Supervisor's Name: Youla Tsantrizos
Supervisor's Email: youla.tsantrizos [at] mcgill.ca
Supervisor's Phone: (514) 398-3638
Supervisor's Website: http://tsantrizos-group.mcgill.ca
Supervisor's department: Chemistry
Course number: CHEM 396 (Chemistry)
Term: Fall 2013-2014
Project start date: Tuesday, September 3, 2013
Project end date: Tuesday, December 3, 2013
Project title: Design and Synthesis of Novel N-BPs
Project description (50-100 words suggested): It is estimated that more than 250,000 new cases of cancer will be diagnosed in Canada in 2013 (according to the Canadian cancer society) and new molecular tools for the treatment of cancer are desperately needed. Nitrogen-containing bisphosphonates (N-BPs) are clinically validated drugs for the treatment of bone cancer metastasis, which claims the lives of approximately 70% of all breast and prostate cancer patients. N-BPs inhibit the human Farnesyl Pyrophosphate Synthase (hFPPS), an enzyme which is important for cancer proliferation. Currently available N-BPs suffer from poor selectivity and are difficult to administer to patients due to their extremely low oral bioavailability. This CHEM 396 project will involve the design and synthesis of novel N-BPs with improved biopharmaceutical properties to address these issues. In particular we aim to synthesize novel inhibitors for hFPPS based on a spiral indole scaffold that would occupy a larger portion of the enzyme’s active site cavity. The project will involve synthesis and structural characterization of many new compounds, as well as learning about the biochemistry involved in oncogenesis.
Prerequisite: 1 term completed at McGill + CGPA of 3.0 or higher; or permission of instructor.
Grading scheme (The final report must be worth at least 50% of final grade): 25% for lab work; 25% for group participation at meeting and presentations of the research; 50% for final report.
Project status: This project is taken.
Ethics, safety, and training: Supervisors are responsible for the ethics and safety compliance of undergraduate students. This project involves: Biohazardous substances; Handling chemicals