0000000000471004

AUTHOR

Rosanna Filosa

0000-0003-1938-5732

showing 3 related works from this author

Scalable (Enantioselective) Syntheses of Novel 3-Methylated Analogs of Pazinaclone, (S)-PD172938 and Related Biologically Relevant Isoindolinones

2022

Herein, we report the application of an efficient and practical K2CO3 promoted cascade reaction of 2-acetylbenzonitrile in the synthesis of novel 3-methylated analogs of Pazinaclone and PD172938, belonging to isoindolinones heterocyclic class bearing a tetrasubstituted stereocenter. Organocatalytic asymmetric synthesis of the key intermediate and its transformation into highly enantioenriched 3-methylated analog of (S)-PD172938 was also developed. These achievements can be of particular interest also for medicinal chemistry, since the methyl group is a very useful structural modification in the rational design of new and more effective bioactive compounds.

heterocyclesisoindolinonesChemistry (miscellaneous)asymmetric synthesisOrganic ChemistryDrug Discoveryheterocycles; asymmetric synthesis; isoindolinonesMolecular MedicinePharmaceutical SciencePhysical and Theoretical ChemistryAnalytical ChemistryMolecules
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MicroRNA targeting by quercetin in cancer treatment and chemoprotection

2019

A growing number of evidences from clinical and preclinical studies have shown that dysregulation of microRNA (miRNA) function contributes to the progression of cancer and thus miRNA can be an effective target in therapy. Dietary phytochemicals, such as quercetin, are natural products that have potential anti-cancer properties due to their proven antioxidant, anti-inflammatory, and anti-proliferative effects. Available experimental studies indicate that quercetin could modulate multiple cancer-relevant miRNAs including let-7, miR-21, miR-146a and miR-155, thereby inhibiting cancer initiation and development. This paper reviews the data supporting the use of quercetin for miRNA-mediated chem…

0301 basic medicineAntineoplastic Agentsmedicine.disease_causeChemopreventionAntioxidants03 medical and health scienceschemistry.chemical_compound0302 clinical medicineNeoplasmsDrug DiscoverymicroRNAAnimalsHumansMedicineEpigeneticsPharmacologyDrug discoverybusiness.industryChemoprotectionCancermedicine.diseaseBiomarker (cell)MicroRNAs030104 developmental biologychemistry030220 oncology & carcinogenesisCancer researchQuercetinQuercetinbusinessCarcinogenesisBiomarkersPharmacological Research
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Dimethyl 2-(1-methyl-3-oxo-1,3-dihydroisobenzofuran-1-yl)malonate

2020

In this work we report a facile access to a 3,3-disubstituted isobenzofuranone by tandem addition/cyclization reaction to methyl 2-acetylbenzoate in the presence of dimethyl malonate, under basic conditions.

isobenzofuranoneTandem010405 organic chemistryOrganic Chemistrycascade reactions010402 general chemistry01 natural sciencesBiochemistryDimethyl malonateMedicinal chemistryquaternary carbonlcsh:QD146-1970104 chemical sciencesPhthalidechemistry.chemical_compoundMalonatechemistrylcsh:Inorganic chemistryphthalidePhysical and Theoretical ChemistryQuaternary carbon
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