O6-alkylguaninderivater, fremgangsmåte for fremstilling og anvendelse derav samt farmasöytiske preparater

O &cir& _ -hetarylalkyl- or naphthylalkylguanine derivatives of formula (I) wherein Y is H, ribosyl, deoxyribosyl, or R"XCHR"', wherein X is O or S, R'' and R''' are alkyl, or substituted derivatives thereof; R' is H, or alkyl or hydroxyalkyl; R i...

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Hauptverfasser: KELLY JANE, WATSON AMANDA JEAN, RAFFERY JOSEPH ANTHONY, MCELHINNEY ROBERT STANLEY, MARGISON GEOFFREY PAUL, MCMURRY THOMAS BRIAN HAMILTON, ELDER RHODERICK HUGH, MCCORMICK JOAN ELIZABETH, WILLINGTON MARK ANDREW
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creator KELLY JANE
WATSON AMANDA JEAN
RAFFERY JOSEPH ANTHONY
MCELHINNEY ROBERT STANLEY
MARGISON GEOFFREY PAUL
MCMURRY THOMAS BRIAN HAMILTON
ELDER RHODERICK HUGH
MCCORMICK JOAN ELIZABETH
WILLINGTON MARK ANDREW
description O &cir& _ -hetarylalkyl- or naphthylalkylguanine derivatives of formula (I) wherein Y is H, ribosyl, deoxyribosyl, or R"XCHR"', wherein X is O or S, R'' and R''' are alkyl, or substituted derivatives thereof; R' is H, or alkyl or hydroxyalkyl; R is (i) a cyclic group having at least one 5- or 6-membered heterocyclic ring, optionally with a carbocyclic or heterocyclic ring fused thereto, the or each heterocyclic ring having at least one hereto atom chosen from O, N or S, or a substituted derivative thereof; or (ii) naphthyl or a substituted derivative thereof; and pharmaceutically acceptable salts thereof, exhibit the ability to deplete O &cir& _ -alkylguanine-DNA alkyltransferase (ATase) activity. A process for preparation of the compounds is described. The compounds have utility in combination with alkylating agents in the chemotherapeutic treatment of tumour cells.
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subjects CHEMISTRY
DERIVATIVES THEREOF
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
NUCLEIC ACIDS
NUCLEOSIDES
NUCLEOTIDES
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
SUGARS
title O6-alkylguaninderivater, fremgangsmåte for fremstilling og anvendelse derav samt farmasöytiske preparater
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