O6-SUBSTITUIERTE GUANINEDERIVATE, VERFAHREN ZU IHRE HERSTELLUNG UND IHRE ANWENDUNG FÜR BEHANDLUNG VON TUMORZELLEN

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: MCMURRY, THOMAS BRIAN HAMILTON, KELLY, JANE CHRISTIE HOSPITAL, PATERSON INST, ELDER, RHODERICK, HUGH, MCCORMICK, JOAN ELIZABETH, MCELHINNEY, ROBERT STANLEY, CARCINOGENESIS, PATERSON INST
Format: Patent
Sprache:ger
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Zusammenfassung: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.