209853-24-7Relevant academic research and scientific papers
Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2- d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors
Romagnoli, Romeo,Prencipe, Filippo,Oliva, Paola,Baraldi, Stefania,Baraldi, Pier Giovanni,Schiaffino Ortega, Santiago,Chayah, Mariem,Kimatrai Salvador, Maria,Lopez-Cara, Luisa Carlota,Brancale, Andrea,Ferla, Salvatore,Hamel, Ernest,Ronca, Roberto,Bortolozzi, Roberta,Mariotto, Elena,Mattiuzzo, Elena,Viola, Giampietro
, p. 1274 - 1290 (2019/01/30)
The clinical evidence for the success of tyrosine kinase inhibitors in combination with microtubule-targeting agents prompted us to design and develop single agents that possess both epidermal growth factor receptor (EGFR) kinase and tubulin polymerization inhibitory properties. A series of 6-aryl/heteroaryl-4-(3′,4′,5′-trimethoxyanilino)thieno[3,2-d]pyrimidine derivatives were discovered as novel dual tubulin polymerization and EGFR kinase inhibitors. The 4-(3′,4′,5′-trimethoxyanilino)-6-(p-tolyl)thieno[3,2-d]pyrimidine derivative 6g was the most potent compound of the series as an antiproliferative agent, with half-maximal inhibitory concentration (IC50) values in the single- or double-digit nanomolar range. Compound 6g bound to tubulin in the colchicine site and inhibited tubulin assembly with an IC50 value of 0.71 μM, and 6g inhibited EGFR activity with an IC50 value of 30 nM. Our data suggested that the excellent in vitro and in vivo profile of 6g may be derived from its dual inhibition of tubulin polymerization and EGFR kinase.
INDOLYLALKYLTHIENOPYRIMIDYLAMINES AS MODULATORS OF THE EP2 RECEPTOR
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Page/Page column 32; 34, (2009/03/07)
The present invention relates to indolylalkylthienopyhmidylamines of the general formula (I), to processes for their preparation and to their use for production of pharmaceutical compositions for treatment of disorders and indications connected to the EP2
THIENOPYRIMIDYLAMINES AS MODULATORS OF THE EP2 RECEPTOR
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Page/Page column 33, (2009/03/07)
The present invention relates to thienopyrimidylamines of the general formula (I), to processes for their preparation and to their use for production of pharmaceutical compositions for treatment of disorders and indications connected to the EP2
Synthesis of thiazolidinones and azetidinones from hydrazino thieno [3,2-d]pyrimidines as potential antimicrobial agents
Shah, Manish,Parikh, Khyati,Parekh, Hansa
, p. 73 - 77 (2007/10/03)
4-Hydrazino-6-phenylthieno [3,2-d] pyrimidine 5 on treatment with aromatic aldehydes yield 4-substituted-benzalhydrazino-6-phenylthieno [3,2-d] pyrimidine 6a-k, which on cyclisation with thioglycolic and thiolactic acid afford corresponding 2-aryl-3-N-(6′
