0000000000535517

AUTHOR

Annalisa Maruca

showing 2 related works from this author

Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myelo…

2022

Despite progressive advances in understanding the molecular biology of acute myeloid leukemia (AML), the conventional therapeutic approach has not changed substantially, and the outcome for most patients is poor. Thus, continuous efforts on the discovery of new compounds with improved features are required. Following a multistep sequence, we have identified a new tetracyclic ring system with strong antiproliferative activity towards several haematological cell lines. The new compounds possess structural properties typical of inactive-state-binding kinase inhibitors and are structurally related to quizartinib which is known as type-II tyrosine kinase inhibitor. In particular, the high activi…

PharmacologyFMS-like tyrosine kinase 3 (FLT3)FLT3/ITD3][13]thiazolo[4Organic Chemistry2H-imidazo [2′1':23][13]thiazolo[45-e]isoindol-8-yl-phenylureas2H-imidazo [2′1':23][13]thiazolo[45-e]isoindol-8-yl-phenylureas; Acute myeloid leukemia (AML); FLT3/ITD; FMS-like tyrosine kinase 3 (FLT3); Internal tandem duplication (ITD)ApoptosisGeneral Medicine2H-imidazo [2′Leukemia Myeloid AcuteMiceInternal tandem duplication (ITD)fms-Like Tyrosine Kinase 35-e]isoindol-8-yl-phenylureasCell Line TumorDrug DiscoveryMutationAcute myeloid leukemia (AML)AnimalsHumansProtein Kinase Inhibitors1':2European journal of medicinal chemistry
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The New Microtubule-Targeting Agent SIX2G Induces Immunogenic Cell Death in Multiple Myeloma

2022

Microtubule-targeting agents (MTAs) are effective drugs for cancer treatment. A novel diaryl [1,2]oxazole class of compounds binding the colchicine site was synthesized as cis-restricted-combretastatin-A-4-analogue and then chemically modified to have improved solubility and a wider therapeutic index as compared to vinca alkaloids and taxanes. On these bases, a new class of tricyclic compounds, containing the [1,2]oxazole ring and an isoindole moiety, has been synthetized, among which SIX2G emerged as improved MTA. Several findings highlighted the ability of some chemotherapeutics to induce immunogenic cell death (ICD), which is defined by the cell surface translocation of Calreticulin (CAL…

Antineoplastic AgentsPemetrexedIsoindolesMicrotubulescancer treatmentCatalysisInorganic ChemistryAdenosine TriphosphateCell Line Tumorimmunogenic cell deathHumansPhysical and Theoretical ChemistryOxazolesVinca AlkaloidsMolecular BiologySpectroscopyOrganic ChemistryICD inducersGeneral MedicineComputer Science Applicationsmultiple myelomaMTAscancer treatment; immunogenic cell death; ICD inducers; MTAs; multiple myelomaTaxoidsCalreticulinColchicineInternational Journal of Molecular Sciences
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