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Dimethyl acetylenedicarboxylate, ethyl propiolate, and E-dibenzoylethylene react with thienopyrimidines (cyclo-pentyl, -hexyl, and -heptyl) derivatives to form thiazolo[3,2-a]thieno-[2,3-d]pyrimidin-2-ylidene) acetates, thieno[2,3-d]pyrimidin-2-ylthioacrylates, and thieno[2',3':4,5]pyrimido[2,1-b][1,3]thiazin-6-ones, respectively. Reactions proceed via cyclization and thio-addition processes. Some derivatives of thienopyrimidines showed high inhibition of Hep-G2 cell growth compared with the growth of untreated control cells. However, the fused heptyl of thienopyrimidothiazines indicates a promising specific antitumor agent against Hep-G2 cells with IC(50 )< 20 microM.
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http://dx.doi.org/10.1002/ardp.200900245 | DOI Listing |
RSC Adv
August 2025
Department of Chemistry, Payame Noor University 19395-4697 Tehran Iran +98 25 3717 9170 +98 25 3717 9170.
This paper describes the design and fabrication of a Ni/Arg@zeolite-Y nanocomposite, and investigates its application as a multifunctional nanocatalyst in the one-pot synthesis of thieno[2,3-]pyrimidinone derivatives. Herein, nickel metal ions were stabilized on NaY zeolite through a sodium exchange process (Ni@zeolite-Y). Then, this catalyst was functionalized the linker 3-chloropropyltriethoxysilane with the basic l-arginine amino acid (Arg@zeolite-NiY).
View Article and Find Full Text PDFEur J Med Chem
November 2016
Cardiff School of Pharmacy and Pharmaceutical Sciences, Cardiff, King Edward VII Avenue, Cardiff, CF103NB, UK.
A structure-based virtual screening technique was applied to the study of the HCV NS3 helicase, with the aim to find novel inhibitors of the HCV replication. A library of ∼450000 commercially available compounds was analysed in silico and 21 structures were selected for biological evaluation in the HCV replicon assay. One hit characterized by a substituted thieno-pyrimidine scaffold was found to inhibit the viral replication with an EC50 value in the sub-micromolar range and a good selectivity index.
View Article and Find Full Text PDFBioorg Med Chem Lett
January 2009
Discovery Chemistry, Research Center, Roche, Nutley, NJ 07110, USA.
Cdc7 kinase plays a critical role in the regulation of DNA replication in eukaryotic cells and has been proposed as a target for cancer therapy. We have identified a class of Cdc7/Dbf4 inhibitors with a pyrido-thieno-pyrimidine core structure. Synthesis of a focused pyrido-thieno-pyrimidine library yielded potent and selective Cdc7 inhibitors with antiproliferative activity against cancer cells in vitro.
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