Category Ranking

98%

Total Visits

921

Avg Visit Duration

2 minutes

Citations

20

Article Abstract

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.

Download full-text PDF

Source
http://dx.doi.org/10.1002/ardp.200900245DOI Listing

Publication Analysis

Top Keywords

thieno[23-d]pyrimidines synthesis
4
synthesis antitumor
4
antitumor antioxidant
4
antioxidant agents
4
agents dimethyl
4
dimethyl acetylenedicarboxylate
4
acetylenedicarboxylate ethyl
4
ethyl propiolate
4
propiolate e-dibenzoylethylene
4
e-dibenzoylethylene react
4

Similar Publications

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 PDF

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 PDF

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.

View Article and Find Full Text PDF