Topoisomerase II inhibitors and therapeutic uses therefor
US5747520A · kind A · utility
Inventors
Key dates
| Filing date | Jun 2, 1995 |
| Grant date | May 5, 1998 |
| Priority date | — |
| Expiry date | Jun 2, 2015 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D499/14
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Azatoxin and derivatives thereof are illustrative of a new class of antitumor drugs that are topoisomerase II (top 2) inhibitors. The pharmacophore inhibits the catalytic activity of the purified enzyme but does not unwind relaxed or supercoiled DNA. It is nonintercalative and has at least two domains: a quasi-planar polycyclic ring system, which may bind between DNA base pairs, and a pendant substituent thought to interact with the enzyme, with the DNA grooves or with both. In SV40 and c-myc DNA, azatoxin induces numerous double-strand breaks according to a cleavage pattern which differs from those of known top 2 inhibitors. Azatoxin also is a potent inhibitor of tubulin polymerization.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.