Tumor Targeting with Novel 6-Substituted Pyrrolo [2,3-d] Pyrimidine Antifolates with Heteroatom Bridge Substitutions via Cellular Uptake by Folate Receptor α and the Proton-Coupled Folate Transporter and Inhibition of de Novo Purine Nucleotide Biosynthesis

Author:

Golani Lalit K.1,Wallace-Povirk Adrianne2,Deis Siobhan M.3,Wong Jennifer3,Ke Jiyuan4,Gu Xin4,Raghavan Sudhir1,Wilson Mike R.5,Li Xinxin1,Polin Lisa25,de Waal Parker W.4,White Kathryn25,Kushner Juiwanna25,O’Connor Carrie2,Hou Zhanjun25,Xu H. Eric46,Melcher Karsten4,Dann Charles E.3,Matherly Larry H.257,Gangjee Aleem1

Affiliation:

1. Division of Medicinal Chemistry, Graduate School of Pharmaceutical Sciences, Duquesne University, 600 Forbes Avenue, Pittsburgh, Pennsylvania 15282, United States

2. Molecular Therapeutics Program, Barbara Ann Karmanos Cancer Institute, 110 East Warren Avenue, Detroit, Michigan 48201, United States

3. Department of Chemistry, Indiana University, Bloomington, Indiana 47405, United States

4. Laboratory of Structural Sciences and Laboratory of Structural Biology and Biochemistry, Van Andel Research Institute, 333 Bostwick Avenue NE, Grand Rapids, Michigan 49503, United States

5. Department of Oncology, Wayne State University School of Medicine, Detroit, Michigan 48201, United States

6. Key Laboratory of Receptor Research, VARI-SIMM Center, Center for Structure and Function of Drug Targets, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 201203, People’s Republic of China

7. Department of Pharmacology, Wayne State University School of Medicine, Detroit, Michigan 48201, United States

Funder

National Cancer Institute

Van Andel Research Institute

Ministry of Science and Technology of the People's Republic of China

National Institute of Diabetes and Digestive and Kidney Diseases

National Institute of General Medical Sciences

National Science Foundation

Eunice and Milt Ring Endowed Chair for Cancer Research

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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