Patent · US Expired

Syntheses and methods of use of new antimitotic agents

US6673937B2 · kind B2 · utility

1Cited by
1References
2Claims
0Family size

Assignee

Inventors

Key dates

Filing dateJul 19, 2001
Grant dateJan 6, 2004
Priority date
Expiry dateJul 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.