Pharmaceutical University (2005-2006)
• Principal Investigator: HAYAHI Yoshio Tokyo University of Pharmacy and Life Science, School of Pharmacy, Professor (10322562)
• Project Period (FY): 2005 – 2007
• Keywords: Chemical Pharmaceutics / Pharmaceutical Science / Prodrug / Organic Chemistry / Cancer / Taxiods / Oligo arginine / Lactic polymer

Research Abstract

Much like conventional pharmaceutics, chemical pharmaceutics deals with the delivery of drugs. However, contrary to conventional pharmaceutics that focused on formulation techniques, chemical pharmaceutics delivers drugs using techniques based on organic chemistry. We developed water-soluble prodrugs based on intramolecular migration reaction in sparingly-water-soluble protease inhibitors and taxoids. Additionally, a new anticancer drug was developed from a structure-activity relationship study of phenylahistin derivatives based on cytotoxic activity derived from anti-microtubule activity and vascular disrupting activity. Furthermore, a novel oligoarginine-based cargo-transporter system for effective intestinal absorption of drugs was developed by applying a new chemical-triggered self-cleavable peptide spacers, and also new lactic acid polymer for better introduction of drugs to the targeted tissues.

Research Products

• [Journal Article] Development of new photoresponsive paclitaxel prodrug (2008)
  • Author(s): Noguchi, M., Skwarczynnski, Y., Hirota, S., 他4名
  • Journal Title: Peptide Science 2007 Pages: 493-496
  • Description: 「研究成果報告書概要(和文)」より
• [Journal Article] Development of novel water-soluble photocleavable protective group and its application for design of photoresponsive paclitaxel prodrugs (2008)
  • Author(s): Noguchi, M., Skwarczynnski, Y., Hirota, S., 他4名
  • Journal Title: Bioorg.Med.Chem. 16 Pages: 5795-5802
  • Description: 「研究成果報告書概要(和文)」より
  • Peer Reviewed
• [Journal Article] Development of new photoresponsive paclitaxel prodrug (2008)
  • Author(s): Noguchi, M., Skwarczynski, M., Prakash, H., Hirota, S., Kimura, T., Hayashi, Y., Kiso, Y
  • Journal Title: Peptide Science 2007, S. Aimoto and S. Ono (Eds.), The Japanese Peptide Society Pages: 493-496
  • Description: 「研究成果報告書概要(欧文)」より
• [Journal Article] Development of novel water-soluble photocleavable protective group and its application for design of photoresponsive paclitaxel prodrugs (2008)
  • Author(s): Noguchi, M., Skwarczynski, M., Prakash, H., Hirota, S., Kimura, T., Hayashi, Y., Kiso, Y
  • Journal Title: Bioorg. Med Chem 16 Pages: 5795-5802
  • Description: 「研究成果報告書概要(欧文)」より
• [Journal Article] Development of oligoarginine-drug conjugates linked to new peptidic self-cleavable spacers toward effective intestinal absorption (2007)
  • Author(s): Hayashi, Y., Takayama, K., 他6名
  • Journal Title: Bioorg.Med.Chem.Lett. 17 Pages: 5129-5132
  • Description: 「研究成果報告書概要(和文)」より
  • Peer Reviewed
• [Journal Article] Application of O-N intramolecular carbon-carbamate migration:Migration of protective groups in amino acids and water-soluble prodrug strategy (2007)
  • Author(s): Skwarczynnski, M., Sohma, Y., Noguchi, M., 他3名
  • Journal Title: PEPTIDES 2006 17 Pages: 5129-5132
  • Description: 「研究成果報告書概要(和文)」より
  • Peer Reviewed
• [Journal Article] Development of first photoactivated prodrugs ofpaclitaxel via modification of henylisoserine moiety (2007)
  • Author(s): Skwarczynnski, Y., Noguchi, M., Hirota, S., 他4名
  • Journal Title: PEPTIDES 2006 2006 Pages: 214-215
  • Description: 「研究成果報告書概要(和文)」より
  • Peer Reviewed
• [Journal Article] Development of first Photoresponsive prodrug of Paclitaxel via Modification of Phenylisoserine moiety (2007)
  • Author(s): Skwarczynnski, Y., Noguchi, M., Hirota, S., 他4名
  • Journal Title: Peptide Science 2007 Pages: 251-252
  • Description: 「研究成果報告書概要(和文)」より
• [Journal Article] New aspects of potent anti-microtubule agents phenylahistin and tubulin photoaffinity labeling (2007)
  • Author(s): Hayashi, Y., Takayama, K., 他5名
  • Journal Title: Peptide Science 2007 Pages: 116
  • Description: 「研究成果報告書概要(和文)」より
• [Journal Article] Development of oligoarginine-drug conjugates linked to new peptidic self-cleavable spacers toward effective intestinal absorption (2007)
  • Author(s): Hayashi, Y., Takayama, K., Suehisa, Y., Fujita, T., Nguyen, J-T., Futaki, S., Yamamoto, A., Kiso, Y
  • Journal Title: Bioorg. Med. Chem. Lett 17-18 Pages: 5129-5132
  • Description: 「研究成果報告書概要(欧文)」より
• [Journal Article] Application of O-N intramolecular carbon-carbamate migration Migrationof protective groups in amino acids and water-soluble prodrug strategy (2007)
  • Author(s): Skwarczynnski, M., Sohma, Y., Noguchi, M., Kimura, T., Hayashi, Y., Kiso, Y
  • Journal Title: PEPTIDES 2006, Rolka, K., Rekowski, P., Silberring, J. (Eds.), Proceedings of the twenty-ninth European Peptide Symposium Pages: 204-205
  • Description: 「研究成果報告書概要(欧文)」より
• [Journal Article] Development of first photoactivated prodrug of paclitaxel via modification of phenylisoserine moiety (2007)
  • Author(s): Skwarczynnski, M., Noguchi, M., Hirota, S., Shoma, Y., Kimura, T., Hayashi, Y., Kiso, Y
  • Journal Title: PEPTIDES 2006, Rolka, K., Rekowski, P., Silberring, J. (Eds.), Proceedings of the twenty-ninth European Peptide Symposium Pages: 214-215
  • Description: 「研究成果報告書概要(欧文)」より
• [Journal Article] Phototaxel : Development of first Photoresponsive prodrug of Paclitaxel via Modification of Phenylisoserine moiety (2007)
  • Author(s): Skwarczynski, M. ; Noguchi, M. ; Hirota, S. ; Sohma, Y. ; Kimura, T. ; Hayashi, Y. ; Kiso, Y
  • Journal Title: Peptide Science 2006, H. Ishida and H. Mihara (Eds.), The Japanese Peptide Society Pages: 251-252
  • Description: 「研究成果報告書概要(欧文)」より
• [Journal Article] Design and synthesis of oligo(D-arginine)-fluorescein conjugates possessing novel self-cleavable spacers as a model for effective intestinal absorption (2007)
  • Author(s): Hayashi, Y., Takayama, K., Suehisa, Y., Fujita, T., Yamamoto, A., Futaki, S., Kiso, Y
  • Journal Title: Peptide Science 2006, H. Ishida and H. Mihara (Eds.), The Japanese Peptide Society Pages: 116
  • Description: 「研究成果報告書概要(欧文)」より
• [Journal Article] Development of Wang Resin Supported Evans-type Oxazolidinone for Asymmetric Reaction (2006)
  • Author(s): Tomoya Kotake, Yoshio Hayashi, 他3名
  • Journal Title: PEPTIDES 2006 Pages: 96-97
  • Description: 「研究成果報告書概要(和文)」より
  • Peer Reviewed
• [Journal Article] O-N Intramolecular alkoxycarbonyl migration of typical protective groups in hydroxyamino acids (2006)
  • Author(s): M. Skwarczynski, Y. Sohma, Y. Hayashi, 他4名
  • Journal Title: Journal of Organic Chemistry 71 Pages: 2542-2545
  • Description: 「研究成果報告書概要(和文)」より
  • Peer Reviewed
• [Journal Article] Development of first photoresponsive prodrug of paclitaxel (2006)
  • Author(s): Skwarczynski, M., Hayashi, Y., Kiso, Y., 他4名
  • Journal Title: Bioorg.Med.Chem.Lett. 16 Pages: 4492-4496
  • Description: 「研究成果報告書概要(和文)」より
  • Peer Reviewed
• [Journal Article] 0-N Intramolecular Acyloxy Migration Reaction:from the Prodrug to the Migration of Protective Groups in Amino Acids (2006)
  • Author(s): Skwarczynski, M., Hayashi, Y., Kiso, Y., 他5名
  • Journal Title: Peptide Science 2006 Pages: 169-172
  • Description: 「研究成果報告書概要(和文)」より
• [Journal Article] Synthesis ofglutamic acid and glutamine peptides possessing a trifluoromethyl ketone group as SARS-CoV 3CL rotease inhibitors (2006)
  • Author(s): Sydnes, M.S., Hayashi, Y., 他6人
  • Journal Title: Tetrahedron 62・36 Pages: 8601-8609
  • Description: 「研究成果報告書概要(和文)」より
  • Peer Reviewed
• [Journal Article] Application of intramolecular carbonate-carbamate migration (2006)
  • Author(s): Skwarczynski, M., Hayashi, Y., Kiso, Y., 他3名
  • Journal Title: Chemistry Today 24 Pages: 30-32
  • Description: 「研究成果報告書概要(和文)」より
  • Peer Reviewed
• [Journal Article] Paclitaxel Prodrugs:Toward Smarter Delivery of Anticancer Agents (2006)
  • Author(s): Skwarczynski, M., Hayashi, Y., Kiso, Y.
  • Journal Title: J.Med.Chem. 49・25 Pages: 7253-7269
  • Description: 「研究成果報告書概要(和文)」より
  • Peer Reviewed
• [Journal Article] O-N intramolecular alkoxycarbonyl migration of typical protective groups in hydroxyamino acids (2006)
  • Author(s): Skwarczynski, M., Sohma, Y., Noguchi, M.,Kimura, T., Hayashi, Y., Kiso, Y
  • Journal Title: J. Org. Chem 71-6 Pages: 2542-2545
  • Description: 「研究成果報告書概要(欧文)」より
• [Journal Article] Development of first photoresponsive prodrug of pachtaxel (2006)
  • Author(s): Skwarczynski, M., Noguchi, M., Hirota, S., Sohma, Y., Kimura, T., Hayashi, Y., Kiso, Y
  • Journal Title: Bioorg. Med. Chem Lett 16-17 Pages: 4492-4496
  • Description: 「研究成果報告書概要(欧文)」より
• [Journal Article] O-N Intramolecular Acyloxy Migration Reaction : from the Prodrug to the Migration of Protective Groups in Amino Acids (2006)
  • Author(s): Skwarczynski, M., Shoma, Y., Noguchi, M., Kimura, M., Hayashi, Y., Hamada, Y., Kimura, T., Kiso, Y
  • Journal Title: Peptide Science 2005, T. Wakamiya (Ed.), The Japanese Peptide Society Pages: 169-172
  • Description: 「研究成果報告書概要(欧文)」より
• [Journal Article] Paclitaxel Prodrugs : Toward Smarter Delivery of Anticancer Agents (2006)
  • Author(s): Skwarczynski, M., Hayashi, Y., Kiso, Y
  • Journal Title: J. Med. Chem 49-25 Pages: 7253-7269
  • Description: 「研究成果報告書概要(欧文)」より
• [Journal Article] Synthesis of glutamic acid and glutamine peptides possessing a trifluoromethyl ketone group as SARS-CoV 3CL protease inhibitors (2006)
  • Author(s): Sydnes, M., S., Hayashi, Y., Sharma, V. K., Hamada, T., Bacha, U., Barrila, J., Freire, E., Kiso, Y
  • Journal Title: Tetrahedron 62-36 Pages: 8601-8609
  • Description: 「研究成果報告書概要(欧文)」より
• [Journal Article] Application of mtramolecular carbonate-carbamate migration (2006)
  • Author(s): Skwarczynski, M., Noguchi, M., Sohma, Y., Kimura, T., Hayashi, Y., Kiso, Y
  • Journal Title: Chemistry Today 24-6 Pages: 30-32
  • Description: 「研究成果報告書概要(欧文)」より
• [Journal Article] No auxiliary, no byproduct strategy for water-soluble prodrugs of taxoids:scope and limitation おf O-N intramolelcular acyl and acyloxy migration reaction (2005)
  • Author(s): M.Skwarczynski, Y.Sohma, Y.Hayashi, 他5名
  • Journal Title: Journal of Medicinal Chemistry 48 Pages: 2655-2666
  • Description: 「研究成果報告書概要(和文)」より
  • Peer Reviewed
• [Journal Article] Design and Synthesis of a New Polymer-supported Evans-type Oxazolidinone:An Efficient Chiral Auxiliary in the Solid-hase Asymmetric Alkylation Reactions (2005)
  • Author(s): T. Kotake, Y. Hayashi, 他5名
  • Journal Title: Tetrahedron 61 Pages: 3819-3833
  • Description: 「研究成果報告書概要(和文)」より
  • Peer Reviewed
• [Journal Article] O-N Intramolecular acyl acyloxy migration reaction in the development of water-soluble prodrugs of taxoids (2005)
  • Author(s): M. Skwarczynski, Y. Sohma, Y. Hayashi, 他5名
  • Journal Title: Peptide Science 2004 Pages: 309-312
  • Description: 「研究成果報告書概要(和文)」より
• [Journal Article] Conversion ofpolymer-bound dipeptide to Evans-type chhal auxiliary:a new tool for efficient solid-hase asymmetric reactions (2005)
  • Author(s): Tomoya Kotake, Yoshio Hayashi, 他3名
  • Journal Title: Peptide Science 2004 Pages: 629-632
  • Description: 「研究成果報告書概要(和文)」より
• [Journal Article] No Auxiliary, No Byproduct Strategy for Water-soluble Prodrugs of Taxoids Scope and Limitation of O-N Intramolecular Acyl and Acyloxy Migration Reaction (2005)
  • Author(s): Skwarczynski, M., Sohma, Y., Noguchi, M., Kimura, M., Hayashi, Y., Kimura, T., Kiso, Y
  • Journal Title: J Med Chem 48-7 Pages: 2655-2666
  • Description: 「研究成果報告書概要(欧文)」より
• [Journal Article] Design and Synthesis of a New Polymer-supported Evans-type Oxazolidinone : An Efficient Chiral Auxiliary in the Solid-phase Asymmetric Alkylation Reactions (2005)
  • Author(s): Kotake, T., Hayashi, Y., Rajesh, S., Mukai, Y., Takiguchi, Y., Kimura, T., Kiso, Y
  • Journal Title: Tetrahedron 61-15 Pages: 3819-3833
  • Description: 「研究成果報告書概要(欧文)」より
• [Journal Article] O-N Intramolecular acyl amd acyloxy migration reaction in the development of water-soluble prodrugs of taxoids (2005)
  • Author(s): Skwarczynski, M., Sohma, Y., Noguchi, M., Kimura, M., Hayashi, Y., Hamada, Y., Kimura, T., Kiso, Y
  • Journal Title: Peptide Science 2004, Y. Shimohigashi (Ed.), The Japanese Peptide Society Pages: 309-312
  • Description: 「研究成果報告書概要(欧文)」より
• [Journal Article] Conversion of polymer-bound dipeptide to Evans-type chiral auxiliary a new tool for efficient solid-phase asymmetric reactions (2005)
  • Author(s): Kotake, T., Hayashi, Y., Takiguchi, Y., Kimura, T., Kiso, Y
  • Journal Title: Peptide Science 2004, Y. Shimohigashi (Ed.), The Japanese Peptide Society Pages: 629-632
  • Description: 「研究成果報告書概要(欧文)」より
• [Journal Article] Development of Wang Resin Supported Evans-type Oxazolidinone for Asymmetric Reaction (2005)
  • Author(s): Kotake, T., Hayashi, Y., Rajesh, S., Kimura, T., Kiso, Y
  • Journal Title: PEPTIDES, pp96-97 (2006), Proceedings of the 19th American Peptide Symposium, Sylvie E. Blondelle (Ed.) American Peptide Society
  • Description: 「研究成果報告書概要(欧文)」より
• [Presentation] 腫瘍部位特異的に再生可能なpaclitaxelの光応答性プロドラッグphototaxelの開発 (2007)
  • Author(s): 野口 真代, 林 良雄, 他5名
  • Organizer: 第26回メディシナルケミストリーシンポジウム
  • Place of Presentation: 相模大野
  • Year and Date: 2007-11-29
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] Development of new photoresponsive paclitaxel prodrug (2007)
  • Author(s): Noguchi, M., Hayashi, Y., 他5名
  • Organizer: 44th Japanese Peptide Symposium
  • Place of Presentation: Toyama
  • Year and Date: 2007-11-08
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] Photo-triggered targeting prodrug of paclitaxel (2007)
  • Author(s): Skwarczynski, M., Hayashi, Y., 他5名
  • Organizer: 2nd European Conference on Chemistry for Life Sciences
  • Place of Presentation: Wroclaw,Poland
  • Year and Date: 2007-09-06
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] Photo-triggered targeting prodrug of paclitaxel (2007)
  • Author(s): Skwarczynski, M., Noguchi, M., Hirota, S., Sohma, Y., Kimura, T., Hayashi, Y., Kiso, Y
  • Organizer: 2nd European Conference on Chemistry for Life Sciences
  • Place of Presentation: Wroclaw, Poland
  • Year and Date: 2007-09-06
  • Description: 「研究成果報告書概要(欧文)」より
• [Presentation] Synthesis of Polylactides with Side Chain Functionality : Ring-Opening Polymerization of a Homobislactone Prepared from Lysine (2007)
  • Author(s): Kodera, H., Kiso, Y., Hayashi, Y., Nishishita, N., Hirano, Y
  • Organizer: 20th American Peptide Symposium Peptides for Youth
  • Place of Presentation: Montreal, Canada
  • Year and Date: 2007-07-26
  • Description: 「研究成果報告書概要(欧文)」より
• [Presentation] 可視光線により腫瘍部位特異的にパクリタキセルを再生するプロドラッグの開発 (2007)
  • Author(s): 野口 真代, 林 良雄
  • Organizer: 第11回がん分子標的治療研究会総会POP研究
  • Place of Presentation: 大阪
  • Year and Date: 2007-07-05
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] Synthesis of Polylactides with Side Chain Functionality:Ring-Opening Polymerization of a Homobislactone Prepared from Lysine (2007)
  • Author(s): Kodera, H., Hayashi, Y., 他3名
  • Organizer: 20th American Peptide Symposium
  • Place of Presentation: Monreal,Canada
  • Year and Date: 2007-06-26
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] 側鎖にアミノ基を有するhomobislactoneを原料とするカチオン型乳酸ポリマーの合成 (2007)
  • Author(s): 林 良雄, 小寺 宏実, 他3名
  • Organizer: 日本薬学会第127年会
  • Place of Presentation: 富山
  • Year and Date: 2007-03-28
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] 0-N Intramolecular Acyl and Alkoxycarbonyl Migration Reactions:From the Prodrug Strategv to the Migration of Protective Groups in Amino Acids (2007)
  • Author(s): Skwarczynski, M., Hayashi, Y., 他4名
  • Organizer: First Indian Peptide Symposium
  • Place of Presentation: Hyderabad,India
  • Year and Date: 2007-02-22
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] O-N Intramolecular Acyl and Alkoxycarbonyl Migration Reactions From the Prodrug Strategy to the Migration of Protective Groups in Amino Acids (2007)
  • Author(s): Skwarczynski, M., Noguchi, M., Sohma, Y., Kimura, T., Hayashi, Y., Kiso, Y
  • Organizer: First Indian Peptide Symposium
  • Place of Presentation: Hyderabad, India
  • Year and Date: 2007-02-22
  • Description: 「研究成果報告書概要(欧文)」より
• [Presentation] 腫瘍部位特異的に再生可能なpaclitaxelの光応答性プロドラッグphototaxelの開発 (2007)
  • Author(s): 野口 真代, 林 良雄, 他5名
  • Organizer: 難病克服をめざした創薬科学合同研究成果発表会
  • Place of Presentation: 京都
  • Year and Date: 2007-01-26
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] Application of O-N intramolecular alkoxycarbonyl migration reaction:from prodrug strategy to migration of protective groups (2007)
  • Author(s): Skwarczynski, M., Hayashi, Y., 他4名
  • Organizer: 難病克服をめざした創薬科学合同研究成果発表会
  • Place of Presentation: 京都
  • Year and Date: 2007-01-26
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] Phototaxel : Development of first Photoresponsive Prodrug of Paclitaxel via Modification of Phenylisoserine Moiety (2006)
  • Author(s): Skwarczynski, M., Noguchi, M., Hirota, S., Sohma, Y., Kimura, T., Hayashi, Y., Kiso, Y
  • Organizer: International Conference of 43rd Japanese Peptide Symposium and 4th Peptide Engineering Meeting
  • Place of Presentation: Yokohama
  • Year and Date: 20061100
  • Description: 「研究成果報告書概要(欧文)」より
• [Presentation] アルツハイマー病・がんを標的としたペプチド基盤生物有機化学研究 (2006)
  • Author(s): 林 良雄
  • Organizer: 大阪大学蛋白質研究所セミナー
  • Place of Presentation: 吹田
  • Year and Date: 20060300
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] Chemical Phamlaceuticsを志向した創薬化学 (2006)
  • Author(s): 林 良雄
  • Organizer: 日本薬学会第126年会シンポジウム
  • Place of Presentation: 仙台
  • Year and Date: 20060300
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] フェニルイソセリン基の修飾によるpaclitaxelの光応答性プロドラッグの開発 (2006)
  • Author(s): Skwarczynski, M., Hayashi, Y., 他5名
  • Organizer: 第32回反応と合成の進歩シンポジウム
  • Place of Presentation: 広島
  • Year and Date: 2006-12-04
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] 腫瘍特異性を指向したpaclitaxelの光応答性プロドラッグphototaxelの開発 (2006)
  • Author(s): Skwarczynski, M., Hayashi, Y., 他5名
  • Organizer: 第25回メディシナルケミストリーシンポジウム
  • Place of Presentation: 名古屋
  • Year and Date: 2006-11-28
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] Toward Smarter Delivery of Paclitaxel:Application of O-N Intrmolecular Acyl and Alkoxycarbonyl Migrations (2006)
  • Author(s): Skwarczynski, M., Hayashi, Y., 他5名
  • Organizer: 2nd International symposium on Biomolecules and Related Compounds
  • Place of Presentation: Kyoto
  • Year and Date: 2006-11-11
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] Development of phototaxel : first photosensitive prodrug of paclitaxel (2006)
  • Author(s): Skwarczynski, M., Noguchi, M., Hirota, S., Sohma, Y., Kimura, T., Hayashi, Y., Kiso, Y
  • Organizer: 2nd International Symposium on Biomolecules and Related Compounds
  • Place of Presentation: Kyoto
  • Year and Date: 2006-11-11
  • Description: 「研究成果報告書概要(欧文)」より
• [Presentation] Oligoarginine prodrugs bearing self-cleavable peptide spacers for effective intestinal absorption (2006)
  • Author(s): Hayashi, Y., Takayama, 他5名
  • Organizer: 2nd International Symposium on Biomolecules and Related Compounds
  • Place of Presentation: Kyoto
  • Year and Date: 2006-11-10
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] Toward Smarter Delivery of Paclitaxel : Application of O-N Intramolecular Acyl and Alkoxycarbonyl Migrations (2006)
  • Author(s): Skwarczynski, M., Noguchi, M., Sohma, Y., Hirota, S., Kimura, T., Hayashi, Y., Kiso, Y
  • Organizer: 2nd International Symposium on Biomolecules and Related Compounds
  • Place of Presentation: Kyoto
  • Year and Date: 2006-11-10
  • Description: 「研究成果報告書概要(欧文)」より
• [Presentation] Phototaxel:Development of first Photoresponsive Prodrug of Paclitaxel via Modification of Phenylisoserine Moiety (2006)
  • Author(s): Skwarczynski, M., Hayashi, Y., 他5名
  • Organizer: International Conference of 43rd Japanese Peptide Symposium and (四)th Peptide Engineering Meeting
  • Place of Presentation: Yokohama
  • Year and Date: 2006-11-06
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] Lysから誘導したhomobislactonc体響とするカチオン型乳酸ポリマーの合成 (2006)
  • Author(s): 林 良雄, 小寺 宏実, 他2名
  • Organizer: 第56回日本薬学会近畿支部総会・大会
  • Place of Presentation: 京都
  • Year and Date: 2006-10-20
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] Intramolecular Nucleophilic Reactions in Peptide Chemistry;Application to Peptide Synthesis and Medicinal Chemistry (2006)
  • Author(s): Hayashi, Y., Sohma, Y., 他3名
  • Organizer: The 11th Akabori Conference(Japanses-German Symposium on Peptide Science)
  • Place of Presentation: Kloster Banz,Germany
  • Year and Date: 2006-09-12
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] Intramolecular Nucleophilic Reactions in Peptide Chemistry ; Application to Peptide Synthesis and Medicinal Chemistry (2006)
  • Author(s): Hayashi, Y., Sohma, Y., Taniguchi, A., Skwarczynski, M., Kiso, Y
  • Organizer: The 11th Akabon Conference (Japanese-German Symposium on Peptide Science)
  • Place of Presentation: Kloster Banz, Germany
  • Year and Date: 2006-09-12
  • Description: 「研究成果報告書概要(欧文)」より
• [Presentation] O-N intramolecular acyl and alkoxycarbonyl migrations:toward smarter delivery of paclitaxel (2006)
  • Author(s): Skwarczynski, M., Hayashi, Y., 他5名
  • Organizer: Integrated Center of Excellence for Medicinal Chemistry of Neuropeptides"From Endogenous systems to Medicines
  • Place of Presentation: Warsaw,Poland
  • Year and Date: 2006-09-09
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] O-N intramolecular acyl and alkoxycarbonyl migrations toward smarter delivery of paclitaxel (2006)
  • Author(s): Slcwarczynski, M., Noguchi, M., Sohma, Y., Hirota, S., Kimura, T., Hayashi, Y., Kiso Y
  • Organizer: Integrated Center Of Excellence For Medicinal Chemistry Of Neuropeptides "From Endogenous Systems to Medicines
  • Place of Presentation: Warsaw, Poland
  • Year and Date: 2006-09-09
  • Description: 「研究成果報告書概要(欧文)」より
• [Presentation] Synthesis of trifluoromethyl ketone-containing glutamic acid and glutamine peptides as severe acute respiratory syndrome coronavirus 3CL protease inhibitors (2006)
  • Author(s): Sydnes, M.S., Hayashi, Y., 他4人
  • Organizer: 29th European Peptide Symposium
  • Place of Presentation: Gdansk,Poland
  • Year and Date: 2006-09-05
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] Synthesis of tnfluoromethyl ketone-containing glutamic acid and glutamine peptides as severe acute respiratory syndrome coronavirus 3CL protease inhibitors (2006)
  • Author(s): Sydnes, M.O., Hayashi, Y., Sharma, V.K., Hamada, T., Bacha, U., Barrila, J., Freire, E., Kiso, Y
  • Organizer: 29th European Peptide Symposium
  • Place of Presentation: Gdansk, Poland
  • Year and Date: 2006-09-05
  • Description: 「研究成果報告書概要(欧文)」より
• [Presentation] Development of first photoactivated prodrug of paclitaxel via modification of phenylisoserine moiety (2006)
  • Author(s): Hayashi, Y., Skwarczynski, M., 他5名
  • Organizer: 29th European Peptide Symposium
  • Place of Presentation: Gdansk,Poland
  • Year and Date: 2006-09-04
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] Development of first photoactivated prodrug of paclitaxel via modification of phenylisoserine moiety (2006)
  • Author(s): Skwarczynslu, M., Noguchi, M., Hirota, S., Sohma, Y., Kimura, T., Hayashi, Y., Kiso, Y
  • Organizer: 29th European Peptide Symposium
  • Place of Presentation: Gdansk, Poland
  • Year and Date: 2006-09-04
  • Description: 「研究成果報告書概要(欧文)」より
• [Presentation] Development of resin supported Evans-type chiral auxiliary for solid-phase asymmetric reaction (2006)
  • Author(s): Y.Hayashi, T.Kotake, 他4名
  • Organizer: ICOB-5&ISCNP-25 IUPAC International Conference on Biodiversity and Natural Products
  • Place of Presentation: Kyoto,Japan
  • Year and Date: 2006-07-26
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] Development of resin supported Evans-type chiral auxiliary for solid-phase asymmetric reaction (2006)
  • Author(s): Hayashi, Y., Kotake, T., Nishiguchi, S., Rajesh, S., Kimura, T., Kiso, Y
  • Organizer: ICOB-5 & ISCNP-25 IUPAC International Conference on Biodiversity and Natural Products
  • Place of Presentation: Kyoto, Japan
  • Year and Date: 2006-07-26
  • Description: 「研究成果報告書概要(欧文)」より
• [Presentation] New approaches of microtubule targeting agents as anti-cancer drugs.International Symposium on Chemistry (2006)
  • Author(s): Hayashi, Y., Skwarczynski, M., 他2名
  • Organizer: International Symposium on Chemistry, Biology & Medicine
  • Place of Presentation: Cyprus
  • Year and Date: 2006-05-30
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] New approaches of microtubule targeting agents as anti-cancer drugs. (2006)
  • Author(s): Hayashi, Y., Skwarczynski, M., Kiso, Y., Lloyd, G.K
  • Organizer: International Symposium on Chemistry, Biology & Medicine
  • Place of Presentation: Cyprus
  • Year and Date: 2006-05-30
  • Description: 「研究成果報告書概要(欧文)」より
• [Presentation] Synthesis of peptides possessing a trifluoromethyl ketone moiety as inhibitors for severeacute respiratory syndrome coronavirus (2006)
  • Author(s): Sydnes, M.S, , Hayashi, Y., 他4人
  • Organizer: 7th Tetrahedron Symposium:
  • Place of Presentation: Kyoto,Japan
  • Year and Date: 2006-05-25
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] O-N Intramolecular carbonate-carbamate migration: from water-soluble taxoid prodrugs to migration of migration of protective groups (2006)
  • Author(s): M.Skwarczynski, Y.Hayashi, 他4名
  • Organizer: 7th Tetrahedron Symposium:
  • Place of Presentation: Kyoto,Japan
  • Year and Date: 2006-05-25
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] Synthesis of peptides possessing a trifluoromethyl ketone moiety as inhibitors for severe acute respiratory syndrome coronavirus (2006)
  • Author(s): Sydnes, M, O, Hayashi, Y, Sharma, V, K, Barrila, J, Freire, E, Kiso, Y
  • Organizer: 7th, Tetrahedron Symposium : Challenges in Organic Chemistry
  • Place of Presentation: Kyoto, Japan
  • Year and Date: 2006-05-25
  • Description: 「研究成果報告書概要(欧文)」より
• [Presentation] O-N Intramolecular carbonate-carbamate migration : from water-soluble taxoid prodrugs to migration of protective groups (2006)
  • Author(s): Skwarczynski, M., Sohma, Y., Noguchi, M., Hayashi, Y., Kimura, T., Kiso Y
  • Organizer: 7th Tetrahedron Symposium : Challenges in Organic Chemistry
  • Place of Presentation: Kyoto, Japan
  • Year and Date: 2006-05-25
  • Description: 「研究成果報告書概要(欧文)」より
• [Presentation] O-N Intramolecular carbonate-carbamate migration:Application to no byproduct strategy in water-soluble prodrugs of taxoids and migration of protective groups in amino acids (2006)
  • Author(s): M.Skwarczynski, Y.Hayashi, 他4名
  • Organizer: Joint International Symposium on Integrated Medicinal Science for Drug Discovery
  • Place of Presentation: Kyoto
  • Year and Date: 2006-03-06
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] O-N Intramolecular carbonate-carbamate migration : Application to no byproduct strategy in water-soluble prodrugs of taxoids and migration of protective groups in amino acids (2006)
  • Author(s): Skwarczynslu, M., Sohma, Y., Noguchi, M., Kimura, M., Hayashi, Y., Kiso, Y
  • Organizer: Joint International Symposium on Integrated Medicinal Science for Drug Discovery-Tradition to Structural Biology/Medicinal Science Research on Difficult Diseases
  • Place of Presentation: Kyoto
  • Year and Date: 2006-03-06
  • Description: 「研究成果報告書概要(欧文)」より
• [Presentation] No by-product strategy:Application of O-N intramolecular acyl and acyloxy migration to water-soluble taxoid prodrugs (2005)
  • Author(s): M.Skwarczynski, Y.Hayashi, 他6名
  • Organizer: 2005 international Chemical Congress of Pacific Basin Societies(Pacifichem 2005)
  • Place of Presentation: Honolulu,USA
  • Year and Date: 2005-12-17
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] No by-product strategy : Application of O-N intramolecular acyl and acyloxy migration to water-soluble taxoid prodnigs (2005)
  • Author(s): Skwarczynski, M., Sohma, Y., Noguchi, M., Kimura, M., Hayashi, Y., Hamada, Y., Kimura, T., Kiso, Y
  • Organizer: international Chemical Congress of Pacific Basin Societies (Pacifichem 2005)
  • Place of Presentation: Honolulu, U.S.A.
  • Year and Date: 2005-12-17
  • Description: 「研究成果報告書概要(欧文)」より
• [Presentation] 0-N分子内アシロキシ転位反応に基づいた新規水溶性taxoidプロドラッグ:isotaxoidsのデザインと合成 (2005)
  • Author(s): Skwarczynski, M., 林 良雄, 他6名
  • Organizer: 第31回反応と合成の進歩シンポジウム
  • Place of Presentation: 神戸
  • Year and Date: 2005-11-08
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] α-ヒドロキシ-β-アミノ酸を利用した固相Evans不斉補助基の開発 (2005)
  • Author(s): 林 良雄, 小竹 智也, 他4名
  • Organizer: 第31回反応と合成の進歩シンポジウム
  • Place of Presentation: 神戸
  • Year and Date: 2005-11-07
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] O-N intramolecular acyloxy migration reaction:from the prodrug strategy to the migration of protective groups in amino acids (2005)
  • Author(s): M.Skwarczynski, Y.Hayashi, 他6名
  • Organizer: 42nd Japanese Peptide Symposium
  • Place of Presentation: Toyonaka,Japan
  • Year and Date: 2005-10-28
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] O-N intramolecular acyloxy migration reaction from the prodrug strategy to the migration of protective groups in amino acids (2005)
  • Author(s): Skwarczynski, M., Sohma, Y., Noguchi, M., Kimura, M., Hayashi, Y., Hamada, Y., Kimura, T., Kiso, Y
  • Organizer: 42nd Japanese Peptide Symposium
  • Place of Presentation: Toyonaka, Japan
  • Year and Date: 2005-10-28
  • Description: 「研究成果報告書概要(欧文)」より
• [Presentation] No by-product strategy in water-soluble taxoid prodrugs:0-N intramolecular acyloxymigration reaction.Intemational Symposium:New Developments in Synthetic Organic ChemistIy ofNatural Products and Medicines (2005)
  • Author(s): M.Skwarczynski, Y.Hayashi, 他6名
  • Organizer: Intemational Symposium:New Developments in Synthetic Organic Chemistry of Natural Products and Medicines
  • Place of Presentation: Kyoto,Japan
  • Year and Date: 2005-09-17
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] Development of Wang resin supported Evans-type oxazolidinone for asymmetric reaction (2005)
  • Author(s): Y.Hayashi, T.Kotake, 他3名
  • Organizer: International Symposium:New Developments in Synthetic Organic Chemistry of Natural Products and Medicines
  • Place of Presentation: Kyoto,Japan
  • Year and Date: 2005-09-17
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] No by-product strategy in water-soluble taxoid prodrugs : O-N intramolecular acyloxy migration reaction (2005)
  • Author(s): Skwarczynslu, M., Sohma, Y., Noguchi, Y., Kimura, M., Hayashi, Y., Hamada, Y., Kimura, T., Kiso, T
  • Organizer: International Symposium : New Developments in Synthetic Organic Chemistry of Natural Products and Medicines
  • Place of Presentation: Kyoto, Japan
  • Year and Date: 2005-09-17
  • Description: 「研究成果報告書概要(欧文)」より
• [Presentation] Development of Wang resin supported Evans-type oxazolidinone for asymmetric reaction (2005)
  • Author(s): Hayashi, Y., Kotake, T., Rajesh, S., Kimura, T., Kiso, Y
  • Organizer: International Symposium : New Developments in Synthetic Organic Chemistry of Natural Products and Medicines
  • Place of Presentation: Kyoto, Japan
  • Year and Date: 2005-09-17
  • Description: 「研究成果報告書概要(欧文)」より
• [Presentation] Development of Wang resin supported Evans-type oxazolidinone for asymmetric reactlon (2005)
  • Author(s): T.Kotake, Y.Hayashi, 他3名
  • Organizer: 19th American Peptide Symposium
  • Place of Presentation: San Diego,U.S.A.
  • Year and Date: 2005-06-20
  • Description: 「研究成果報告書概要(和文)」より
• [Presentation] Development of Wang resin supported Evans-type oxazolidinone for asymmetric reaction (2005)
  • Author(s): Kotake, T., Hayashi, Y., Rajesh, S., Kimura, T., Kiso, Y
  • Organizer: 19th American Peptide Symposium : Understanding Biology Using Peptides
  • Place of Presentation: San Diego, U.S.A
  • Year and Date: 2005-06-20
  • Description: 「研究成果報告書概要(欧文)」より