Pyrazolo[3,4-d]pyrimidine based scaffold derivatives targeting kinases as anticancer agents

Ismail, Nasser S. M.; Ali, Eslam M.H.; Ibrahim, Diaa A.; Serya, Rabah A. T.; Ella, Dalal A. Abou El

doi:10.1016/j.fjps.2016.02.002

Cited by 46 publications

(29 citation statements)

References 99 publications

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“…The IR spectra (KBr) were recorded on a Perkin Elmer 1650 spectrometer (Shelton, CT, USA). 1 H-NMR and 13 C-NMR spectra were recorded on a JEOL EX-300 and JEOL ECA-500 (Shimadzu, Tokyo, Japan).…”

Section: General Informationmentioning

confidence: 99%

“…Pyrazolopyrimidines have important biological functions including herbicidal [12] and antitumor activity [13]; pyrazolopyrimidine derivatives have been found as purine analogs [14] and have significant properties as antimetabolites in purine biochemical reactions such as neuropeptide Y1 receptor antagonists [15]. Also, the pyrazolo [4,3-d]pyrimidinone class of compounds is very important in the treatment of impotence [16], used as an PDE5 inhibitor.…”

Section: Introductionmentioning

confidence: 99%

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Synthesis and Biological Evaluation of N- Pyrazolyl Derivatives and Pyrazolopyrimidine Bearing a Biologically Active Sulfonamide Moiety as Potential Antimicrobial Agent

Hafez

El‐Gazzar

2016

Molecules

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Abstract:A series of novel pyrazole-5-carboxylate containing N-triazole derivatives 3,4; different heterocyclic amines 7a-b and 10a-b; pyrazolo [4,3-d]pyrimidine containing sulfa drugs 14a,b; and oxypyrazolo [4,3-d]pyrimidine derivatives 17, 19, 21 has been synthesized. The structure of the newly synthesized compounds was elucidated on the basis of analytical and spectral analyses. All compounds have been screened for their in vitro antimicrobial activity against three gram-positive and gram-negative bacteria as well as three fungi. The results revealed that compounds 14b and 17 had more potent antibacterial activity against all bacterial strains than reference drug Cefotaxime. Moreover compounds 4, 7b, and 12b showed excellent antifungal activities against Aspergillus niger and Candida albicans in low inhibitory concentrations but slightly less than the reference drug miconazole against Aspergillus flavus.

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Section: General Informationmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Synthesis and Biological Evaluation of N- Pyrazolyl Derivatives and Pyrazolopyrimidine Bearing a Biologically Active Sulfonamide Moiety as Potential Antimicrobial Agent

Hafez

El‐Gazzar

2016

Molecules

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“…Pyrazolo [3,4-d]pyrimidine nucleus is the bioisostere of purine [4] [5], which exhibits promising activity as antitumor by competitive inhibition for ATP kinase enzymes. Many pyrazolo [3,4-d]pyrimidine derivatives were reported as antitumor agents [6] [7] [8]. The cytotoxic activity of such compound may attribute to inhibition of several enzymes such as tyrosine kinase [9], Src kinase [10], cyclin dependent kinase (CDK) [11], mammalian target of rapamycin (mTOR) [12] and glycogen synthase kinase (GSK) [13] [14].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization and <i>In Vitro</i> Antitumor Evaluation of New Pyrazolo[3,4-d]Pyrimidine Derivatives

El-Morsy¹,

Elsayed²,

Abulkhair³

2017

OJMC

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A new series of 3-(methylthio)-1-phenyl-1H-pyrazolo[3,4-d]pyrimidine derivatives was synthesized. The structures of the new derivatives were confirmed by the spectral data and elemental analyses. The antitumor activity of this series against human breast adenocarcinoma cell line MCF7 was evaluated. Out of twenty new derivatives, ten were revealed mild to moderate activity compared with doxorubicin as a reference antitumor. Among this new series N-(2-chlorophenyl)-2-(3-(methylthio)-4-oxo-1-phenyl-1H-pyrazolo[3,4-d]py rimidin-5(4H)-yl)acetamide (13 a) was found the most active one with IC 50 equal to 23 µM.

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“…Hence exhibits promising activity as antitumor by competitive inhibition for ATP kinase enzymes. Many pyrazolo [3,4-d]pyrimidine derivatives were reported as antitumor agents [6][7][8]. The cytotoxic activity of such compound may attributed to inhibition of several enzymes such as tyrosine kinase [9], Src kinase [10], cyclin dependent kinase (CDK) [11], mammalian target of rapamycin (mTOR) [12] and glycogen synthase kinase (GSK) [13,14].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization and In Vitro Antitumor Evaluation of New Pyrazolo[3,4-d]Pyrimidine Derivatives

El-Morsy¹,

Elsayed²,

Abulkhair³

2017

Organic Chem Curr Res

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Pyrazolo[3,4-d]pyrimidine based scaffold derivatives targeting kinases as anticancer agents

Cited by 46 publications

References 99 publications

Synthesis and Biological Evaluation of N- Pyrazolyl Derivatives and Pyrazolopyrimidine Bearing a Biologically Active Sulfonamide Moiety as Potential Antimicrobial Agent

Synthesis and Biological Evaluation of N- Pyrazolyl Derivatives and Pyrazolopyrimidine Bearing a Biologically Active Sulfonamide Moiety as Potential Antimicrobial Agent

Synthesis, Characterization and <i>In Vitro</i> Antitumor Evaluation of New Pyrazolo[3,4-d]Pyrimidine Derivatives

Synthesis, Characterization and In Vitro Antitumor Evaluation of New Pyrazolo[3,4-d]Pyrimidine Derivatives

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Pyrazolo[3,4-d]pyrimidine based scaffold derivatives targeting kinases as anticancer agents

Cited by 46 publications

References 99 publications

Synthesis and Biological Evaluation of N- Pyrazolyl Derivatives and Pyrazolopyrimidine Bearing a Biologically Active Sulfonamide Moiety as Potential Antimicrobial Agent

Synthesis and Biological Evaluation of N- Pyrazolyl Derivatives and Pyrazolopyrimidine Bearing a Biologically Active Sulfonamide Moiety as Potential Antimicrobial Agent

Synthesis, Characterization and &lt;i&gt;In Vitro&lt;/i&gt; Antitumor Evaluation of New Pyrazolo[3,4-d]Pyrimidine Derivatives

Synthesis, Characterization and In Vitro Antitumor Evaluation of New Pyrazolo[3,4-d]Pyrimidine Derivatives

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Synthesis, Characterization and <i>In Vitro</i> Antitumor Evaluation of New Pyrazolo[3,4-d]Pyrimidine Derivatives