Tetrahedron

1 H NMR studies on the reductively triggered release of heterocyclic and steroid drugs from 4, 7-dioxoindole-3-methyl prodrugs

S Ferrer, DP Naughton, MD Threadgill

Index: Ferrer, Sandra; Naughton, Declan P.; Threadgill, Michael D. Tetrahedron, 2003 , vol. 59, # 19 p. 3445 - 3454

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Citation Number: 26

Abstract

Hypoxia is a feature of several disease states, including cancer and rheumatoid arthritis. Prodrug systems which, after bioreduction, selectively release active drugs in these tissues may be important in therapy. An improved preparation of 1, 2-dimethyl-3-hydroxymethyl-5- methoxyindole-4, 7-dione was developed. Mitsunobu coupling with (5-substituted) isoquinolin-1-ones (potent inhibitors of poly (ADP-ribose) polymerase) gave 1-(1, 2- ...