Search results for "4-d]pyrimidine"

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Pyrazole[3,4-d]pyrimidine derivatives loaded into halloysite as potential CDK inhibitors

2021

Uncontrolled cell proliferation is a hallmark of cancer as a result of rapid and deregulated progression through the cell cycle. The inhibition of cyclin-dependent kinases (CDKs) activities is a promising therapeutic strategy to block cell cycle of tumor cells. In this work we reported a new example of nanocomposites based on halloysite nanotubes (HNTs)/pyrazolo[3,4-d]pyrimidine derivatives (Si306 and Si113) as anticancer agents and CDK inhibitors. HNTs/Si306 and HNTs/Si113 nanocomposites were synthesized and characterized. The release kinetics were also investigated. Antitumoral activity was evaluated on three cancer cell lines (HeLa, MDA-MB-231 and HCT116) and the effects on cell cycle ar…

Cell cycle checkpointPyrimidinePharmaceutical Science02 engineering and technologyCDK inhibitors; Halloysite; Nanocomposites; Pyrazolo[34-d]pyrimidine derivatives; Cell Cycle Checkpoints; Cell Line Tumor; Clay; Humans; Pyrazoles; PyrimidinesPyrazolo[34-d]pyrimidine derivativesPyrazole030226 pharmacology & pharmacyCell LineNanocompositesHeLa03 medical and health scienceschemistry.chemical_compound0302 clinical medicineCyclin-dependent kinaseCell Line TumorPyrazolo[3HumansSettore BIO/06 - Anatomia Comparata E CitologiaSettore CHIM/02 - Chimica FisicaTumorbiologyChemistryKinaseCell growth4-d]pyrimidine derivativesHalloysiteSettore CHIM/06 - Chimica OrganicaCell Cycle CheckpointsCell cycle021001 nanoscience & nanotechnologybiology.organism_classificationSettore BIO/18 - GeneticaPyrimidinesSettore CHIM/03 - Chimica Generale E Inorganicabiology.proteinCancer researchClayPyrazoles0210 nano-technologyCDK inhibitors
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Pyrazolo[3,4-d]pyrimidine derivatives as COX-2 selective inhibitors: synthesis and molecular modelling studies.

2009

The pyrazolo[3,4-d]pyrimidine system shows a multitude of interesting pharmacological properties. Owing to the potential anti-inflammatory activity of 5-benzamido-pyrazolo[3,4-d]pyrimidin- 4-one derivatives and considering the easy synthesis of this class of compounds, a set of new 5- benzamido-1H-pyrazolo[3,4-d]pyrimidin-4-ones has been prepared in 42-80% yields by reacting 5- aminopyrazole-4(N-benzoyl)carbohydrazide derivatives and the opportune triethylorthoesters. Compounds 8a, b, 10a–d, and 11a, b revealed a superior inhibitory profile against COX-2, when compared to that of reference standards NS398 and indomethacin. Molecular modelling studies confirmed the obtained biological result…

Models MolecularSulfonamidesSheepCyclooxygenase 2 InhibitorsIndomethacinAnti-Inflammatory AgentsSettore CHIM/08 - Chimica FarmaceuticaStructure-Activity Relationship4(3H)-QuinazolinonePyrimidinesDocking Pyrazolo[34-d]pyrimidineCyclooxygenase 1AnimalsHumansPyrazolesComputer SimulationCOX-2 inhibitorNitrobenzenesArchiv der Pharmazie
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