Development of Tethered Hsp90 Inhibitors Carrying Radioiodinated Probes to Specifically Discriminate and Kill Malignant Breast Tumor Cells
Technical Report,01 May 2015,30 Apr 2016
Duke University Durham United States
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We have proposed to develop tethered Hsp90 inhibitor capable of carrying various radioactive iodine isotopes for early detection and ablation of metastatic breast cancers. These probes specifically target a surface form of heat shock protein 90 eHsp90 that is expressed on malignant cells and internalized. In this report we describe our chemistry efforts to synthesize a non-radioactive tethered Hsp90 inhibitor, methods developed for stannylation of the molecule such that it can be effectively radioiodinated with either I121 or I124. Two paths of synthesis were developed. A standard operating procedure was developed and transferred to our collaborator who developed protocols for radioiodination. An in active control molecule was also developed. These molecules will be tested as imaging agents in mouse models of breast cancer.
- Medicine and Medical Research
- Physical Chemistry