137446-90-3Relevant academic research and scientific papers
Glucopyranosides derived from 6-aryl-5-cyano-2-(methylthio)pyrimidin-4(3H)ones
Abdou, Ibrahim M.,Attia, Adel M.,Strekowski, Lucjan
, p. 15 - 21 (2002)
The reaction of 2,3,4,6-tetra-O-acetyl-α-D-glucopyranosyl bromide with a 6-aryl-5-cyano-2-(methylthio)pyrimidin-4(3H)one in aqueous acetone in the presence of KOH furnishes a 4-(β-D-glucopyranosyloxy)pyrimidine and a 3-(β-D-glucopyranosyl)pyrimidine as the major and minor product, respectively.
Design, Synthesis and Antibacterial Activity of Novel Pyrimidine-Containing 4H-Chromen-4-One Derivatives**
Chen, Mei,He, Ming,Liu, Tingting,Peng, Feng,Su, Shijun,Tang, Xuemei,Xie, Chengwei,Xue, Wei,Zhan, Wenliang,Zhou, Qing
, (2021/07/12)
A series of pyrimidine-containing 4H-chromen-4-one derivatives were designed and synthesized by combining bioactive substructures. Preliminary biological activity results showed that most of the compounds displayed significant inhibitory activities in vit
Synthesis and in vitro investigation of novel cytotoxic pyrimidine and pyrazolopyrimidne derivatives showing apoptotic effect
Arafa, Reem K.,Maher, Ahmed,Nissan, Yassin M.,Ragab, Fatma A.,Seif, Emad M.
, (2020/02/11)
A series of novel derivatives of hydrazinylpyrimidines, pyrazolylpyrimidines and 3-amino[3,4-d]pyrazolopyrimidines have been synthesized and tested for their in vitro cytotoxic activity against 60 tumor cell lines by NCI. The in vitro cytotoxic IC50 values for the most active compounds were determined against the colon-KM12 cell line (5d, 7c and 7d), breast-MCF-7 (6a) and melanoma-MDA-MB-435 (6h) using 5-fluorouracil (5-FU) as a positive control. Derivatives 5d and 7c were found to be the most potent derivatives against KM12 cell line (IC50 = 1.73 and 1.21 μM, respectively) with a high selectivity index (SI) (18.82 and 35.49, respectively) compared to 5-FU (IC50 = 12.26 μM, SI = 1.93). Compounds 5d and 7c were further investigated for their apoptotic behavior in KM12 cell line. The investigations showed the up-regulation of caspase 3/9 and the pro-apoptotic factor Bax. On the other hand, the expression of the anti-apoptotic factor Bcl-2, was down-regulated, as well as its inhibition at a nanomolar concentration. Furthermore, the apoptotic effect for derivatives 5d and 7c in KM12 cells was detected using annexin V-FITC staining method.
Substituted pyrimidine-containing myricetin derivative as well as preparation method and application thereof
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Paragraph 0029; 0034-0035; 0128; 0134-0135, (2020/12/05)
The invention discloses a substituted pyrimidine-containing myricetin derivative as well as a preparation method and application thereof. The general structural formula of the myricetin derivative isshown in the specification, R represents a substituted phenyl group or a substituted aromatic heterocyclic group; n is the number of carbon in a carbon chain and is 2-6; wherein the substituted phenylgroup is on the ortho-, meta-and para- position of a benzene ring and contains C1-6 alkyl groups, C1-6 alkoxyl groups, nitro groups, halogen atoms and hydrogen atoms; the aromatic heterocyclic groupis thienyl, furyl, pyrrolyl or pyridyl; and substituent groups on substituted aromatic heterocycle are ortho-, meta-and para- positions and contain C1-6 alkyl groups, C1-6 alkoxyl groups, nitro groups, halogen atoms and hydrogen atoms. The derivative can well inhibit the activity of pathogenic bacteria of plants.
Synthesis, molecular modeling, and biological evaluation of novel benzimidazole derivatives as inhibitors of hepatitis C virus RNA replication
El Diwani, Hoda Ibrahim,Abdel-Mohsen, Heba Tawfik,Salama, Ismail,Ragab, Fatma Abdel-Fattah,Ramla, Mostafa Mahmoud,Galal, Shadia Ahmed,Abdalla, Mohamed Mostafa,Abdel-Wahab, Abeer,El Demellawy, Maha Adel
, p. 856 - 866 (2015/02/19)
In this study, synthesis and docking studies of a series of new benzimidazole derivatives linked to substituted pyrimidines either through the methylenethio linkage or its bioisosteric methylene amino bridge were carried out. All the synthesized compounds were evaluated for their hepatitis C virus (HCV) RNA replication-inhibitory activity. Compounds 4d, 4f, and 4h were found to be more potent than VX-950 (IC50/90of 4d=0.123/0.321, 4f=0.145/0.345, 4h=0.129/0.432, VX-950=0.20/0.45μM, respectively) and 6d (IC50/90=0.116/0.452μM) displayed activity very similar to that of the standard. Compounds 4d, 4f, 4h, and 6d were potent HCV RNA replication inhibitors and are good drug candidates for further investigations.
Synthesis, biological evaluation and molecular docking studies of some pyrimidine derivatives
Fargualy, Ahmed M.,Habib, Nargues S.,Ismail, Khadiga A.,Hassan, Ahmed M. M.,Sarg, Marwa T. M.
, p. 276 - 295 (2013/10/01)
Some novel pyrimidine-5-carbonitrile derivatives bearing various substituent have been synthesized. The structures of target compounds were confirmed by elemental analysis and spectral data. Some selected members of the newly synthesized compounds were investigated for their cytotoxic potency against certain human tumor cell lines. Five representative active anticancer compounds 6a, 6c, 6d, 17a and 18a were subjected to docking using MOE program on the 3D structure of two enzymes, namely; thymidylate synthase and dihydrofolate reductase. The antimicrobial activities of the synthesized compounds were tested against Staphylococcus aureus, Pseudomonas aeruginosa, Shigella flexneri and Candida albicans. Compounds 2c, 7a and 9c showed broad spectrum antimicrobial activity.
Novel dihydropyrimidines and its pyrazole derivatives: Synthesis and pharmacological screening
Ramesh,Bhalgat, Chetan M.
experimental part, p. 1882 - 1891 (2011/05/06)
In the present study, we have synthesized novel dihydropyrimidines (1a-j), their dimethylated adducts (2a-j), and hydrazine derivatives (3a-j) of 2a-j and subsequently their pyrazole derivatives (4a-j). Elemental analysis, IR, 1H NMR and mass s
Synthesis of some new pyrimidine and fused pyrimidine derivatives (part I)
Ahmed, Gamal A.,El-Bahai, Said,Nasser,El-Salam, M. Abd
, p. 72 - 75 (2007/10/03)
2-Hydroxy- and 2-Mercapto-3,4-dihydro-4-oxo-6-(furyl)-Pyrimidine-5-carbonitriles (3a,b) were synthesized by two different routes. Methylation of 3a with methyl iodide gave the S-methyl derivative 4, which could also be prepared by two other different meth
