Synthesis and Biological Activity of a Novel Series of 6-Substituted Thieno[2,3-d]pyrimidine Antifolate Inhibitors of Purine Biosynthesis with Selectivity for High Affinity Folate Receptors over the Reduced Folate Carrier and Proton-Coupled Folate Transporter for Cellular Entry†

Yijun Deng; Xilin Zhou; Sita Kugel Desmoulin; Jianmei Wu; Christina Cherian; Zhanjun Hou; Larry H. Matherly; Aleem Gangjee

doi:10.1021/jm8011323

Synthesis and Biological Activity of a Novel Series of 6-Substituted Thieno[2,3-d]pyrimidine Antifolate Inhibitors of Purine Biosynthesis with Selectivity for High Affinity Folate Receptors over the Reduced Folate Carrier and Proton-Coupled Folate Transporter for Cellular Entry†

Journal of Medicinal Chemistry ◽

10.1021/jm8011323 ◽

2009 ◽

Vol 52 (9) ◽

pp. 2940-2951 ◽

Cited By ~ 57

Author(s):

Yijun Deng ◽

Xilin Zhou ◽

Sita Kugel Desmoulin ◽

Jianmei Wu ◽

Christina Cherian ◽

...

Keyword(s):

Biological Activity ◽

Purine Biosynthesis ◽

Reduced Folate Carrier ◽

Folate Receptors ◽

High Affinity ◽

Cellular Entry

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Synthesis and Biological Activity of 6-Substituted Pyrrolo[2,3-d]pyrimidine Thienoyl Regioisomers as Inhibitors of de Novo Purine Biosynthesis with Selectivity for Cellular Uptake by High Affinity Folate Receptors and the Proton-Coupled Folate Transporter over the Reduced Folate Carrier

Journal of Medicinal Chemistry ◽

10.1021/jm201688n ◽

2012 ◽

Vol 55 (4) ◽

pp. 1758-1770 ◽

Cited By ~ 34

Author(s):

Lei Wang ◽

Christina Cherian ◽

Sita Kugel Desmoulin ◽

Shermaine Mitchell-Ryan ◽

Zhanjun Hou ◽

...

Keyword(s):

Biological Activity ◽

Cellular Uptake ◽

De Novo ◽

Purine Biosynthesis ◽

Reduced Folate Carrier ◽

Folate Receptors ◽

High Affinity ◽

De Novo Purine Biosynthesis

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Synthesis and Antitumor Activity of a Novel Series of 6-Substituted Pyrrolo[2,3-d]pyrimidine Thienoyl Antifolate Inhibitors of Purine Biosynthesis with Selectivity for High Affinity Folate Receptors and the Proton-Coupled Folate Transporter over the Reduced Folate Carrier for Cellular Entry

Journal of Medicinal Chemistry ◽

10.1021/jm9015729 ◽

2010 ◽

Vol 53 (3) ◽

pp. 1306-1318 ◽

Cited By ~ 44

Author(s):

Lei Wang ◽

Christina Cherian ◽

Sita Kugel Desmoulin ◽

Lisa Polin ◽

Yijun Deng ◽

...

Keyword(s):

Antitumor Activity ◽

Purine Biosynthesis ◽

Reduced Folate Carrier ◽

Folate Receptors ◽

High Affinity ◽

Cellular Entry

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Discovery of Novel Antifolate Inhibitors of De Novo Purine Nucleotide Biosynthesis with Selectivity for High Affinity Folate Receptors and the Proton-Coupled Folate Transporter Over the Reduced Folate Carrier for Cellular Entry

Targeted Drug Strategies for Cancer and Inflammation ◽

10.1007/978-1-4419-8417-3_6 ◽

2011 ◽

pp. 119-134 ◽

Cited By ~ 3

Author(s):

Larry H. Matherly ◽

Aleem Gangjee

Keyword(s):

De Novo ◽

Reduced Folate Carrier ◽

Purine Nucleotide ◽

Nucleotide Biosynthesis ◽

Folate Receptors ◽

High Affinity ◽

Cellular Entry

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Design, synthesis and biological evaluation of novel pyrrolo[2,3-d]pyrimidine as tumor-targeting agents with selectivity for tumor uptake by high affinity folate receptors over the reduced folate carrier

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2020.115544 ◽

2020 ◽

Vol 28 (12) ◽

pp. 115544 ◽

Cited By ~ 1

Author(s):

Lalit K. Golani ◽

Farhana Islam ◽

Carrie O'Connor ◽

Aamod S. Dekhne ◽

Zhanjun Hou ◽

...

Keyword(s):

Tumor Targeting ◽

Biological Evaluation ◽

Reduced Folate Carrier ◽

Tumor Uptake ◽

Design Synthesis ◽

Folate Receptors ◽

High Affinity ◽

Synthesis And Biological Evaluation

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Design and biological activity of new high-affinity ligands for the urokinase-type plasminogen activator receptor (CD87)

Peptides for the New Millennium - American Peptide Symposia ◽

10.1007/0-306-46881-6_215 ◽

2006 ◽

pp. 543-545

Author(s):

Niko Schmiedeberg ◽

Markus Bürgle ◽

Olaf Wilhelm ◽

Friedrich Lottspeich ◽

Henner Graeff ◽

...

Keyword(s):

Biological Activity ◽

Plasminogen Activator ◽

Affinity Ligands ◽

High Affinity ◽

Type Plasminogen Activator ◽

Urokinase Type Plasminogen Activator ◽

Plasminogen Activator Receptor

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Synthesis and biological activity of high-affinity retinoic acid receptor antagonists

Bioorganic & Medicinal Chemistry ◽

10.1016/s0968-0896(99)00055-3 ◽

1999 ◽

Vol 7 (7) ◽

pp. 1321-1338 ◽

Cited By ~ 31

Author(s):

Alan T. Johnson ◽

Liming Wang ◽

Andrew M. Standeven ◽

Maria Escobar ◽

Roshantha A.S. Chandraratna

Keyword(s):

Biological Activity ◽

Retinoic Acid ◽

Retinoic Acid Receptor ◽

Receptor Antagonists ◽

Acid Receptor ◽

High Affinity

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Characterization of a Folate Transporter in HeLa Cells with a Low pH Optimum and High Affinity for Pemetrexed Distinct from the Reduced Folate Carrier

Clinical Cancer Research ◽

10.1158/1078-0432.ccr-04-0645 ◽

2004 ◽

Vol 10 (18) ◽

pp. 6256-6264 ◽

Cited By ~ 59

Author(s):

Yanhua Wang ◽

Rongbao Zhao ◽

I. David Goldman

Keyword(s):

Hela Cells ◽

Low Ph ◽

Reduced Folate Carrier ◽

Ph Optimum ◽

High Affinity

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Epidermal growth factor: Biological activity requires persistent occupation of high-affinity cell surface receptors

Proceedings of the National Academy of Sciences ◽

10.1073/pnas.75.12.5788 ◽

1978 ◽

Vol 75 (12) ◽

pp. 5788-5791 ◽

Cited By ~ 93

Author(s):

Y. Shechter ◽

L. Hernaez ◽

P. Cuatrecasas

Keyword(s):

Biological Activity ◽

Growth Factor ◽

Epidermal Growth Factor ◽

Cell Surface ◽

Cell Surface Receptors ◽

Surface Receptors ◽

High Affinity ◽

Epidermal Growth

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Evidence that biological activity of NGF is mediated through a novel subclass of high affinity receptors

Neuron ◽

10.1016/0896-6273(91)90067-a ◽

1991 ◽

Vol 6 (4) ◽

pp. 649-663 ◽

Cited By ~ 195

Author(s):

Gisela Weskamp ◽

Louis F. Reichardt

Keyword(s):

Biological Activity ◽

High Affinity

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Designed Nanocage Displaying Ligand-Specific Peptide Bunches for High Affinity and Biological Activity

ACS Nano ◽

10.1021/nn403184u ◽

2013 ◽

Vol 7 (9) ◽

pp. 7462-7471 ◽

Cited By ~ 51

Author(s):

Jae Og Jeon ◽

Soyoun Kim ◽

Eunsu Choi ◽

Kihyuk Shin ◽

Kiweon Cha ◽

...

Keyword(s):

Biological Activity ◽

High Affinity ◽

Specific Peptide

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