0000000000330929

AUTHOR

Johnny Moretto

showing 2 related works from this author

cis-Dichloroplatinum(II) complexes tethered to dibenzo[c,h][1,6]naphthyridin-6-ones: Synthesis and cytotoxicity in human cancer cell lines in vitro

2013

A novel family of cisplatin-type complexes tethered to dibenzo[c,h][1,6]naphthyridin-6-one topoisomerase inhibitor via a polymethylene chain and their nonplatinated counterparts were prepared. Their potential cytotoxicity was assessed in three human colorectal cancer cell lines HCT 116, SW480 and HT-29 and compared to the reference molecules cisplatin and oxaliplatin. Platinated compounds were poorly active whilst nonplatinated dibenzo[c,h][1,6]naphthyridin-6-one moieties exhibited higher cytotoxic properties than cisplatin and oxaliplatin whatever the length of the polymethylene chain; molecules containing the tri- and hexamethylene chain length were the most cytotoxic.

Organoplatinum Compoundsmedicine.drug_classStereochemistryAntineoplastic AgentsStructure-Activity RelationshipCell Line TumorDrug DiscoverymedicineHumansCytotoxic T cellMoleculeNaphthyridinesCytotoxicityCell ProliferationPharmacologyCisplatinDose-Response Relationship DrugMolecular StructureChemistryOrganic ChemistryGeneral MedicineHCT116 CellsIn vitroOxaliplatinCell cultureDrug Screening Assays AntitumorHT29 CellsTopoisomerase inhibitormedicine.drugEuropean Journal of Medicinal Chemistry
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Human-based evidence for the therapeutic potential of arginase inhibitors in cardiovascular diseases

2020

Arginase is a ubiquitous enzyme that regulates polyamine- and nitric-oxide-requiring vascular functions. It is well-established that, in mammals, arginase overactivation contributes to endothelial dysfunction, a hallmark of cardiovascular diseases. The pharmacological potential of arginase inhibition for improving vascular function is largely supported by a wide range of data from animal studies. However, caution is required before extrapolating animal data to humans because interspecies differences in arginase expression and localization have been observed. For this reason, this review presents the existing arguments from human data in favor of a role of arginase in cardiovascular diseases…

0301 basic medicine[SDV]Life Sciences [q-bio]Bioinformatics03 medical and health sciencesAnimal dataVASCULAR FUNCTIONS0302 clinical medicineDrug DiscoverymedicineHumansEnzyme InhibitorsEndothelial dysfunctionComputingMilieux_MISCELLANEOUSPharmacologyArginasebusiness.industrymedicine.disease3. Good healthArginase030104 developmental biologyCardiovascular Diseases030220 oncology & carcinogenesisEndothelium VascularAnimal studiesVascular functionbusinessDrug Discovery Today
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