Development of Radiohalogenated Osimertinib Derivatives as Imaging Probes for Companion Diagnostics of Osimertinib

Autor:	Kenji Mishiro, Ryuichi Nishii, Izumi Sawazaki, Tomoki Sofuku, Takeshi Fuchigami, Hitomi Sudo, Nurmaya Effendi, Akira Makino, Yasushi Kiyono, Kazuhiro Shiba, Junichi Taki, Seigo Kinuya, Kazuma Ogawa
Rok vydání:	2022
Předmět:	Male Acrylamides Mice Inbred BALB C Aniline Compounds Halogenation Mice Nude ErbB Receptors Iodine Radioisotopes Carcinoma Non-Small-Cell Lung Cell Line Tumor Mutation Drug Discovery Animals Humans Molecular Medicine Tissue Distribution Bromine Radioisotopes Radiopharmaceuticals
Zdroj:	Journal of Medicinal Chemistry. 65:1835-1847
ISSN:	1520-4804 0022-2623
DOI:	10.1021/acs.jmedchem.1c01211
Popis:	Osimertinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor approved for treating non-small-cell lung cancer (NSCLC) with EGFR mutations. Genetic testing is required to detect the mutation for selecting patients who can use osimertinib. Here, we report an attempt to develop nuclear imaging probes that detect the EGFR mutations. We designed and synthesized I-osimertinib and Br-osimertinib with a radioactive or nonradioactive halogen atom at an indole ring in osimertinib and evaluated them.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9d717c01948db47e77a353b6c172573f https://doi.org/10.1021/acs.jmedchem.1c01211 Zobrazit plný text záznamu