Serendipitous Discovery of a Prodrug of a PARP-1 Inhibitor

During SAR development of previously reported pyrrolocarbazole 1, a potent PARP‐1 inhibitor, compound 14, was discovered serendipitously to be a prodrug of compound 1. Compound 14 behaves as a water‐soluble prodrug of pyrrolocarbazole 1, a potent PARP‐1 inhibitor.

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Bibliographic Details
Published in:Chemical biology & drug design 2013-09, Vol.82 (3), p.348-350
Main Authors: Dunn, Derek, Husten, Jean, Aimone, Lisa D., Ator, Mark A., Chatterjee, Sankar
Format: Article
Language:English
Subjects:
Animals
Carbazoles - chemistry
Carbazoles - metabolism
Carbazoles - pharmacokinetics
Chickens
Drug Evaluation, Preclinical
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - metabolism
Enzyme Inhibitors - pharmacokinetics
Half-Life
oncology
PARP-1
Phthalimides - chemistry
Phthalimides - metabolism
Phthalimides - pharmacokinetics
Poly(ADP-ribose) Polymerase Inhibitors
Poly(ADP-ribose) Polymerases - metabolism
Prodrugs - chemistry
Prodrugs - metabolism
Prodrugs - pharmacokinetics
Protein Binding
pyrrolocarbazole
Rats
Structure-Activity Relationship
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Summary:During SAR development of previously reported pyrrolocarbazole 1, a potent PARP‐1 inhibitor, compound 14, was discovered serendipitously to be a prodrug of compound 1. Compound 14 behaves as a water‐soluble prodrug of pyrrolocarbazole 1, a potent PARP‐1 inhibitor.
ISSN:1747-0277
1747-0285
DOI:10.1111/cbdd.12165