99mTc(CO)3 nucleus-labeled isonitrile-containing palbociclib derivative and preparation method and application thereof

Abstract

The invention discloses a 99mTc(CO)3 nucleus-labeled isonitrile-containing palbociclib derivative of which the molecular general formula is [99mTc(CO)3(CNPBB)3]+. In the structural formula, a 99mTc(CO)3 nucleus is taken as a central nucleus, and carbon atoms of isonitrile groups in CNPBB ligand molecules replace water molecules on a [99mTc(CO)3(H2O)3]+ intermediate to form a [99mTc(CO)3(CNPBB)3]+complex, wherein n is equal to 2 and 3. The [99mTc(CO)3(CN3PBB)3]+ complex is obtained through specific preparation steps of synthesis of ligands CN2PBB and CN3PBB, synthesis of complexes [99mTc(CO)3(CN2PBB)3]+ and [99mTc(CO)3(CN3PBB)3]+, and the like. The complex has high radiochemical purity and good stability, and is used as a tumor imaging agent in the field of nuclear medicine.

Description

technical field [0001] The present invention relates to 99m The field of Tc-labeled radiopharmaceutical chemistry and clinical nuclear medicine technology, specifically relates to a 99m Tc(CO) 3 Preparation and use of nuclear-labeled isocyanide-containing palbociclib derivatives. Background technique [0002] Tumor is formed when the body's cell cycle loses normal regulation under the action of carcinogenic factors, resulting in abnormal proliferation of cell clones. The normal cell cycle includes G1 phase, S phase, G2 phase and M phase. In this process, many enzymes and proteins play a regulatory and controlling role, such as cyclin-dependent kinases, cyclins, and retinoblastoma proteins. Among them, CDK4 / 6 plays an important role in the transition from G1 phase to S phase of the cell cycle. When CDK4 / 6 combines with cyclinD to form a complex, it can phosphorylate Rb, thereby realizing the transition of the cell cycle from G1 phase to S phase. Abnormal expression of C...

AI Technical Summary

Problems solved by technology

not yet seen 99m Tc-labeled CDK4 / 6 inhibitors have been reported as tumor imaging agents, so the development of new 99m Tc-labeled CDK4 / 6 inhibitors have important practical significance as tumor imaging agents

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