O.sup.6 -substituted guanine compounds and methods for depleting O.sup.6 -alkylguanine-DNA alkyltransferase levels
US5091430A · kind A · utility
17Cited by
1References
12Claims
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Key dates
| Filing date | Mar 13, 1990 |
| Grant date | Feb 25, 1992 |
| Priority date | — |
| Expiry date | Mar 13, 2010 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07H19/16
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
O.sup.6 -substituted guanine compounds of the formula ##STR1## wherein R is a benzyl group or a substituted benzyl group, cause a depletion of O.sup.6 -alkylguanine-DNA alkyltransferase (AGT) activity in mammalian cells. These compounds may be administered to a host so as to reduce AGT levels in tumor cells of the host in order to increase host responsiveness to anti-neoplastic alkylating agents, including chloroethylating agents, such as chloroethylnitrosoureas, for chemotherapeutic treatment of a number of neoplasms.
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