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 published an article on February 14 ,2019. The article was titled 《Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2-d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors》, and you may find the article in Journal of Medicinal Chemistry.HPLC of Formula: 169759-79-9 The information in the text is summarized as follows:
The clin. 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 I 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 I bound to tubulin in the colchicine site and inhibited tubulin assembly with an IC50 value of 0.71 μM, and I inhibited EGFR activity with an IC50 value of 30 nM. Our data suggested that the excellent in vitro and in vivo profile of I may be derived from its dual inhibition of tubulin polymerization and EGFR kinase. The experimental process involved the reaction of Methyl 4-amino-[2,2′-bithiophene]-5-carboxylate(cas: 169759-79-9HPLC of Formula: 169759-79-9)
Methyl 4-amino-[2,2′-bithiophene]-5-carboxylate(cas: 169759-79-9) belongs to anime. Amine, any member of a family of nitrogen-containing organic compounds that is derived, either in principle or in practice, from ammonia (NH3). Naturally occurring amines include the alkaloids, which are present in certain plants; the catecholamine neurotransmitters (i.e., dopamine, epinephrine, and norepinephrine); and a local chemical mediator, histamine, that occurs in most animal tissues.HPLC of Formula: 169759-79-9
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