Synthesis, Characterization and Reactivities of New HDAC Inhibitors
Poster Number
12B
Format
Poster Presentation
Faculty Mentor Name
Qinliang Zhao
Faculty Mentor Department
Chemistry
Additional Faculty Mentor Name
Xin Guo
Additional Faculty Mentor Department
Pharmaceutics and Medicinal Chemistry
Graduate Student Mentor Name
Chao Feng
Graduate Student Mentor Department
Chemistry
Additional Mentors
Yingbo Huang, y_huang10@u.pacific.edu Department of Pharmaceutics and Medicinal Chemistry.
Abstract/Artist Statement
The advancement of tumors and growing resistance to existing anticancer drugs required the constant need for new drugs and/or therapies. Histone deacetylase (HDAC) is found to be overexpressed in some cancer cells, which condenses the chromatin structure of tumor suppressor genes, cell-cycle inhibitor genes and apoptosis inducer genes. Our innovative approach to these problems is to develop bifunctional platinum complexes stabilized by newly designed HDAC inhibitors. Each inhibitor comprises of a main scaffold, a zinc-binding group, a protein recognition cap and also a coordination site to metal ions. The HDAC inhibitors were synthesized, purified, and have been characterized by MS and NMR analysis. Platinum ions were anchored at the coordination site of the inhibitors, resulting in the desired metal complexes. Cell viability studies of the inhibitors and selected bifunctional compounds demonstrated the critical and unique role of each component in the inhibitor and metal complexes.
Location
DeRosa University Center Ballroom
Start Date
27-4-2018 12:30 PM
End Date
27-4-2018 2:30 PM
Synthesis, Characterization and Reactivities of New HDAC Inhibitors
DeRosa University Center Ballroom
The advancement of tumors and growing resistance to existing anticancer drugs required the constant need for new drugs and/or therapies. Histone deacetylase (HDAC) is found to be overexpressed in some cancer cells, which condenses the chromatin structure of tumor suppressor genes, cell-cycle inhibitor genes and apoptosis inducer genes. Our innovative approach to these problems is to develop bifunctional platinum complexes stabilized by newly designed HDAC inhibitors. Each inhibitor comprises of a main scaffold, a zinc-binding group, a protein recognition cap and also a coordination site to metal ions. The HDAC inhibitors were synthesized, purified, and have been characterized by MS and NMR analysis. Platinum ions were anchored at the coordination site of the inhibitors, resulting in the desired metal complexes. Cell viability studies of the inhibitors and selected bifunctional compounds demonstrated the critical and unique role of each component in the inhibitor and metal complexes.