Pyrrolo-indole and pyrrolo-quinoline derivatives as prodrugs for tumour treatment

Mark Searcey; Laurence Patterson

Pyrrolo-indole and pyrrolo-quinoline derivatives as prodrugs for tumour treatment

Mark Searcey (Inventor), Laurence Patterson (Inventor)

Research output: Patent

Abstract

Compounds of the general formula (I) or (IA) in which X is H, Y is a leaving group, R<1 >and optionally also R<3 >preferably being an aromatic DNA binding subunit are prodrug analogues of duocarmycin. The compounds are expected to be hydroxylated at the carbon atom to which X is joined, by cytochrome P450, in particular by CYP1B1, expressed at high levels in tumours. The prodrug is expected to be activated preferentially in tumour cells, where it will act as a DNA alkylating agent preventing cell division.

Original language	English
Patent number	US2004157873A1
Publication status	Published - 12 Aug 2004

Cite this

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title = "Pyrrolo-indole and pyrrolo-quinoline derivatives as prodrugs for tumour treatment",

abstract = "Compounds of the general formula (I) or (IA) in which X is H, Y is a leaving group, R<1 >and optionally also R<3 >preferably being an aromatic DNA binding subunit are prodrug analogues of duocarmycin. The compounds are expected to be hydroxylated at the carbon atom to which X is joined, by cytochrome P450, in particular by CYP1B1, expressed at high levels in tumours. The prodrug is expected to be activated preferentially in tumour cells, where it will act as a DNA alkylating agent preventing cell division.",

author = "Mark Searcey and Laurence Patterson",

year = "2004",

month = aug,

day = "12",

language = "English",

type = "Patent",

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AU - Patterson, Laurence

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N2 - Compounds of the general formula (I) or (IA) in which X is H, Y is a leaving group, R<1 >and optionally also R<3 >preferably being an aromatic DNA binding subunit are prodrug analogues of duocarmycin. The compounds are expected to be hydroxylated at the carbon atom to which X is joined, by cytochrome P450, in particular by CYP1B1, expressed at high levels in tumours. The prodrug is expected to be activated preferentially in tumour cells, where it will act as a DNA alkylating agent preventing cell division.

AB - Compounds of the general formula (I) or (IA) in which X is H, Y is a leaving group, R<1 >and optionally also R<3 >preferably being an aromatic DNA binding subunit are prodrug analogues of duocarmycin. The compounds are expected to be hydroxylated at the carbon atom to which X is joined, by cytochrome P450, in particular by CYP1B1, expressed at high levels in tumours. The prodrug is expected to be activated preferentially in tumour cells, where it will act as a DNA alkylating agent preventing cell division.

M3 - Patent

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