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Antifolate agents: a patent review (2006 – 2010)

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Pages 1293-1308 | Published online: 27 May 2011

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Mansi, Pankaj Khanna, Deepshikha Gupta, Shilpa Yadav & Leena Khanna. (2023) Hydrotrope assisted green synthesis of dicoumarols and in silico and in vitro antibacterial, antioxidant and xanthine oxidase inhibition studies. Journal of Biomolecular Structure and Dynamics 41:19, pages 9651-9665.
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Tanuja Joshi, Hemlata Pundir & Subhash Chandra. (2022) Deep-learning based repurposing of FDA-approved drugs against Candida albicans dihydrofolate reductase and molecular dynamics study. Journal of Biomolecular Structure and Dynamics 40:18, pages 8420-8436.
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Amy C Anderson & Dennis L Wright. (2014) Antifolate agents: a patent review (2010 – 2013). Expert Opinion on Therapeutic Patents 24:6, pages 687-697.
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Articles from other publishers (26)

Keith Lange, Kathleen M. Frey, Tyler Eck, Cheryl A. Janson, Ueli Gubler & Nina M. Goodey. (2023) Crystal structure of dihydrofolate reductase from the filarial nematode W. bancrofti in complex with NADPH and folate. PLOS Neglected Tropical Diseases 17:4, pages e0011303.
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O. V. Kholodniak, M. Tniguer, I. S. Nosulenko, A. O. Kinichenko, K. I. Kandybey, O. M. Antypenko & S. I. Kovalenko. (2022) 1-Cycloalkanecarbonyl-substituted thioureas and thiosemicarbazides as effective dihydrofolate reductase inhibitors with antibacterial activity. Biopolymers and Cell 38:1, pages 26-36.
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Vishal Sangha, Erica I. Williams, Patrick T. Ronaldson & Reina Bendayan. 2022. Drug Transporters. Drug Transporters 283 317 .
Yue Li, Yifan Ouyang, Han Wu, Peng Wang, Yu Huang, Xue Li, Hongtong Chen, Yu Sun, Xinxin Hu, Xiukun Wang, Guoqing Li, Yun Lu, Congran Li, Xi Lu, Jing Pang, Tongying Nie, Xiaohong Sang, Luyao Dong, Wenting Dong, Jiandong Jiang, Ian C. Paterson, Xinyi Yang, Wei Hong, Hao Wang & Xuefu You. (2022) The discovery of 1, 3-diamino-7H-pyrrol[3, 2-f]quinazoline compounds as potent antimicrobial antifolates. European Journal of Medicinal Chemistry 228, pages 113979.
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Galal H. Elgemeie & Reham A. Mohamed-Ezzat. 2022. New Strategies Targeting Cancer Metabolism. New Strategies Targeting Cancer Metabolism 1 33 .
Danuta Drozdowska. 2022. Comprehensive Pharmacology. Comprehensive Pharmacology 271 294 .
Tian-Yi Zhang, Chun-Shi Li, Ming-Yue Cui, Xue-Qian Bai, Jiang-Hui Chen, Ze-Wen Song, Bo Feng & Xue-Kun Liu. (2020) Design, synthesis and evaluation of dihydrotriazine derivatives-bearing 5-aryloxypyrazole moieties as antibacterial agents. Molecular Diversity 25:2, pages 861-876.
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Jacynthe L. Toulouse, Genbin ShiClaudèle Lemay-St-Denis, Maximilian C. C. J. C. Ebert, Daniel Deon, Marc Gagnon, Edward Ruediger, Kévin Saint-Jacques, Delphine Forge, Jean Jacques Vanden Eynde, Anne Marinier, Xinhua Ji & Joelle N. Pelletier. (2020) Dual-Target Inhibitors of the Folate Pathway Inhibit Intrinsically Trimethoprim-Resistant DfrB Dihydrofolate Reductases. ACS Medicinal Chemistry Letters 11:11, pages 2261-2267.
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Jungang Chen, Haiwei Zhang & Xulin Chen. (2020) Pemetrexed inhibits Kaposi's sarcoma-associated herpesvirus replication through blocking dTMP synthesis. Antiviral Research 180, pages 104825.
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Agnieszka Wróbel, Karolina Arciszewska, Dawid Maliszewski & Danuta Drozdowska. (2019) Trimethoprim and other nonclassical antifolates an excellent template for searching modifications of dihydrofolate reductase enzyme inhibitors. The Journal of Antibiotics 73:1, pages 5-27.
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Manickam Yogavel, Joanne E. Nettleship, Akansha Sharma, Karl Harlos, Abhishek Jamwal, Rini Chaturvedi, Manmohan Sharma, Vitul Jain, Jyoti Chhibber-Goel & Amit Sharma. (2018) Structure of 6-hydroxymethyl-7,8-dihydropterin pyrophosphokinase–dihydropteroate synthase from Plasmodium vivax sheds light on drug resistance. Journal of Biological Chemistry 293:39, pages 14962-14972.
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Xuan Yang, Wassihun Wedajo, Yoshiyuki Yamada, Sue-Li Dahlroth, Jason Jun-Long Neo, Thomas Dick & Wai-Keung Chui. (2018) 1,3,5-triazaspiro[5.5]undeca-2,4-dienes as selective Mycobacterium tuberculosis dihydrofolate reductase inhibitors with potent whole cell activity. European Journal of Medicinal Chemistry 144, pages 262-276.
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Joanna Panecka-Hofman, Ina Pöhner, Francesca Spyrakis, Talia Zeppelin, Flavio Di Pisa, Lucia Dello Iacono, Alessio Bonucci, Antonio Quotadamo, Alberto Venturelli, Stefano Mangani, Maria Paola Costi & Rebecca C. Wade. (2017) Comparative mapping of on-targets and off-targets for the discovery of anti-trypanosomatid folate pathway inhibitors. Biochimica et Biophysica Acta (BBA) - General Subjects 1861:12, pages 3215-3230.
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Geoffrey Schwertz, Matthias C. Witschel, Matthias Rottmann, Roger Bonnert, Ubolsree Leartsakulpanich, Penchit Chitnumsub, Aritsara Jaruwat, Wanwipa Ittarat, Anja Schäfer, Raphael A. Aponte, Susan A. Charman, Karen L. White, Abhijit Kundu, Surajit Sadhukhan, Mel Lloyd, Gail M. Freiberg, Myron Srikumaran, Marc Siggel, Adrian Zwyssig, Pimchai Chaiyen & François Diederich. (2017) Antimalarial Inhibitors Targeting Serine Hydroxymethyltransferase (SHMT) with in Vivo Efficacy and Analysis of their Binding Mode Based on X-ray Cocrystal Structures. Journal of Medicinal Chemistry 60:12, pages 4840-4860.
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Kinga Nyíri & Beáta G. Vértessy. (2017) Perturbation of genome integrity to fight pathogenic microorganisms. Biochimica et Biophysica Acta (BBA) - General Subjects 1861:1, pages 3593-3612.
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Daniel M. Czyż, Neeta Jain-Gupta, Howard A. Shuman & Sean Crosson. (2016) A dual-targeting approach to inhibit Brucella abortus replication in human cells. Scientific Reports 6:1.
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Amrisha Bhosle & Nagasuma Chandra. (2016) Structural analysis of dihydrofolate reductases enables rationalization of antifolate binding affinities and suggests repurposing possibilities. FEBS Journal 283:6, pages 1139-1167.
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Anuradha Kumar, Ana Guardia, Gonzalo Colmenarejo, Esther Pérez, Ruben R. Gonzalez, Pedro Torres, David Calvo, Ruben M. Gómez, Fátima Ortega, Elena Jiménez, Raquel C. Gabarro, Joaquín Rullás, Lluis Ballell & David R. Sherman. (2015) A Focused Screen Identifies Antifolates with Activity on Mycobacterium tuberculosis . ACS Infectious Diseases 1:12, pages 604-614.
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Nagendra Muddala, Baskar Nammalwar, Subhashini Selvaraju, Christina Bourne, Mary Henry, Richard Bunce, K. Berlin, Esther Barrow & William Barrow. (2015) Evaluation of New Dihydrophthalazine-Appended 2,4-Diaminopyrimidines against Bacillus anthracis: Improved Syntheses Using a New Pincer Complex. Molecules 20:4, pages 7222-7244.
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Kristen M. Lamb, Michael N. Lombardo, Jeremy Alverson, Nigel D. Priestley, Dennis L. Wright & Amy C. Anderson. (2014) Crystal Structures of Klebsiella pneumoniae Dihydrofolate Reductase Bound to Propargyl-Linked Antifolates Reveal Features for Potency and Selectivity. Antimicrobial Agents and Chemotherapy 58:12, pages 7484-7491.
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Baskar Nammalwar, N. Muddala, Christina Bourne, Mary Henry, Philip Bourne, Richard Bunce, Esther Barrow, K. Berlin & William Barrow. (2014) Synthesis and Biological Evaluation of 2,4-Diaminopyrimidine-Based Antifolate Drugs against Bacillus anthracis. Molecules 19:3, pages 3231-3246.
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Sandra Piras, Antonio Carta, Irene Briguglio, Paola Corona, Giuseppe Paglietti, Rosaria Luciani, Maria Paola Costi & Stefania Ferrari. (2014) 2-[N-Alkyl(R-phenyl)-aminomethyl]-3-phenyl-7-trifluoromethylquinoxalines as anticancer agents inhibitors of folate enzymes. European Journal of Medicinal Chemistry 75, pages 169-183.
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Christina R. Bourne, Nancy Wakeham, Nicole Webb, Baskar Nammalwar, Richard A. Bunce, K. Darrell Berlin & William W. Barrow. (2014) The Structure and Competitive Substrate Inhibition of Dihydrofolate Reductase from Enterococcus faecalis Reveal Restrictions to Cofactor Docking . Biochemistry 53:7, pages 1228-1238.
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Christina Bourne. (2014) Utility of the Biosynthetic Folate Pathway for Targets in Antimicrobial Discovery. Antibiotics 3:1, pages 1-28.
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Christina R. Bourne, Nancy Wakeham, Baskar Nammalwar, Vladimir Tseitin, Philip C. Bourne, Esther W. Barrow, Shankari Mylvaganam, Kal Ramnarayan, Richard A. Bunce, K. Darrell Berlin & William W. Barrow. (2013) Structure–activity relationship for enantiomers of potent inhibitors of B. anthracis dihydrofolate reductase. Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics 1834:1, pages 46-52.
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Clarissa M. Czekster & John S. Blanchard. (2012) One Substrate, Five Products: Reactions Catalyzed by the Dihydroneopterin Aldolase from Mycobacterium tuberculosis. Journal of the American Chemical Society 134:48, pages 19758-19771.
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