Benz-indole and benzo-quinoline derivatives as prodrugs for...

Details Benz-indole and benzo-quinoline derivatives as prodrugs for... Benz-indole and benzo-quinoline derivatives as prodrugs for...

2007-03-20

2007-03-20

Powers, Fiona T. (Department: 1626)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C548S427000

Reexamination Certificate

active

10468744

ABSTRACT:
Compounds of the general formula (I) or (IA) in which X is H, Y is a leaving group, R1preferably 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 tumors. The prodrug is expected to be activated preferentially in tumor cells, where it will act as a DNA alkylating agent preventing cell division

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Dale L. Boger, et al., “Synthesis of CC-1065 and Duocarmycin Analogs via Intramolecular Aryl Radical Cyclization of a Tethered Vinyl Chloride,” Tetrahdron Letters 39 (1998) pp. 2227-2230.

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