Search results for "ISOINDOLO-QUINOXALINE"

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ISOINDOLO-QUINOXALINE DERIVATIVES HAVING ANTITUMOR ACTIVITY, PROCESS FOR THEIR PRODUCTION AND THEIR USE

2008

New isoindolo[2,1-a]quinoxaline derivatives of general formula (1 ), wherein R represents H or OH and R5 represents H or CN, have been prepared with simple procedures starting from known intermediates and resulted to posses potent in vitro antitumor activity against a panel of about 60 different human tumor cell lines belonging to several kinds of tumors, both hematological and solid. Preparations containing such derivatives as active ingredients are proposed as drugs to be employed in cancer therapy both alone and in combination with other chemotherapeutics.

ISOINDOLO-QUINOXALINE ANTITUMOR ACTIVITYSettore CHIM/08 - Chimica Farmaceutica
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Aza-isoindolo and isoindolo-azaquinoxaline derivatives with antiproliferative activity

2015

Abstract Three new ring systems, pyrido[2′,3′:3,4]pyrrolo[1,2- a ]quinoxalines, pyrido[3′,2′:3,4]pyrrolo[1,2- a ]quinoxalines and pyrido[2′,3′:5,6]pyrazino[2,1- a ]isoindoles, were synthesized through an aza-substitution on the already active isoindolo-quinoxaline system and in particular in the position 7 or 4 of the isoindole moiety and in position 5 of the quinoxaline portion. All new compounds were screened by the National Cancer Institute (Bethesda, MD) against a panel of 60 human tumor cell lines. Biological results of the most active derivatives, with pGI 50 values between 7.09 and 7.27, confirmed the importance of the presence of methoxy substituents for biological activity. The ant…

QuinoxalineIsoindolesAzaisoindolo-quinoxalinesStereochemistryAntiproliferative activity; Apoptosis; Azaisoindolo-quinoxalines; DNA interaction; Isoindolo-azaquinoxalines; Quinoxalines; Antineoplastic Agents; Apoptosis; Aza Compounds; Cell Line Tumor; Cell Proliferation; Dose-Response Relationship Drug; Drug Screening Assays Antitumor; Humans; Isoindoles; Molecular Structure; Quinoxalines; Structure-Activity Relationship; Drug Discovery3003 Pharmaceutical Science; Organic Chemistry; Pharmacology; Medicine (all)ApoptosisAntineoplastic AgentsAntiproliferative activityIsoindolesRing (chemistry)Drug Screening AssaysCell LineDose-Response Relationshipchemistry.chemical_compoundStructure-Activity RelationshipQuinoxalineCell Line TumorQuinoxalinesDrug DiscoverymedicineMoietyHumansAntiproliferative activity; Apoptosis; Azaisoindolo-quinoxalines; DNA interaction; Isoindolo-azaquinoxalines; Quinoxalines; Drug Discovery3003 Pharmaceutical Science; Organic Chemistry; PharmacologyCell ProliferationPharmacologyAza CompoundsAzaisoindolo-quinoxalineTumorDose-Response Relationship DrugMolecular StructureDrug Discovery3003 Pharmaceutical ScienceMedicine (all)Organic ChemistryApoptosiBiological activityGeneral MedicineAntitumorCell cycleSettore CHIM/08 - Chimica FarmaceuticaDNA interactionSettore ING-IND/22 - Scienza E Tecnologia Dei MaterialiMechanism of actionchemistryIsoindolo-azaquinoxalineDrug Screening Assays Antitumormedicine.symptomDrugIsoindoleIsoindolo-azaquinoxalines
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