Synthesis, characterization, and anticancer activity of new copper thiosemicarbazone compound holding ONNS quadridentate system

MEDI 349

Haiyuan Zhang, hazhang@med.wayne.edu and Fangyu Peng, fpeng@pet.wayne.edu. Pediatrics and Radiology, School of Medicne, Wayne State University, 3901 Beaubien Blvd, Detroit, MI 48201
Many metal complexes were found to be highly potent against various types of human cancer cells. However, clinical application of majority of anti-cancer metal complexes tested in vitro was hampered by lack of tumor specificity. One of promising approaches to overcome this limitation is targeted delivery of these anti-cancer metal complexes to tumor tissues. Anti-cancer copper complex is especially attractive for targeted cancer therapy because targeted delivery of anticancer copper complexes may be monitored non-invasively by positron emission tomography (PET) when positron emitting copper isotopes, such as copper-64, are used to radio-label the compound. In current study, 8-hydroxyquinoline was coupled to 2-carboxaldehyde–thiosemicarbazide to make 8-hydroxyquinoline-2-carboxaldehyde–thiosemicarbazide (HQTS) holding a unique ONNS quadridentate system. The HQTS-copper complex suppressed proliferation and induced apoptosis of human neuroblastoma and malignant glioblastoma cells. The CuHQTS complex holds potential for targeted cancer therapy monitored by PET imaging.
 

Poster Session
7:00 PM-9:00 PM, Wednesday, August 22, 2007 BCEC -- Exhibit Hall - B2, Poster

Division of Medicinal Chemistry

The 234th ACS National Meeting, Boston, MA, August 19-23, 2007