Author

Si YangFollow

Graduation Date

Winter 10-31-2017

Availability

One-year Embargo

Submission Type

thesis

Degree Name

MS

Department

Medicinal Chemistry

School

School of Pharmacy

Committee Chair

Aleem Gangjee

Committee Member

Patrick Flaherty

Committee Member

Marc W. Harrold

Keywords

Anticancer, Antifolate, Pyrrolo[2, 3-d]pyrimidines, chemotherapy, GARFTase inhibitors, Folate Receptor, PCFT, Reduced Folate Carrier, de novo purine synthesis

Abstract

This thesis mainly focuses on the introduction of the background and work have been done in the areas of antifolates development, such as folate function, its three uptake mechanisms inside human cells, antifolates’ role in chemotherapy, et. al. In addition, the Structure-Activity-Relationship design rationale for the series of antifolates will also be discussed. Nevertheless, the details of synthesizing these pyrrolo[2,3-d]pyrimidines as potential antifolates have been described, including chemistry reviews on the pyrrolo[2,3-d]pyrimidine scaffold, and the challenges encountered and the solutions how to solve or improve in order to achieve better yield.

Language

English

Available for download on Monday, December 10, 2018

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