Syntheses and methods of use of new antimitotic agents
US6673937B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Jul 19, 2001 |
| Grant date | Jan 6, 2004 |
| Priority date | — |
| Expiry date | Jul 19, 2021 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D493/10
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Oxidative cyclization of bis-naphthyl ethers allows concise total syntheses of palmarumycin CP1 and deoxypreussomerin A in 8-9 steps and 15-35% overall yield from 5-hydroxy-8-methoxy-1-tetralone. A small library of palmarumycin analogs was created. Biological evaluation of these naphthoquinone spiroketals against MCF-7 and MDA-MB-231 human breast cancer cells revealed several low-micromolar growth inhibitors. A number of the analogs inhibit the thioredoxin—thioredoxin reductase system.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.