Thieno[2,3‐d]pyrimidine‐Core Compounds Show Activity against Clinically Relevant Gram‐Positive Bacteria
Sign Up to like & getrecommendations! Published in 2022 at "ChemMedChem"
DOI: 10.1002/cmdc.202200207
Abstract: Thieno[2,3‐d]pyrimidines represent a novel antibacterial prodrug scaffold, previously identified through a screening campaign against Mycobacterium tuberculosis in which the formation of highly antimycobacterial metabolites catalyzed by the nitroreductase Mrx2 is suggested to be the relevant… read more here.
Keywords: thieno pyrimidine; pyrimidine core; activity; core compounds ... See more keywords
A novel thieno[2,3-d]pyrimidine derivative inhibiting vascular endothelial growth factor receptor-2: A story of computer-aided drug discovery.
Sign Up to like & getrecommendations! Published in 2023 at "Drug development research"
DOI: 10.1002/ddr.22083
Abstract: Following the pharmacophoric features of vascular endothelial growth factor receptor 2 (VEGFR-2) inhibitors, a novel thieno[2,3-d]pyrimidine derivative has been designed and its activity against VEGFR-2 has been demonstrated by molecular docking studies that showed an… read more here.
Keywords: pyrimidine derivative; growth; thieno pyrimidine; drug ... See more keywords
Subtle modifications to a thieno[2,3-d]pyrimidine scaffold yield negative allosteric modulators and agonists of the dopamine D2 receptor.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.01.061
Abstract: We recently described a structurally novel series of negative allosteric modulators (NAMs) of the dopamine D2 receptor (D2R) based on thieno[2,3-d]pyrimidine 1, showing it can be structurally simplified to reveal low molecular weight, fragment-like NAMs… read more here.
Keywords: allosteric modulators; thieno pyrimidine; negative allosteric; dopamine receptor ... See more keywords
Design, synthesis, biological evaluation and molecular docking study of novel thieno[3,2-d]pyrimidine derivatives as potent FAK inhibitors.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.112024
Abstract: A series of 2,7-disubstituted-thieno[3,2-d]pyrimidine derivatives were designed, synthesized and evaluated as novel focal adhesion kinase (FAK) inhibitors. The novel 2,7-disubstituted-thieno[3,2-d]pyrimidine scaffold has been designed as a new kinase inhibitor platform that mimics the bioactive conformation… read more here.
Keywords: mda 231; compound 26f; pyrimidine derivatives; thieno pyrimidine ... See more keywords
Electrospray ionization collision induced dissociation of thieno[3,2-d]pyrimidine derivatives
Sign Up to like & getrecommendations! Published in 2020 at "International Journal of Mass Spectrometry"
DOI: 10.1016/j.ijms.2020.116411
Abstract: Abstract 2,4-substituted thieno[3,2-d]pyrimidines, with different l -amino acid methyl ester substituent on 4-C and methyl or methylthio substituent on 2-C, showed a complex and analytically valuable fragmentation behaviour under positive ion electrospray ionization collision-induced dissociation… read more here.
Keywords: induced dissociation; pyrimidine derivatives; thieno pyrimidine; ionization collision ... See more keywords
Discovery of a Potent Thieno[2,3-d]pyrimidine-2,4-dione-Based Protoporphyrinogen IX Oxidase Inhibitor through an In Silico Structure-Guided Optimization Approach.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of agricultural and food chemistry"
DOI: 10.1021/acs.jafc.1c05665
Abstract: A key objective for herbicide research is to develop new compounds with improved bioactivity. Protoporphyrinogen IX oxidase (PPO) is an essential target for herbicide discovery. Here, we report using an in silico structure-guided optimization approach… read more here.
Keywords: thieno pyrimidine; pyrimidine dione; structure guided; guided optimization ... See more keywords
Identification of Thieno[3,2-d]pyrimidine Derivatives as Dual Inhibitors of Focal Adhesion Kinase and FMS-like Tyrosine Kinase 3.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00459
Abstract: Focal adhesion kinase (FAK) is overexpressed in highly invasive and metastatic cancers. To identify novel FAK inhibitors, we designed and synthesized various thieno[3,2-d]pyrimidine derivatives. An intensive structure-activity relationship (SAR) study led to the identification of… read more here.
Keywords: focal adhesion; adhesion kinase; kinase; pyrimidine derivatives ... See more keywords
Thieno[2,3-d]pyrimidine-Based Positive Allosteric Modulators of Human Mas-Related G Protein-Coupled Receptor X1 (MRGPRX1).
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01709
Abstract: Mas-related G protein-coupled receptor X1 (MRGPRX1) is a human sensory neuron-specific receptor and potential target for the treatment of pain. Positive allosteric modulators (PAMs) of MRGPRX1 have the potential to preferentially activate the receptors at… read more here.
Keywords: mrgprx1; receptor; thieno pyrimidine; mas related ... See more keywords
Rapid Access to Kinase Inhibitor Pharmacophores by Regioselective C-H Arylation of Thieno[2,3-d]pyrimidine.
Sign Up to like & getrecommendations! Published in 2020 at "Organic letters"
DOI: 10.1021/acs.orglett.0c00143
Abstract: Regioselective C-H arylations of thieno[2,3-d]pyrimidine are accomplished under palladium catalysis. Thieno[2,3-d]pyrimidines react with aryl iodides at the C6-position and with aryl boronic acids at the C5-position, showing excellent regioselectivity. Mechanistic investigations indicate that the regioselectivity… read more here.
Keywords: rapid access; kinase; pyrimidine; arylation ... See more keywords
Synthesis, Antitumor Activity, and In Silico Drug Design of New Thieno[2,3-d]Pyrimidine-4-One Derivatives as Nonclassical Lipophilic Dihydrofolate Reductase Inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "ACS Omega"
DOI: 10.1021/acsomega.2c06078
Abstract: Synthesis of a new series of 20 compounds bearing the thieno[2,3-d]pyrimidine-4-one scaffold was achieved. The inhibitory activity of these compounds was performed over 60 cell lines of human tumor at single and five dose concentrations.… read more here.
Keywords: antitumor; thieno pyrimidine; pyrimidine one; activity ... See more keywords
Synthesis of Some New Substituted Thieno[2,3-d]pyrimidine Derivatives as Antimicrobial Agents
Sign Up to like & getrecommendations! Published in 2019 at "Russian Journal of General Chemistry"
DOI: 10.1134/s1070363219070247
Abstract: A series of thieno-pyrimidine derivatives are synthesized from 5′-amino-2,3′-bithiophene-4′-carboxylate via the corresponding intermediate N-benzoylated carboxamide derivatives. The target compounds are tested for antibacterial and antifungal activity. Some of the synthesized compounds demonstrate potent antibacterial activity… read more here.
Keywords: thieno pyrimidine; derivatives antimicrobial; substituted thieno; synthesis new ... See more keywords