Novel Technetium-99m-labelled ribociclib isocyanide derivatives for imaging cyclin-dependent kinase (CDK4/6) expression in cancer

European Journal of Medicinal Chemistry, Год журнала: 2025, Номер 286, С. 117264 - 117264

Опубликована: Янв. 11, 2025

Язык: Английский

Synthesis and Imaging of Novel CDK19‐Targeted Tracers Incorporating an Albumin‐Binding Moiety

Journal of Labelled Compounds and Radiopharmaceuticals, Год журнала: 2025, Номер 68(3)

Опубликована: Март 1, 2025

ABSTRACT Cyclin‐dependent kinase 19 (CDK19) is a potential target for the diagnosis and treatment of prostate cancer. We have previously studied series CDK19‐targeted PET tracers, but in‐depth drug optimization needed to improve physiochemical properties such large polar tracers. The albumin strategy has received widespread attention in recent years, we synthesized 68 Ga‐IRM‐14a Ga‐IRM‐14b based on strategy. After vivo imaging studies mice, found that introducing moiety will significantly change physicochemical existing polarity thereby increasing tissue uptake retention, which beneficial future treatment. In short, be an important field radiopharmaceutical optimization.

Язык: Английский

Synthesis of 4‐Cyclobutene‐Isoquinolines From Aryl Imidates by Ru(II)‐Catalyzed Domino C–H Activation/Cyclization

Applied Organometallic Chemistry, Год журнала: 2024, Номер unknown

Опубликована: Ноя. 13, 2024

ABSTRACT A highly regioselective approach for constructing 4‐cyclobutene‐isoquinoline derivatives through ruthenium‐catalyzed domino C–H activation/cyclization of aryl imidates has been demonstrated. This new transformation tolerates various substituted functional groups on and propargylic monofluoroalkynes, resulting in the corresponding products being delivered moderate yields.

Язык: Английский