Cargando…

Chroman-4-One Derivatives Targeting Pteridine Reductase 1 and Showing Anti-Parasitic Activity

Flavonoids have previously been identified as antiparasitic agents and pteridine reductase 1 (PTR1) inhibitors. Herein, we focus our attention on the chroman-4-one scaffold. Three chroman-4-one analogues (1–3) of previously published chromen-4-one derivatives were synthesized and biologically evalua...

Descripción completa

Detalles Bibliográficos
Autores principales:	Di Pisa, Flavio, Landi, Giacomo, Dello Iacono, Lucia, Pozzi, Cecilia, Borsari, Chiara, Ferrari, Stefania, Santucci, Matteo, Santarem, Nuno, Cordeiro-da-Silva, Anabela, Moraes, Carolina B., Alcantara, Laura M., Fontana, Vanessa, Freitas-Junior, Lucio H., Gul, Sheraz, Kuzikov, Maria, Behrens, Birte, Pöhner, Ina, Wade, Rebecca C., Costi, Maria Paola, Mangani, Stefano
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	MDPI 2017
Materias:	Article
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6155272/ https://www.ncbi.nlm.nih.gov/pubmed/28282886 http://dx.doi.org/10.3390/molecules22030426

Ejemplares similares

Multitarget, Selective Compound Design Yields Potent Inhibitors of a Kinetoplastid Pteridine Reductase 1
por: Pöhner, Ina, et al.
Publicado: (2022)

Repurposing the Trypanosomatidic GSK Kinetobox for the Inhibition of Parasitic Pteridine and Dihydrofolate Reductases
por: Santucci, Matteo, et al.
Publicado: (2021)

Crystal structure of the ternary complex of Leishmania major pteridine reductase 1 with the cofactor NADP(+)/NADPH and the substrate folic acid
por: Dello Iacono, Lucia, et al.
Publicado: (2022)

Exploiting the 2-Amino-1,3,4-thiadiazole Scaffold To Inhibit Trypanosoma brucei Pteridine Reductase in Support of Early-Stage Drug Discovery
por: Linciano, Pasquale, et al.
Publicado: (2017)

Evidence of Pyrimethamine and Cycloguanil Analogues as Dual Inhibitors of Trypanosoma brucei Pteridine Reductase and Dihydrofolate Reductase
por: Tassone, Giusy, et al.
Publicado: (2021)

In Silico Identification and In Vitro Evaluation of Natural Inhibitors of Leishmania major Pteridine Reductase I
por: Herrmann, Fabian C., et al.
Publicado: (2017)

Sesquiterpene Lactones with Dual Inhibitory Activity against the Trypanosoma brucei Pteridine Reductase 1 and Dihydrofolate Reductase
por: Possart, Katharina, et al.
Publicado: (2021)

Accelerating Drug Discovery Efforts for Trypanosomatidic Infections Using an Integrated Transnational Academic Drug Discovery Platform
por: Moraes, Carolina B., et al.
Publicado: (2019)

Combined gene deletion of dihydrofolate reductase-thymidylate synthase and pteridine reductase in Leishmania infantum
por: Bhattacharya, Arijit, et al.
Publicado: (2021)

Evidence of Destabilization of the Human Thymidylate Synthase (hTS) Dimeric Structure Induced by the Interface Mutation Q62R
por: Pozzi, Cecilia, et al.
Publicado: (2019)

Development and validation of a cytochrome c-coupled assay for pteridine reductase 1 and dihydrofolate reductase
por: Shanks, Emma J., et al.
Publicado: (2010)

Identification of Kaurane-Type Diterpenes as Inhibitors of Leishmania Pteridine Reductase I
por: Herrera-Acevedo, Chonny, et al.
Publicado: (2021)

Structure and reactivity of Trypanosoma brucei pteridine reductase: inhibition by the archetypal antifolate methotrexate
por: Dawson, Alice, et al.
Publicado: (2006)

Dissecting the Metabolic Roles of Pteridine Reductase 1 in Trypanosoma brucei and Leishmania major
por: Ong, Han B., et al.
Publicado: (2011)

Trypanosoma brucei pteridine reductase 1 is essential for survival in vitro and for virulence in mice
por: Sienkiewicz, Natasha, et al.
Publicado: (2010)

Structure-Based Design and Synthesis of Antiparasitic Pyrrolopyrimidines Targeting Pteridine Reductase 1
por: Khalaf, Abedawn I., et al.
Publicado: (2014)

In Silico and In Vitro Search for Dual Inhibitors of the Trypanosoma brucei and Leishmania major Pteridine Reductase 1 and Dihydrofolate Reductase
por: Possart, Katharina, et al.
Publicado: (2023)

Structure of recombinant Leishmania donovani pteridine reductase reveals a disordered active site
por: Barrack, Keri L., et al.
Publicado: (2010)

Structure-Based Design of Pteridine Reductase Inhibitors Targeting African Sleeping Sickness and the Leishmaniases
por: Tulloch, Lindsay B., et al.
Publicado: (2009)

Design, Synthesis and Biological Evaluation of Novel Inhibitors of Trypanosoma brucei Pteridine Reductase 1
por: Spinks, Daniel, et al.
Publicado: (2011)

Design, Synthesis and Antiparasitic Evaluation of Click Phospholipids
por: Magoulas, George E., et al.
Publicado: (2021)

Structure and dynamics of pteridine reductase 1: the key phenomena relevant to enzyme function and drug design
por: Panecka-Hofman, Joanna, et al.
Publicado: (2023)

Dual and selective inhibitors of pteridine reductase 1 (PTR1) and dihydrofolate reductase-thymidylate synthase (DHFR-TS) from Leishmania chagasi
por: Teixeira, Bárbara Velame Ferreira, et al.
Publicado: (2019)

High-Throughput Phenotypic Screening and Machine Learning Methods Enabled the Selection of Broad-Spectrum Low-Toxicity Antitrypanosomatidic Agents
por: Linciano, Pasquale, et al.
Publicado: (2023)

Gene Regulation of Pteridine Reductase 1 in Leishmania Promastigotes and Amastigotes Using a Full-Length Antisense Construct
por: Kheirandish, F, et al.
Publicado: (2013)

Application of a simple quantum chemical approach to ligand fragment scoring for Trypanosoma brucei pteridine reductase 1 inhibition
por: Jedwabny, Wiktoria, et al.
Publicado: (2017)

Structural and Functional Characterization of the Human Thymidylate Synthase (hTS) Interface Variant R175C, New Perspectives for the Development of hTS Inhibitors
por: Pozzi, Cecilia, et al.
Publicado: (2019)

3-Nitro-2-phenylchroman
por: Zhao, Pei-Hua, et al.
Publicado: (2012)

3-Bromochroman-4-one
por: Shaikh, Mahidansha M., et al.
Publicado: (2013)

Identification of Novel Potential Inhibitors of Pteridine Reductase 1 in Trypanosoma brucei via Computational Structure-Based Approaches and in Vitro Inhibition Assays
por: Kimuda, Magambo Phillip, et al.
Publicado: (2019)

Cooption of the pteridine biosynthesis pathway underlies the diversification of embryonic colors in water striders
por: Vargas-Lowman, Aidamalia, et al.
Publicado: (2019)

Structural Comparison of Enterococcus faecalis and Human Thymidylate Synthase Complexes with the Substrate dUMP and Its Analogue FdUMP Provides Hints about Enzyme Conformational Variabilities
por: Pozzi, Cecilia, et al.
Publicado: (2019)

An orally effective dihydropyrimidone (DHPM) analogue induces apoptosis-like cell death in clinical isolates of Leishmania donovani overexpressing pteridine reductase 1
por: Singh, Neeloo, et al.
Publicado: (2009)

One Scaffold, Three Binding Modes: Novel and Selective Pteridine Reductase 1 Inhibitors Derived from Fragment Hits Discovered by Virtual Screening
por: Mpamhanga, Chidochangu P., et al.
Publicado: (2009)

Comparison of Pteridine Normalization Methods in Urine for Detection of Bladder Cancer
por: Kośliński, Piotr, et al.
Publicado: (2020)

1H-Benzo[g]pteridine-2,4-dione
por: Uppu, Rao M., et al.
Publicado: (2023)

Urinary pteridines as a discriminator of atherosclerotic risk in patients with diabetes
por: Marumo, Mikio, et al.
Publicado: (2021)

Structural Bases for the Synergistic Inhibition of Human Thymidylate Synthase and Ovarian Cancer Cell Growth by Drug Combinations
por: Pozzi, Cecilia, et al.
Publicado: (2021)

Doubly Decarboxylative Synthesis of 4-(Pyridylmethyl)chroman-2-ones and 2-(Pyridylmethyl)chroman-4-ones under Mild Reaction Conditions †
por: Bojanowski, Jan, et al.
Publicado: (2021)

Advances in Leishmania Research: From Basic Parasite Biology to Disease Control
por: Santarém, Nuno, et al.
Publicado: (2023)

Cannot write session to /tmp/vufind_sessions/sess_sanq741caoijr7paladkbakc7s