Analogues of the azinomycins as antitumour agents and as prodrugs

Mark Searcey; Laurence Hylton Patterson; Klaus Pors; Maxwell Casely-Hayford

Analogues of the azinomycins as antitumour agents and as prodrugs

Mark Searcey (Inventor), Laurence Hylton Patterson (Inventor), Klaus Pors (Inventor), Maxwell Casely-Hayford (Inventor)

Research output: Patent

Abstract

Compounds of general formula (I) or a salt thereof in which R1 is preferably an aromatic DNA binding subunit are oxidation-activated prodrugs. The compounds are expected to be converted into an epoxide at the alkene to which R2 is attached by cytochrome P450, in particular CYPIBI, expressed at high levels in tumours. R3 preferably comprises a Nitrogen mustard to provide a prodrug which has 2 alkylating groups. The prodrugs are expected to be activated preferentially in tumour cells.

Original language	English
Patent number	WO2006097730A1
Publication status	Published - 18 Mar 2005

Cite this

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title = "Analogues of the azinomycins as antitumour agents and as prodrugs",

abstract = "Compounds of general formula (I) or a salt thereof in which R1 is preferably an aromatic DNA binding subunit are oxidation-activated prodrugs. The compounds are expected to be converted into an epoxide at the alkene to which R2 is attached by cytochrome P450, in particular CYPIBI, expressed at high levels in tumours. R3 preferably comprises a Nitrogen mustard to provide a prodrug which has 2 alkylating groups. The prodrugs are expected to be activated preferentially in tumour cells.",

author = "Mark Searcey and Patterson, {Laurence Hylton} and Klaus Pors and Maxwell Casely-Hayford",

year = "2005",

month = mar,

day = "18",

language = "English",

type = "Patent",

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AU - Searcey, Mark

AU - Patterson, Laurence Hylton

AU - Pors, Klaus

AU - Casely-Hayford, Maxwell

PY - 2005/3/18

Y1 - 2005/3/18

N2 - Compounds of general formula (I) or a salt thereof in which R1 is preferably an aromatic DNA binding subunit are oxidation-activated prodrugs. The compounds are expected to be converted into an epoxide at the alkene to which R2 is attached by cytochrome P450, in particular CYPIBI, expressed at high levels in tumours. R3 preferably comprises a Nitrogen mustard to provide a prodrug which has 2 alkylating groups. The prodrugs are expected to be activated preferentially in tumour cells.

AB - Compounds of general formula (I) or a salt thereof in which R1 is preferably an aromatic DNA binding subunit are oxidation-activated prodrugs. The compounds are expected to be converted into an epoxide at the alkene to which R2 is attached by cytochrome P450, in particular CYPIBI, expressed at high levels in tumours. R3 preferably comprises a Nitrogen mustard to provide a prodrug which has 2 alkylating groups. The prodrugs are expected to be activated preferentially in tumour cells.

M3 - Patent

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