Abstract
The isoquinolinone-based tricyclic compounds were designed and synthesized. Preliminary biological study of these compounds provided potent compounds 17a, 33b, 33c, 33d, and 33g with low nanomolar IC50s against PARP-1 enzyme.
Keywords:
Antitumor; Isoquinolinone-based tricycles; PARP-1 inhibitors.
Copyright © 2014 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Enzyme Activation / drug effects
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology*
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Inhibitory Concentration 50
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Isoquinolines / chemistry*
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Isoquinolines / pharmacology*
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Molecular Structure
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Poly(ADP-ribose) Polymerase Inhibitors*
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Poly(ADP-ribose) Polymerases / chemistry
Substances
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Enzyme Inhibitors
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Isoquinolines
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Poly(ADP-ribose) Polymerase Inhibitors
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Poly(ADP-ribose) Polymerases