0000000000134678

AUTHOR

Giancarlo Grossi

showing 3 related works from this author

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
researchProduct

Synthesis of (E)- and (Z)-29-methylidyne-2,3-oxidosqualene derivatives as inhibitors of liver and yeast oxidosqualene cyclase

2002

The synthesis of (E)- and (Z)-29-methylidyne-2,3-oxidosqualene derivatives is described starting from the C22 and C17 squalene aldehyde monobromohydrins. The conversion was achieved by means of a Wittig reaction, followed by desilylation of the terminal acetylene. For trisubstituted 1,3-enynes, preliminary alkylation with a suitable allyl bromide was performed. A new procedure for the synthesis of squalene aldehyde C27, C22 and C17 monobromohydrins is also described. Some of the new compounds behaved as inhibitors of pig liver and yeast oxidosqualene cyclase and were time-dependent inhibitors of the animal enzyme.

chemistry.chemical_classificationAllyl bromideoxidosqualene derivatives; oxidosqualene cyclase; squaleneStereochemistryAlkylationsqualeneAldehydeYeast23-Oxidosqualenechemistry.chemical_compoundSqualeneEnzymechemistryWittig reactionoxidosqualene cyclaselipids (amino acids peptides and proteins)oxidosqualene derivatives
researchProduct

ChemInform Abstract: Synthesis of (E)- and (Z)-29-Methylidyne-2,3-oxidosqualene Derivatives as Inhibitors of Liver and Yeast Oxidosqualene Cyclase.

2010

The synthesis of (E)- and (Z)-29-methylidyne-2,3-oxidosqualene derivatives is described starting from the C22 and C17 squalene aldehyde monobromohydrins. The conversion was achieved by means of a Wittig reaction, followed by desilylation of the terminal acetylene. For trisubstituted 1,3-enynes, preliminary alkylation with a suitable allyl bromide was performed. A new procedure for the synthesis of squalene aldehyde C27, C22 and C17 monobromohydrins is also described. Some of the new compounds behaved as inhibitors of pig liver and yeast oxidosqualene cyclase and were time-dependent inhibitors of the animal enzyme.

chemistry.chemical_classificationAllyl bromideStereochemistryGeneral MedicineAlkylationAldehydeYeast23-Oxidosqualenechemistry.chemical_compoundSqualeneEnzymechemistryWittig reactionlipids (amino acids peptides and proteins)ChemInform
researchProduct