SYNTHESIS AND COMPOSITION OF AMINO ACID LINKING GROUPS CONJUGATED TO COMPOUNDS USED FOR THE TARGETED IMAGING OF TUMORS

摘要

The present disclosure relates to compounds that are useful as near-infrared fluorescence probes, wherein the compounds include i) a pteroyl ligand that binds to a target receptor protein, ii) a dye molecule, and iii) a linker molecule that comprises an amino acid or derivative thereof. The disclosure further describes methods and compositions for incorporating the compounds as used for the targeted imaging of tumors. Conjugation of the amino acid linking groups increase specificity and detection of the compound. Methods and compositions for use thereof in diagnostic imaging are contemplated.

主权项

1. A method of imaging a carcinoma that expresses a folate receptor comprising the steps of:
a. administering to a patient in need of an effective amount of a compound capable of binding to a cancerous cell having the formula:or a pharmaceutically acceptable salt or isotope thereof, wherein: X is an single amino acid or a single amino acid derivative thereof, wherein the single amino acid or single amino acid derivative contains an —OH, —NH2, or —SH functional group, and Y is a dye that has a fluorescence excitation and emission spectra in the near infra-red range, wherein Y is represented by the formula:wherein, R1 is independently selected from the group consisting of O, S, N and C, and R2 is independently selected from the group consisting of CH2 and CH2CH2, and the compound enhances the fluorescence of the dye, Y; and
b. fluorescent imaging of an area of concern in the patient's body where the compound has been bound to a cancerous cell wherein the carcinoma is selected from the group consisting of cervical cancer, ovarian cancer, breast cancer, leukemia cancer, and lung cancer.