6533b837fe1ef96bd12a3173
RESEARCH PRODUCT
Synthesis of Triazenoazaindoles: a New Class of Triazenes with Antitumor Activity
Paola BrunGirolamo CirrincioneFrancesco Dall'acquaAlessia SalvadorIgnazio CastagliuoloAntonina StagnoPatrizia DianaBarbara ParrinoOlaf-georg IssingerAnna CarbonePaola BarrajaDaniela Vedaldisubject
Programmed cell deathIndolesToxicology and Pharmaceutics (all)DacarbazineAntineoplastic AgentsAntiproliferative activityPharmacologyEGF receptorsDrug Screening AssaysBiochemistryCell LineFlow cytometryCell Line TumorNeoplasmsDrug DiscoveryTriazenoazaindolemedicineHumansTriazeno derivativesGeneral Pharmacology Toxicology and PharmaceuticsCytotoxicityPharmacologyAntitumor agentsTumorEpidermal Growth Factormedicine.diagnostic_testChemistryMelanomaOrganic ChemistryCancerAntitumorTriazenoazaindoles; Dacarbazine; Antitumor Activitymedicine.diseaseErbB ReceptorsDacarbazineApoptosisCell cultureMolecular MedicineDrug Screening Assays AntitumorAntitumor ActivityTriazenesTriazenoazaindolesAntiproliferative activity; Antitumor agents; EGF receptors; Triazeno derivatives; Antineoplastic Agents; Cell Line Tumor; Dacarbazine; Drug Screening Assays Antitumor; Humans; Indoles; Neoplasms; Receptor Epidermal Growth Factor; Triazenes; Pharmacology Toxicology and Pharmaceutics (all); Organic Chemistry; Molecular MedicineReceptormedicine.drugdescription
Despite improvements in the treatment and prevention of cancer, the number of new diagnoses continues to rise; this has fuelled substantial interest in the development of new and effective chemotherapeutic agents. Compounds of the triazene class, such as dacarbazine, have been used in the clinical management of many cancer types including brain, leukemia, and melanoma. A new compound class bearing a triazenoazaindole scaffold was synthesized with the aim of identifying new antiproliferative agents. Compounds 5 a-g and 6 a-c were screened against a panel of human tumor cell lines, and two of them, 5 e and 5 f, showed cytotoxicity (GI(50) range: 2.2-8.2 μM) in all cell lines. These two compounds even maintained their cytotoxicity in some multidrug-resistant cell lines. Flow cytometry analysis demonstrated their ability to induce cell death by apoptosis with involvement of lysosomes.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2011-01-01 | ChemMedChem |