211-astatine containing radiotherapeutics for the treatment of cancer
Abstract
Described herein is an alpha-emitting radionuclide, 211At, which has been incorporated into a selective sigma-2 ligand moiety to provide cytotoxic capabilities to a chemical compound. As described herein, a compound of formula (I), wherein R1-R4, m, and n are defined herein, was prepared and utilized in in vitro and in vivo tumor targeting of alpha-emitting sigma-2 ligand in a breast cancer model. In one embodiment, the compound is 5-(211At)—N-(4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-2,3-dimethoxybenzamide.
- Inventors:
- Issue Date:
- Research Org.:
- Univ. of Pennsylvania, Philadelphia, PA (United States)
- Sponsoring Org.:
- USDOE Office of Science (SC), Biological and Environmental Research (BER)
- OSTI Identifier:
- 1600218
- Patent Number(s):
- 10457642
- Application Number:
- 15/571,055
- Assignee:
- The Trustees of the University of Pennsylvania (Philadelphia, PA)
- Patent Classifications (CPCs):
-
A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61K - PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
G - PHYSICS G21 - NUCLEAR PHYSICS G21H - OBTAINING ENERGY FROM RADIOACTIVE SOURCES
- DOE Contract Number:
- SC0012476
- Resource Type:
- Patent
- Resource Relation:
- Patent File Date: 04/26/2016
- Country of Publication:
- United States
- Language:
- English
Citation Formats
Pryma, Daniel A., Lieberman, Brian P., Makvandi, Mehran, and Mach, Robert H. 211-astatine containing radiotherapeutics for the treatment of cancer. United States: N. p., 2019.
Web.
Pryma, Daniel A., Lieberman, Brian P., Makvandi, Mehran, & Mach, Robert H. 211-astatine containing radiotherapeutics for the treatment of cancer. United States.
Pryma, Daniel A., Lieberman, Brian P., Makvandi, Mehran, and Mach, Robert H. Tue .
"211-astatine containing radiotherapeutics for the treatment of cancer". United States. https://www.osti.gov/servlets/purl/1600218.
@article{osti_1600218,
title = {211-astatine containing radiotherapeutics for the treatment of cancer},
author = {Pryma, Daniel A. and Lieberman, Brian P. and Makvandi, Mehran and Mach, Robert H.},
abstractNote = {Described herein is an alpha-emitting radionuclide, 211At, which has been incorporated into a selective sigma-2 ligand moiety to provide cytotoxic capabilities to a chemical compound. As described herein, a compound of formula (I), wherein R1-R4, m, and n are defined herein, was prepared and utilized in in vitro and in vivo tumor targeting of alpha-emitting sigma-2 ligand in a breast cancer model. In one embodiment, the compound is 5-(211At)—N-(4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-2,3-dimethoxybenzamide.},
doi = {},
journal = {},
number = ,
volume = ,
place = {United States},
year = {2019},
month = {10}
}
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