1374641-91-4Relevant academic research and scientific papers
Synthesis of various fused pyrimidine rings and their pharmacological and antimicrobial evaluation
Salem, Mounir A.,Marzouk, Magda I.,Mahmoud, Naglaa F.
, p. 1059 - 1073 (2014)
Various fused pyrimidines, such as furo[2,3-d]pyrimidine, triazolo- [1,5-a]pyrimidine and tetrazolo[1,5-a]pyrimidine, were synthesized in the reactions of thioxopyrimidine-6(1H)-ones with ethyl chloroacetate (under different reaction conditions), thiourea and sodium nitrite. Pyrimidine thiones reacted with POCl3/PCl5 to give the chloro derivatives which reacted with sodium azide and thiourea to give tetrazolo[1,5-c]pyrimidines, and pyrimido pyrimidines. Thioxopyrimidine-6(1H)-ones reacted with benzylamine to give pyrrolo[2,3-d]pyrimidinethiones. Theoretical calculation using MIDO/3, Fukui indices and the heat of formation of some compounds were carried out. The pharmacological and antimicrobial activities of some of the synthesized products were also evaluated.
Novel 2-thiopyrimidine derivatives as CDK2 inhibitors: Molecular modeling, synthesis, and anti-tumor activity evaluation
Fathalla, Omar Abd El-Fattah M.,Ismail, Mohamed A. H.,Anwar, Manal M.,Abouzid, Khaled A. M.,Ramadan, Aisha A. K.
, p. 659 - 673 (2013/04/10)
A novel series of pyrimidine-benzenesulfonamide derivatives as potential cyclin-dependent kinase 2 inhibitors were designed depending upon the molecular docking simulation study. This study was preceded by modification and optimization of the lead compound 4-(2-amino-4-methylthiazol-5-yl)-N-(3- nitrophenyl) pyrimidin-2-amine. The target proposed compounds were synthesized using the derivative 6-(3,4-dimethoxyphenyl)-4-oxo-2-thioxo-1,2,3,4- tetrahydropyrimidine-5-carbonitrile (1) as a key starting compound. Some of the synthesized derivatives were selected as representative examples to evaluate their anti-proliferative activity against cultured human Hela cell line using doxorubicin as a reference drug and the results obtained were correlated with the data of molecular modeling simulation study. The structures of the novel derivatives were confirmed on the bases of micro-analytical and spectral data.
