81136-47-2Relevant academic research and scientific papers
4-Substituted thieno[2,3-d]pyrimidines as potent antibacterial agents: Rational design, microwave-assisted synthesis, biological evaluation and molecular docking studies
Gill, Rupinder K.,Singh, Harpreet,Raj, Tilak,Sharma, Anuradha,Singh, Gagandeep,Bariwal, Jitender
, p. 1115 - 1121 (2017/10/06)
In an attempt to discover a new class of antibacterial agents with improved efficacy and to overcome the drug-resistant problems, some novel 4-substituted thieno[2,3-d]pyrimidines have been synthesized via microwave-assisted methodology and evaluated for their in vitro antibacterial activity against various pathogenic bacterial strains. Compounds 12b and 13c showed the promising inhibitory potencies against Staphylococcus aureus, Bacillus subtilis, Pseudomonas aeruginosa and Escherichia coli with MICs ranging from 2 to 10?μg/ml. Compound 13c was also found to be highly potent against methicillin-resistant S. aureus (MRSA) with MIC value of 4?μg/ml. Docking simulation studies have been performed to unravel the mode of action and association study indicate the binding of potent compounds with DHPS enzyme. In silico ADME studies suggest the drug-like characteristics of the potent compounds.
Synthesis and study of antiproliferative activity of novel thienopyrimidines on glioblastoma cells
Pédeboscq, Stéphane,Gravier, Denis,Casadebaig, Fran?oise,Hou, Geneviève,Gissot, Arnaud,De Giorgi, Francesca,Ichas, Fran?ois,Cambar, Jean,Pometan, Jean-Paul
experimental part, p. 2473 - 2479 (2010/07/08)
The receptor tyrosine kinases (for example EGFR, PDGFR, VEGFR) are a transmembrane protein family which plays a crucial role in tumor growth, survival, metastasis dissemination and angiogenesis. During the past 10 years, many tyrosine kinase inhibitors (T
