2004 Fiscal Year Final Research Report Summary
Development of Anticancer and Antiviral Agents Based on Diketopiperazine as a Bio-function-Mimicking Molecular Platform
| Project/Area Number |
15590102
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Drug development chemistry
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| Research Institution | Kyoto Pharmaceutical University |
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Principal Investigator |
HAYASHI Yoshio Kyoto Pharmaceutical University, Associate Professor, 薬学部, 助教授 (10322562)
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| Project Period (FY) |
2003 – 2004
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| Keywords | Diketopiperazine / Bio-function-Mimicking Molecular Platform / Anticancer Agent / Phenylahistin / Convenient Synthetic Method / Racemization / Anti-microtubule Agent / Monodehydrodiketopiperazine |
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| Research Abstract |
To understand the usefulness of diketopiperazine (DKP) template as a bio-function-mimicking molecular platform in medicinal chemistry, in this research project, we planed to establish a convenient synthetic method for DKP and develop a new anticancer agent based on the DKP structure. As results, 1) a new convenient synthetic procedure for monodehydro-DKP derivatives which has a dehydro-structure at anα,β-position of the DKP ring. 2) this method was successfully applied to the synthesis of a chiral derivative of naturally occurring anticancer agent, phenylahistin. 3) a structural optimization of DKP was carried out to obtain a highly potent anticancer derivative, and a derivative which is not only potent but also stable against cytochrome P450 metabolism was developed. 4) Additionally, in an anticancer drug, a water-soluble prodrug for highly insoluble anti-microtubule agent was also developed, and 5) New efficient solid-supported chiral auxiliary for the preparation of chiral amino acids, which are needed for diketopiperazine synthesis as starting materials, was developed.
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Research Products
(16 results)
