23121-14-4Relevant academic research and scientific papers
Design and synthesis of pyrazolo[3,4-d]pyrimidines: Nitric oxide releasing compounds targeting hepatocellular carcinoma
Elshaier, Yaseen A.M.M.,Shaaban, Mohamed A.,Abd El Hamid, Mohammed K.,Abdelrahman, Mostafa H.,Abou-Salim, Mahrous A.,Elgazwi, Sara M.,Halaweish, Fathi
, p. 2956 - 2970 (2017/05/24)
A new series of pyrazolo[3,4-d]pyrimidines tethered with nitric oxide (NO) producing functionality was designed and synthesized. Sulforhodamine B (SRB) protein assay revealed that NO releasing moiety in the synthesized compounds significantly decreased the cell growth more than the des-NO analogues. Compounds 7C and 7G possessing N-para-substituted phenyl group, released the highest NO concentration of 4.6% and 4.7% respectively. Anti-proliferative activity of synthesized compounds on HepG2 cell line identified compounds 7h, 7p, 14a and 14b as the most cytotoxic compounds in the series of IC50?=?3, 5, 3 and 5?μM, respectively, compared to erlotinib as a reference drug (IC50?=?25?μM). Flow cytometry studies revealed that 7?h arrested the cells in G0/G1 phase of cell cycle while 7p arrested the cells in S phase. Moreover, docking study of the synthesized compounds on EGFR (PDB code: 1M17) and cytotoxicity study indicated that N-1 phenyl para substitution, pyrazole C-3 alkyl substitution and tethering the nitrate moiety through butyl group had a significant impact on the activity.
Synthesis of novel 2-alkyl-4-substituted-amino-pyrazolo[3,4-d]pyrimidines as new leads for anti-bacterial and anti-cancer activity
Devarakonda, Murty,Doonaboina, Raghava,Vanga, Sreedher,Vemu, Jahnavi,Boni, Sathoshini,Mailavaram, Raghu Prasad
, p. 1090 - 1101 (2013/04/10)
Treatment of 6-alkyl-1-phenyl-4-chloro-(1H)-pyrazolo[3,4-d]pyrimidines, with different amines afforded a series of compounds whose identity and purity were confirmed by spectral and analytical means. The compounds were tested for antibacterial activity against four organisms viz. Staphylococcus aureus (Gram positive), S. epidermidis (Gram positive), Bacillus subtilis (Gram positive), Escherichia coli (Gram negative) using amoxicillin as standard control. Compounds 4d, 6b, 6c have shown best antibacterial activity in the series. The antiproliferative activity was tested against human skin cancer cell line G361. The compounds 3d, 4d, 5b, 5d, 5e, 6c, 7a were found to be the best of the series and showed the activity at micromolar concentration.
PYRAZOLO-PYRIMIDINE ANILINE COMPOUNDS
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Page 37; 38, (2010/02/05)
Compounds having the formula (I), where all substituents are as defined herein, and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors.
Preparation of Heteroarenecarbonitriles by Reaction of Haloheteroarenes with Potassium Cyanide Catalyzed by Sodium p-Toluenesulfinate
Miyashita, Akira,Suzuki, Yumiko,Ohta, Kiyono,Higashino, Takeo
, p. 345 - 356 (2007/10/02)
Several heteroarenecarbonitriles were prepared by reaction of haloheteroarenes with potassium cyanide catalyzed by sodium p-toluenesulfinate (1) or sodium methanesulfinate (2).In the reaction pathway, the cyanation proceeds through the formation of the su
