論文 - 詳細
| RRC ID | 39234 |
|---|---|
| 著者 | Kageyama Y, Yamazaki Y, Okuno H. |
| タイトル | Novel approaches to prodrugs of anticancer diaminodichloroplatinum(II) complexes activated by stereoselective enzymatic ester hydrolysis. |
| ジャーナル | J Inorg Biochem |
| Abstract |
A series of dichloro(ethylenediamine)-type platinum complexes bearing ester-, amide- and ether-bonded alkyl straight chains (C2-C18) was prepared as a model for the prodrug of cis-diamminedichloroplatinum (CDDP). Evaluation of cytotoxic activity of the complexes against the S-180 cell line proved that their enzymatic hydrolysis in the cells lowered the permeability to the cell membranes resulting in an increase of pharmacological activity. Optically active isomers of dichloro(N-2(2-phenylpropanoyloxy)ethyl)-2,3-diaminopropanamide )platinum(II) were prepared. They were re-activated stereoselectively, and a tenfold difference in activity was observed based on the differences in chiral discrimination by enzymes. |
| 巻・号 | 70(1) |
| ページ | 25-32 |
| 公開日 | 1998-4-1 |
| DOI | 10.1016/s0162-0134(98)00009-9 |
| PII | S0162-0134(98)00009-9 |
| PMID | 9661285 |
| MeSH | Animals Antineoplastic Agents / chemistry Antineoplastic Agents / metabolism* Antineoplastic Agents / therapeutic use Cell Membrane Permeability / drug effects Cisplatin / analogs & derivatives* Cisplatin / metabolism Cisplatin / therapeutic use Hydrolysis Liver Neoplasms, Experimental / drug therapy Liver Neoplasms, Experimental / metabolism Magnetic Resonance Spectroscopy Prodrugs / chemistry Prodrugs / metabolism* Prodrugs / therapeutic use Rats Sarcoma 180 / drug therapy Sarcoma 180 / metabolism Stereoisomerism Tumor Cells, Cultured |
| IF | 3.212 |
| 引用数 | 13 |
| WOS 分野 | CHEMISTRY, INORGANIC & NUCLEAR BIOCHEMISTRY & MOLECULAR BIOLOGY |
| リソース情報 | |
| ヒト・動物細胞 | Anr4(RCB0449) |