Radiolabeled and fluorescent PARP inhibitors for imaging and radiotherapy
AssigneeThe Trustees of the University of Pennsylvania
InventorsRobert H. Mach, Sean Reilly, Mehran Makvandi, Kuiying Xu, Daniel A. Pryma, Roger A. Greenberg
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Abstract
The present disclosure relates to compounds of Formula I and II, wherein R1-R20 and FL are defined herein. Also provided are methods of targeting alpha-radiation to poly(ADP-ribose)polymerase 1 (PARP-1) enzyme expression, reducing proliferation of cancer cells, reducing proliferation of cancer cells, detecting intact and enzymatically active poly(ADP-ribose)polymerase 1 (PARP-1) enzyme expression, detecting PARP-1 enzyme expression in a subjects tissue sample, monitoring cancer treatment in a subject, or detecting a PARP-1 receptive cancer in a subject.
Claims12
A compound of Formula I:
- wherein:
- X—Y—Z is N—C═N, C═C—NH, or CH—C═N;
- is a single or double bond;
- and
- R1 to R10 are, independently, H, halogen, optionally substituted C1-6alkyl, optionally substituted C3-7cycloalkyl, or optionally substituted heteroaryl;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.