Novel Metal Ion Based Estrogen Mimics for Molecular Imaging

Technical Report · Mon Jan 30 04:00:00 EST 2006

DOI:https://doi.org/10.2172/875440· OSTI ID:875440

Rajagopalan, Raghavan ^[1]

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1. Biofleixis, LLC

The overall objective of the SBIR Phase I proposal is to prepare and evaluate a new class of {sup 99m}Tc or {sup 94m}Tc containing estrogen-like small molecules ('estrogen mimics') for SPECT or PET molecular imaging of estrogen receptor positive (ER+) tumors. In this approach, the metal ion is integrated into the estrone skeleton by isosteric substitution of a carbon atom in the steroidal structure to give new class of mimics that are topologically similar to the native estrogen (Fig. 1). Although both N{sub 2}S{sub 2} and N{sub 3}S mimics 1 and 2 were considered as target structures, molecular modeling study revealed that the presence of the acetyl group at position-15 in the N{sub 3}S mimic 2 causes steric hinderance toward binding of 2 to SHBG. Therefore, initial efforts were directed at the synthesis and evaluation of the N{sub 2}S{sub 2} mimic 1.

• Research Organization: Bioflexis
• Sponsoring Organization: USDOE - Office of Science (SC)
• DOE Contract Number: FG02-04ER83908
• OSTI ID: 875440
• Report Number(s): DOE/ER/83908-2 Final Report
• Country of Publication: United States
• Language: English

Related Subjects

37 INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY
ATOMS
CARBON
ESTROGENS
ESTRONE
EVALUATION
NEOPLASMS
SIMULATION
SINGLE PHOTON EMISSION COMPUTED TOMOGRAPHY
SKELETON
SYNTHESIS
Steroid mimics, estrogen mimics, estrogen receptors, ER positive tumors, molecular imaging, and metal-based estrogen mimics.
TARGETS