Synthesis of 5-substituted-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one analogs and their biological evaluation as anticancer agents: mTOR inhibitors.

doi:10.1016/j.ejmech.2014.04.051

Paper

Synthesis of 5-substituted-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one analogs and their biological evaluation as anticancer agents: mTOR inhibitors.

Published Jun 10, 2014 · G. L. Reddy, S. Guru, M. Srinivas

European journal of medicinal chemistry

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33

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Abstract

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Study Snapshot

The developed microwave-assisted strategy for synthesis of 5-substituted-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones shows promising anticancer activity through apoptosis and mTOR inhibition.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Synthesis of 5-substituted-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one analogs and their biological evaluation as anticancer agents: mTOR inhibitors.

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References

Synthesis of imine-pyrazolopyrimidinones and their mechanistic interventions on anticancer activity.

Imine-pyrazolopyrimidinones show promising in vitro anticancer activity against prostate and breast cancer cell lines, with low micromolar IC 50 values.

Medicinal attributes of pyrazolo[3,4-d]pyrimidines: a review.

Pyrazolopyrimidines show potential medicinal significance in central nervous system, cardiovascular system, cancer, and inflammation due to their biochemical and biophysical properties.

mTOR kinase structure, mechanism and regulation by the rapamycin-binding domain

The mTOR kinase is a highly restricted access protein kinase, controlled by the FKBP12-rapamycin-binding domain, which acts as a gatekeeper to regulate cell growth and is frequently deregulated in cancer.

Identification of pyrazolo-pyrimidinones as GHS-R1a antagonists and inverse agonists for the treatment of obesity

Pyazolo-pyrimidinones show potential as GHS-R1a antagonists and inverse agonists for obesity treatment, reducing food intake in mice through a mechanism involving GHS-R1a.

Anticancer activity, toxicity and pharmacokinetic profile of an indanone derivative.

Indanone 1, a gallic acid-based indanone derivative, is a safe and moderately active anticancer agent with well-tolerated pharmacokinetics in mice.

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