論文 - 詳細
| RRC ID | 18568 |
|---|---|
| 著者 | Takagaki T, Bando T, Kitano M, Hashiya K, Kashiwazaki G, Sugiyama H. |
| タイトル | Evaluation of PI polyamide conjugates with eight-base pair recognition and improvement of the aqueous solubility by PEGylation. |
| ジャーナル | Bioorg Med Chem |
| Abstract |
To investigate the effect of elongating base-pair (bp) recognition sequences, we synthesized N-methylpyrrole-N-methylimidazole (PI) polyamide conjugates with eight-bp recognition (3-5). The DNA alkylating activities of conjugates 3-5 were evaluated by high-resolution denaturing polyacrylamide gel electrophoresis with a 208-bp DNA fragment. Conjugates 3-5 showed high alkylating activities at nanomolar concentrations. We then addressed the following issue about PI conjugates. Generally, PI polyamide conjugates hardly dissolve in aqueous solution. To improve the aqueous solubility, by the introduction of hydrophilic groups, we synthesized PI polyamide conjugates that were modified with a seco-CBI moiety (6-11). Conjugates 9-11 that were modified by methoxypolyethylene glycol (PEG) 750 acquired moderate solubility and stability in aqueous solution. In addition, conjugates 10 and 11 had high cytotoxicity against A549 and DU145. |
| 巻・号 | 19(19) |
| ページ | 5896-902 |
| 公開日 | 2011-10-1 |
| DOI | 10.1016/j.bmc.2011.08.009 |
| PII | S0968-0896(11)00633-X |
| PMID | 21903400 |
| MeSH | Antineoplastic Agents, Alkylating / chemical synthesis Antineoplastic Agents, Alkylating / chemistry* Antineoplastic Agents, Alkylating / toxicity Base Pairing / drug effects Cell Line, Tumor Drug Design Electrophoresis, Polyacrylamide Gel Humans Imidazoles / chemistry Nylons / chemical synthesis Nylons / chemistry* Nylons / toxicity Polyethylene Glycols / chemistry* Pyrroles / chemistry Solubility Water / chemistry |
| IF | 3.073 |
| 引用数 | 9 |
| WOS 分野 | CHEMISTRY, MEDICINAL CHEMISTRY, ORGANIC BIOCHEMISTRY & MOLECULAR BIOLOGY |
| オルトメトリクス指標 |
オルトメトリクス指標項目
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| 最多言及媒体 | Patent(IFI CLAIMS) |
| 各媒体での言及数の合計 | 2 |
| 過去6か月間でのオルトメトリクス指標の変動値 | 0.0 |
| リソース情報 | |
| ヒト・動物細胞 | DU145(RCB2143) |