Search results for "4-E]ISOINDOLE"

showing 5 items of 5 documents

[1,2]Oxazolo[5,4-e]isoindoles as promising tubulin polymerization inhibitors

2016

Abstract A series of [1,2]Oxazolo [5,4- e ]isoindoles has been synthesized through a versatile and high yielding sequence. All the new structures showed in the 1 HNMR spectra, the typical signal in the 8.34–8.47 ppm attributable to the H-3 of the [1,2]oxazole moiety. Among all derivatives, methoxy benzyl substituents at positions 3 and 4 or/and 5 were very effective in reducing the growth of different tumor cell lines, including diffuse malignant peritoneal mesothelioma (DMPM), an uncommon and rapidly malignancy poorly responsive to available therapeutic options. The most active compound 6j was found to impair tubulin polymerization, cause cell cycle arrest at G2/M phase and induce apoptosi…

0301 basic medicineCell cycle checkpointIsoindoles2]Oxazolo[5StereochemistryDiffuse malignant peritoneal mesotheliomaα-hydroxyalkyl ketonesAntineoplastic AgentsApoptosisIsoindoles01 natural sciencesTubulin Polymerization Inhibitors03 medical and health scienceschemistry.chemical_compoundIsomerismTubulinCell Line TumorDrug DiscoveryHumansMoietyProtein Structure QuaternaryOxazole[12]Oxazolo[54-e]isoindolePharmacology010405 organic chemistryChemistryAntitubulin agentsDrug Discovery3003 Pharmaceutical ScienceOrganic ChemistryGeneral MedicineSettore CHIM/08 - Chimica FarmaceuticaTubulin Modulators0104 chemical sciencesAntitubulin agentG2 Phase Cell Cycle Checkpointsα-hydroxyalkyl ketone030104 developmental biologyApoptosisActive compound4-e]isoindolesProton NMRM Phase Cell Cycle CheckpointsAntitubulin agents; Diffuse malignant peritoneal mesothelioma; [1; 2]Oxazolo[5; 4-e]isoindoles; α-hydroxyalkyl ketones; Pharmacology; Drug Discovery3003 Pharmaceutical Science; Organic Chemistry[1Drug Screening Assays AntitumorProtein Multimerization
researchProduct

Isoxazolo[5,4-e]isoindole a new ring system with potent antitumor activity

2011

4-e]isoindoleIsoxazolo[5; 4-e]isoindole; Combretastatin; antitumor agentsCombretastatinIsoxazolo[5antitumor agentsIsoxazolo[54-e]isoindole Combretastatin antitumor agents
researchProduct

Evaluation of [1,2]oxazolo[5,4-e]isoindoles in lymphoma cells

2020

Anti-tubulin agents are important chemotherapeutics. Combretastatin A-4 (CA-4) emerged as lead compound for the design of new tubulin-binding agents. Its analogues 4,5-diarylisoxazoles, containing the [1,2]oxazole ring as linker of two aryl moieties, displayed higher antitubulin activity than CA-4. [1,2]oxazolo[5,4-e]isoindoles also gave excellent results reducing cell growth of NCI-60 tumor cell lines and diffuse malignant peritoneal mesothelioma (DMPM) cells. Selected derivatives showed in vivo antitumor activity at well-tolerated doses in a DMPM xenograft model. [1,2]oxazolo[5,4-e]isoindoles were screened in four lymphoma histotypes: germinal center B-cell and activated diffuse large B c…

Cancer ResearchOncologyIsoindolesChemistryCancer researchmedicineanti-tubulin agent[12]oxazolo[54-e]isoindolelymphoma histotypemedicine.diseaseSettore CHIM/08 - Chimica FarmaceuticaLymphomaEuropean Journal of Cancer
researchProduct

ISOXAZOLO[5,4-E]ISOINDOLE: A NEW RING SYSTEM WITH POTETIAL PHOTOBIOLOGICAL PROPERTIES

2008

ISOXAZOLO[54-E]ISOINDOLESettore CHIM/08 - Chimica Farmaceutica
researchProduct

Development of [1,2]oxazoloisoindoles tubulin polymerization inhibitors: Further chemical modifications and potential therapeutic effects against lym…

2022

Lymphomas are among the ten most common cancers, and, although progress has been achieved in increasing survival, there is still an unmet need for more effective therapeutic approaches, including better options for patients with refractory tumors that initially respond but then relapse. The lack of effective alternative treatment options highlights the need to develop new therapeutic strategies capable of improving survival prospects for lymphoma patients. Herein, we describe the identification and exploration of the SAR of a series of [1,2]oxazolo[5,4-e]isoindoles as potent small molecules that bind to the colchicine site of tubulin and that have promise for the treatment of refractory lym…

PharmacologyBinding SitesLymphomaAntitubulin agentsColchicine siteOrganic ChemistryAntineoplastic AgentsGeneral MedicineIsoindolesTubulin ModulatorsT2R-TTL–ComplexesStructure-Activity RelationshipTubulinNeoplasmsCell Line TumorDrug DiscoveryHumans[12]oxazolo[54-e]isoindolesColchicineX-ray crystallographyEuropean Journal of Medicinal Chemistry
researchProduct