Indoline and tetrahydro-quinolines as prodrugs for tumour treatment

Mark Searcey; Laurence Patterson

Indoline and tetrahydro-quinolines as prodrugs for tumour treatment

Mark Searcey (Inventor), Laurence Patterson (Inventor)

Research output: Patent

Abstract

Compounds of the general formula I or IA or a salt in which X is H, Y is a leaving group, R<1 >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	US2004157880A1
Publication status	Published - 12 Aug 2004

Cite this

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title = "Indoline and tetrahydro-quinolines as prodrugs for tumour treatment",

abstract = "Compounds of the general formula I or IA or a salt in which X is H, Y is a leaving group, R<1 >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.",

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language = "English",

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AU - Patterson, Laurence

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N2 - Compounds of the general formula I or IA or a salt in which X is H, Y is a leaving group, R<1 >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 or a salt in which X is H, Y is a leaving group, R<1 >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.

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