論文 - 詳細
| RRC ID | 58120 |
|---|---|
| 著者 | Matsumoto Y, Kuriki H, Kitamura T, Takahashi D, Toshima K. |
| タイトル | Total Synthesis and Structure-Activity Relationship Study of Vineomycin A1. |
| ジャーナル | J Org Chem |
| Abstract |
The first total synthesis of vineomycin A1 (1) has been accomplished. Structure-activity relationship studies for cytotoxicity against human breast cancer MCF-7 cells using several synthetic vineomycin A1 analogues differing in the number and position of glycon moieties revealed that the cytotoxicity increased as the number of glycon moieties increased. The position of the glycon moiety was one of the key factors for the cytotoxicity of 1. Moreover, in vitro analysis of the cytotoxicity of 1 against MCF-7 cells indicated for the first time that 1 effectively induced cancer cell death by apoptosis, not by acting as a DNA intercalating agent. |
| 巻・号 | 84(22) |
| ページ | 14724-14732 |
| 公開日 | 2019-11-15 |
| DOI | 10.1021/acs.joc.9b02304 |
| PMID | 31642324 |
| MeSH | Anthraquinones / chemical synthesis Anthraquinones / chemistry Anthraquinones / pharmacology* Antineoplastic Agents / chemical synthesis Antineoplastic Agents / chemistry Antineoplastic Agents / pharmacology* Apoptosis / drug effects Cell Line, Tumor Cell Proliferation / drug effects Dose-Response Relationship, Drug Drug Screening Assays, Antitumor Humans Molecular Conformation Structure-Activity Relationship |
| IF | 4.745 |
| 引用数 | 1 |
| リソース情報 | |
| ヒト・動物細胞 | MCF7(RCB1904) HCT116(RCB2979) A549 |