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Folate transporter dynamics and therapy with classic and tumor-targeted antifolates

Scientific reports, 2021-03, Vol.11 (1), p.6389-14, Article 6389

2021

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Development of substituted pyrido[3,2-d]pyrimidines as potent and selective dihydrofolate reductase inhibitors for pneumocystis pneumonia infection

Bioorganic & medicinal chemistry letters, 2019-08, Vol.29 (15), p.1874-1880

2019

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Design and Synthesis of Classical and Nonclassical 6-Arylthio-2,4-diamino-5-ethylpyrrolo[2,3-d]pyrimidines as Antifolates

Journal of medicinal chemistry, 2007-06, Vol.50 (13), p.3046-3053

2007

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Targeted therapy of pyrrolo[2,3-d]pyrimidine antifolates in a syngeneic mouse model of high grade serous ovarian cancer and the impact on the tumor microenvironment

Scientific reports, 2022-07, Vol.12 (1), p.11346-11346, Article 11346

2022

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Dual Targeting of Epithelial Ovarian Cancer Via Folate Receptor α and the Proton-Coupled Folate Transporter with 6-Substituted Pyrrolo[2,3- d ]pyrimidine Antifolates

Molecular cancer therapeutics, 2017-05, Vol.16 (5), p.819-830

2017

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Folate Transport and One-Carbon Metabolism in Targeted Therapies of Epithelial Ovarian Cancer

Cancers, 2021-12, Vol.14 (1), p.191

2021

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Design, Synthesis, and Biological Evaluation of 5,6,7,8-Tetrahydrobenzo[4,5]thieno[2,3- d ]pyrimidines as Microtubule Targeting Agents

Molecules (Basel, Switzerland), 2022-01, Vol.27 (1), p.321

2022

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Therapeutic targeting of a novel 6-substituted pyrrolo [2,3-d]pyrimidine thienoyl antifolate to human solid tumors based on selective uptake by the proton-coupled folate transporter

Molecular pharmacology, 2011-12, Vol.80 (6), p.1096-1107

2011

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Recent advances in classical and non-classical antifolates as antitumor and antiopportunistic infection agents: part I

Anti-cancer agents in medicinal chemistry, 2007-09, Vol.7 (5), p.524

2007

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Discovery of 5‑Substituted Pyrrolo[2,3‑d]pyrimidine Antifolates as Dual-Acting Inhibitors of Glycinamide Ribonucleotide Formyltransferase and 5‑Aminoimidazole-4-carboxamide Ribonucleotide Formyltransferase in De Novo Purine Nucleotide Biosynthesis: Implications of Inhibiting 5‑Aminoimidazole-4-carboxamide Ribonucleotide Formyltransferase to AMPK Activation and Antitumor Activity

Journal of medicinal chemistry, 2013-12, Vol.56 (24), p.10016-10032

2013

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Therapeutic targeting malignant mesothelioma with a novel 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate via its selective uptake by the proton-coupled folate transporter

Cancer chemotherapy and pharmacology, 2013-04, Vol.71 (4), p.999-1011

2013

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Recent advances in classical and non-classical antifolates as antitumor and antiopportunistic infection agents: Part II

Anti-cancer agents in medicinal chemistry, 2008-02, Vol.8 (2), p.205

2008

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Janus Compounds, 5-Chloro-N⁴-methyl-N⁴-aryl-9H-pyrimido[4,5-b]indole-2,4-diamines, Cause Both Microtubule Depolymerizing and Stabilizing Effects

Molecules (Basel, Switzerland), 2016-12, Vol.21 (12), p.1661-1661

2016

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The evolving biology of the proton‐coupled folate transporter: New insights into regulation, structure, and mechanism

The FASEB journal, 2022-02, Vol.36 (2), p.e22164-n/a

2022

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Dual Inhibitors of Thymidylate Synthase and Dihydrofolate Reductase as Antitumor Agents: Design, Synthesis, and Biological Evaluation of Classical and Nonclassical Pyrrolo[2,3-d]pyrimidine Antifolates

Journal of medicinal chemistry, 2006-02, Vol.49 (3), p.1055-1065

2006

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Therapeutic Targeting of Mitochondrial One-Carbon Metabolism in Cancer

Molecular cancer therapeutics, 2020-11, Vol.19 (11), p.2245-2255

2020

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Synthesis and Biological Evaluation of 2,4-Diamino-6-(arylaminomethyl)pyrido[2,3-d]pyrimidines as Inhibitors of Pneumocystis carinii and Toxoplasma gondii Dihydrofolate Reductase and as Antiopportunistic Infection and Antitumor Agents

Journal of medicinal chemistry, 2003-11, Vol.46 (23), p.5074-5082

2003

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EXTH-27. FLAG-003 AS A SMALL MOLECULE ORAL THERAPY FOR THE TREATMENT OF GLIOMA

Neuro-oncology (Charlottesville, Va.), 2016-11, Vol.18 (suppl_6), p.vi65-vi65

2016

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Pneumocystis carinii and Toxoplasma gondii Dihydrofolate Reductase Inhibitors and Antitumor Agents: Synthesis and Biological Activities of 2,4-Diamino-5-methyl-6-[(monosubstituted anilino)methyl]- pyrido[2,3-d]pyrimidines

Journal of medicinal chemistry, 1999-07, Vol.42 (13), p.2447-2455

1999

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The promise and challenges of exploiting the proton-coupled folate transporter for selective therapeutic targeting of cancer

Cancer chemotherapy and pharmacology, 2018-01, Vol.81 (1), p.1-15

2018

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Design, Synthesis, and Biological Evaluation of 2,4-Diamino-5-methyl-6-substituted-pyrrolo[2,3-d]pyrimidines as Dihydrofolate Reductase Inhibitors

Journal of medicinal chemistry, 2004-07, Vol.47 (14), p.3689-3692

2004

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Synthesis of N-{4-[(2,4-Diamino-5-methyl-4,7-dihydro-3H- pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-l-glutamic Acid and N-{4-[(2-Amino-4-oxo-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin- 6-yl)thio]benzoyl}-l-glutamic Acid as Dual Inhibitors of Dihydrofolate Reductase and Thymidylate Synthase and as Potential Antitumor Agents

Journal of medicinal chemistry, 2005-11, Vol.48 (23), p.7215-7222

2005

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Role of Lysine 411 in Substrate Carboxyl Group Binding to the Human Reduced Folate Carrier, as Determined by Site-Directed Mutagenesis and Affinity Inhibition

Molecular pharmacology, 2008-04, Vol.73 (4), p.1274-1281

2008

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Novel non-classical C9-methyl-5-substituted-2,4-diaminopyrrolo[2,3- d]pyrimidines as potential inhibitors of dihydrofolate reductase and as anti-opportunistic agents

Bioorganic & medicinal chemistry, 2006-12, Vol.14 (24), p.8341-8351

2006

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The human proton-coupled folate transporter: Biology and therapeutic applications to cancer

Cancer biology & therapy, 2012-12, Vol.13 (14), p.1355-1373

2012

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Folate transporter dynamics and therapy with classic and tumor-targeted antifolates

Development of substituted pyrido[3,2-d]pyrimidines as potent and selective dihydrofolate reductase inhibitors for pneumocystis pneumonia infection

Design and Synthesis of Classical and Nonclassical 6-Arylthio-2,4-diamino-5-ethylpyrrolo[2,3-d]pyrimidines as Antifolates

Targeted therapy of pyrrolo[2,3-d]pyrimidine antifolates in a syngeneic mouse model of high grade serous ovarian cancer and the impact on the tumor microenvironment

Dual Targeting of Epithelial Ovarian Cancer Via Folate Receptor α and the Proton-Coupled Folate Transporter with 6-Substituted Pyrrolo[2,3- d ]pyrimidine Antifolates

Folate Transport and One-Carbon Metabolism in Targeted Therapies of Epithelial Ovarian Cancer

Design, Synthesis, and Biological Evaluation of 5,6,7,8-Tetrahydrobenzo[4,5]thieno[2,3- d ]pyrimidines as Microtubule Targeting Agents

Therapeutic targeting of a novel 6-substituted pyrrolo [2,3-d]pyrimidine thienoyl antifolate to human solid tumors based on selective uptake by the proton-coupled folate transporter

Recent advances in classical and non-classical antifolates as antitumor and antiopportunistic infection agents: part I

Therapeutic targeting malignant mesothelioma with a novel 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate via its selective uptake by the proton-coupled folate transporter

Recent advances in classical and non-classical antifolates as antitumor and antiopportunistic infection agents: Part II

Janus Compounds, 5-Chloro-N⁴-methyl-N⁴-aryl-9H-pyrimido[4,5-b]indole-2,4-diamines, Cause Both Microtubule Depolymerizing and Stabilizing Effects

The evolving biology of the proton‐coupled folate transporter: New insights into regulation, structure, and mechanism

Dual Inhibitors of Thymidylate Synthase and Dihydrofolate Reductase as Antitumor Agents: Design, Synthesis, and Biological Evaluation of Classical and Nonclassical Pyrrolo[2,3-d]pyrimidine Antifolates

Therapeutic Targeting of Mitochondrial One-Carbon Metabolism in Cancer

Synthesis and Biological Evaluation of 2,4-Diamino-6-(arylaminomethyl)pyrido[2,3-d]pyrimidines as Inhibitors of Pneumocystis carinii and Toxoplasma gondii Dihydrofolate Reductase and as Antiopportunistic Infection and Antitumor Agents

EXTH-27. FLAG-003 AS A SMALL MOLECULE ORAL THERAPY FOR THE TREATMENT OF GLIOMA

Pneumocystis carinii and Toxoplasma gondii Dihydrofolate Reductase Inhibitors and Antitumor Agents: Synthesis and Biological Activities of 2,4-Diamino-5-methyl-6-[(monosubstituted anilino)methyl]- pyrido[2,3-d]pyrimidines

The promise and challenges of exploiting the proton-coupled folate transporter for selective therapeutic targeting of cancer

Design, Synthesis, and Biological Evaluation of 2,4-Diamino-5-methyl-6-substituted-pyrrolo[2,3-d]pyrimidines as Dihydrofolate Reductase Inhibitors

Role of Lysine 411 in Substrate Carboxyl Group Binding to the Human Reduced Folate Carrier, as Determined by Site-Directed Mutagenesis and Affinity Inhibition

Novel non-classical C9-methyl-5-substituted-2,4-diaminopyrrolo[2,3- d]pyrimidines as potential inhibitors of dihydrofolate reductase and as anti-opportunistic agents

The human proton-coupled folate transporter: Biology and therapeutic applications to cancer

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